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  1. 誘導(dǎo)疾病模型產(chǎn)品 PROTAC Immunology/Inflammation Anti-infection
  2. 泌尿系統(tǒng)疾病模型 五官類疾病模型 Molecular Glues Complement System Antibiotic Cyclophilin
  3. Cyclosporin A

Cyclosporin A  (Synonyms: 環(huán)孢素; Cyclosporine A; Ciclosporin A; CsA)

目錄號(hào): HY-B0579 純度: 99.90%
COA 產(chǎn)品使用指南

Cyclosporin A (Cyclosporine A) 是一種免疫抑制劑,能與親環(huán)素結(jié)合,抑制 protein phosphatase 2B (PP2B/calcineurin) 活性的IC50 值為 7 nM。Cyclosporin A 也抑制 CD11a/CD18 粘附分子。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Cyclosporin A Chemical Structure

Cyclosporin A Chemical Structure

CAS No. : 59865-13-3

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Other Forms of Cyclosporin A:

MCE 顧客使用本產(chǎn)品發(fā)表的 121 篇科研文獻(xiàn)

WB
Proliferation Assay
IF

    Cyclosporin A purchased from MCE. Usage Cited in: Exp Mol Med. 2022 Feb;54(2):129-142.  [Abstract]

    Representative western blotting images of cGAS and STING in the Cyclosporine (CsA; 10?μM; for 24?h)- or DMSO-treated NP cells.

    Cyclosporin A purchased from MCE. Usage Cited in: Exp Mol Med. 2022 Feb;54(2):129-142.  [Abstract]

    Representative western blotting images of NLRP3, ASC, pro-CASP-1, cleaved CASP-1, GSDMD, and cleaved GSDMD in the (CsA; 10?μM; for 24?h)- or DMSO-treated NP cells.

    Cyclosporin A purchased from MCE. Usage Cited in: Exp Mol Med. 2022 Feb;54(2):129-142.  [Abstract]

    Representative immunofluorescence images of STING with different degrees of polymerization in the Cyclosporine (CsA; 10?μM; for 24?h)- or DMSO-treated NP cells.

    Cyclosporin A purchased from MCE. Usage Cited in: Redox Biol. 2022 Aug;54:102355.

    Cells are treated with or without Cyclosporine A (CsA; 2 μM) for 4 h in presence of NRC-03 (45 μg/mL). TUNEL immunofluorescence staining and quantification of TUNEL positive cells.

    Cyclosporin A purchased from MCE. Usage Cited in: Redox Biol. 2022 Aug;54:102355.

    Cells are treated with or without Cyclosporine A (CsA; 2 μM) for 4 h in presence of NRC-03 (45 μg/mL). Cell viability determined by CCK-8.

    Cyclosporin A purchased from MCE. Usage Cited in: Aging Dis. 2022 Oct 1;13(5):1546-1561.  [Abstract]

    Additionally, similar to P-gp siRNA silence, pharmacological inhibition of P-gp with Cyclosporine A (CsA; 22 mg/kg) significantly attenuates P-gp expression levels in ischemic brain as compared to vehicle treatment.

    Cyclosporin A purchased from MCE. Usage Cited in: Nat Commun. 2021 May 18;12(1):2915.  [Abstract]

    Immunoblot analysis of Cytochrome c from cytosolic extracts and mitochondria from indicated cells pre-treated with DMSO or Cyclosporine A (50?μM) for 1?h, followed with PFOS treatment (150?μM, 6?h).

    Cyclosporin A purchased from MCE. Usage Cited in: Cell Death Dis. 2021 Apr 20;12(5):413.  [Abstract]

    Inhibition of NR-induced increase of co-localized puncta (LC3 and TOM20) after 1?μMCyclosporin A (CsA) pretreatment.

    Cyclosporin A purchased from MCE. Usage Cited in: Cell Death Dis. 2021 Apr 1;12(4):336.  [Abstract]

    Immunofluorescence staining of subcellular localization of NFATC1 in RANK overexpression and control cells with or without treatment of 10?μg/mL Cyclosporin A (CsA).

    Cyclosporin A purchased from MCE. Usage Cited in: Cell Rep. 2021 Nov 30;37(9):110069.  [Abstract]

    Colony formation of CRC cells treated with Cyclosporine A (CsA; 2.5-5 μM) in combination with 5-FU or OXA for 48 h.

    Cyclosporin A purchased from MCE. Usage Cited in: Cell Rep. 2021 Nov 30;37(9):110069.  [Abstract]

    Immunoblotting analysis of indicated apoptotic markers expression in CRC cells treated with Cyclosporine A (CsA; 2.5-5 μM) in combination with 5-FU or OXA.

    Cyclosporin A purchased from MCE. Usage Cited in: Proc Natl Acad Sci U S A. 2021 Jan 12;118(2):e2009539118.  [Abstract]

    Calcineurin activities of the PCE after FK506 or Cyclosporine A (CsA; 4 μM) treatment Zebrafish.

    Cyclosporin A purchased from MCE. Usage Cited in: Br J Pharmacol. 2021 Jun;178(11):2305-2323.  [Abstract]

    Smooth muscle cells are treated cyclosporin A (CsA, 1 μM) or PDTC (10 μM) for 24 h before measuring the activity of PPARγ2 promoter.

    Cyclosporin A purchased from MCE. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):598.  [Abstract]

    A549 cells are pretreated with 5?μM Cyclosporin A (CSA) for 2?h, followed by treatment with 80?μM Hirsutine for 24?h. equal amount of lysates are subjected to immunoprecipitation using anti-ANT1 antibody, the associated CypD is determined using immunoblotting.
    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM[3]. Cyclosporin A also inhibits CD11a/CD18 adhesion[8].

    IC50 & Target

    Cyclophilin D

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    2008 IC50
    2.7 μM
    Compound: Cyclosporine A
    Inhibition of MRP1 in human 2008 cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay
    Inhibition of MRP1 in human 2008 cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay
    [PMID: 24184213]
    2008 IC50
    2.81 μM
    Compound: CsA
    Inhibition of MRP1 (unknown origin) expressed in human 2008 cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay
    Inhibition of MRP1 (unknown origin) expressed in human 2008 cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay
    [PMID: 23851114]
    A2780 GI50
    8.94 μM
    Compound: Cyclosporine A
    Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 27100033]
    A2780 ADR IC50
    0.919 μM
    Compound: CsA
    Inhibition of ABCB1 in human A2780adr cells pre-incubated for 30 mins followed by calcein AM addition and further incubated for 60 mins by calcein AM assay
    Inhibition of ABCB1 in human A2780adr cells pre-incubated for 30 mins followed by calcein AM addition and further incubated for 60 mins by calcein AM assay
    [PMID: 25855895]
    A2780 ADR IC50
    0.92 μM
    Compound: Cyclosporine A
    Inhibition of MDR1 in human doxorubicin-resistant A2780adr cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay
    Inhibition of MDR1 in human doxorubicin-resistant A2780adr cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay
    [PMID: 24184213]
    A2780 ADR IC50
    0.99 μM
    Compound: CsA
    Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay
    Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay
    [PMID: 23851114]
    A2780 ADR IC50
    1.21 μM
    Compound: Cyclosporine A
    Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcien-AM efflux preincubated for 30 mins followed by calcien-AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay
    Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcien-AM efflux preincubated for 30 mins followed by calcien-AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay
    [PMID: 27676469]
    A2780 ADR IC50
    1.4 μM
    Compound: Cyclosporin A
    Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay
    Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay
    [PMID: 19250834]
    A2780 ADR IC50
    1.41 μM
    Compound: Cyclosporine A
    Inhibition of ABCB1 in human A2780/ADR cells incubated for 30 mins measured up to 3600 secs with time intervals of 60 secs by calcein accumulation assay
    Inhibition of ABCB1 in human A2780/ADR cells incubated for 30 mins measured up to 3600 secs with time intervals of 60 secs by calcein accumulation assay
    [PMID: 27100033]
    A2780 ADR GI50
    8.63 μM
    Compound: Cyclosporine A
    Cytotoxicity against human A2780/ADR cells overexpressing ABCB1 assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human A2780/ADR cells overexpressing ABCB1 assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 27100033]
    B-cell IC50
    0.07 μg/mL
    Compound: cyclosporin A
    Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
    Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
    [PMID: 14738397]
    B-cell IC50
    0.74 μM
    Compound: CsA
    Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in LPS-induced mouse B-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay
    Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in LPS-induced mouse B-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay
    [PMID: 35678710]
    Breast cancer cell line EC50
    0.5 μM
    Compound: Cyclosporin A
    Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%.
    Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%.
    [PMID: 11784143]
    Breast cancer cell line EC50
    0.6 μM
    Compound: Cyclosporin A
    Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%
    Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%
    [PMID: 11784143]
    CCRF-CEM IC50
    3.4 μM
    Compound: 1
    Inhibitory activity against Human MDR1 P-Glycoprotein ABC Transporter using leukemia CEM cells
    Inhibitory activity against Human MDR1 P-Glycoprotein ABC Transporter using leukemia CEM cells
    [PMID: 12361387]
    HEK293 IC50
    0.7 μM
    Compound: Cyclosporine A
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate
    [PMID: 22587986]
    HEK293 IC50
    0.7 μM
    Compound: Cyclosporine A
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate
    [PMID: 22587986]
    HEK293 IC50
    1.2 μM
    Compound: Cyclosporine A
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate
    [PMID: 22587986]
    HEK293 IC50
    1.3 μM
    Compound: Cyclosporin A
    Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting
    Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting
    [PMID: 22541068]
    HEK293 IC50
    1.4 μM
    Compound: Cyclosporin A
    Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting
    Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting
    [PMID: 22541068]
    HEK293 IC50
    37 μM
    Compound: Cyclosporin A
    Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting
    Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting
    [PMID: 22541068]
    HeLa IC50
    6.6 μM
    Compound: Cs
    Antiviral activity against HPV-18 infected in human HeLa cells assessed as inhibition of viral replication after 3 days
    Antiviral activity against HPV-18 infected in human HeLa cells assessed as inhibition of viral replication after 3 days
    [PMID: 18212100]
    HFF IC50
    > 10000 nM
    Compound: CSA
    Inhibition of fetal calf serum-induced proliferation of human foreskin fibroblast assessed as [3H]thymidine incorporation after 4 days by scintillation counting
    Inhibition of fetal calf serum-induced proliferation of human foreskin fibroblast assessed as [3H]thymidine incorporation after 4 days by scintillation counting
    [PMID: 14593182]
    Huh-5-2 EC50
    0.3 μM
    Compound: Cyclosporine A
    Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay
    Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay
    [PMID: 18625766]
    Huh-5-2 EC50
    306 nM
    Compound: CsA
    Antiviral activity against Hepatitis C virus genotype 1b I389luc-ubi-neo/NS3-3'/5.1 subgenomic replicon infected in human Huh5-2 cells after 4 days by luciferase assay
    Antiviral activity against Hepatitis C virus genotype 1b I389luc-ubi-neo/NS3-3'/5.1 subgenomic replicon infected in human Huh5-2 cells after 4 days by luciferase assay
    10.1039/C1MD00227A
    Huh-5-2 CC50
    4.4 μM
    Compound: CsA
    Cytostatic activity against human Huh5-2 cells assessed as decrease in cell proliferation after 3 days by MTS method
    Cytostatic activity against human Huh5-2 cells assessed as decrease in cell proliferation after 3 days by MTS method
    10.1039/C1MD00227A
    Huh-5-2 CC50
    6 μM
    Compound: Cyclosporine A
    Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay
    Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay
    [PMID: 18625766]
    Huh-7 EC50
    > 10 μM
    Compound: CsA
    Antiviral activity against cyclosporine A/NIM-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay
    Antiviral activity against cyclosporine A/NIM-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay
    [PMID: 20176894]
    Huh-7 EC50
    0.21 μM
    Compound: CsA
    Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay
    Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay
    [PMID: 20176894]
    Huh-7 EC50
    137 nM
    Compound: CsA
    Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis
    Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis
    10.1039/C1MD00227A
    Huh-7 EC50
    198 nM
    Compound: CsA
    Antiviral activity against Hepatitis C virus genotype 1a H77 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis
    Antiviral activity against Hepatitis C virus genotype 1a H77 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis
    10.1039/C1MD00227A
    Huh-7 EC50
    3.39 μM
    Compound: CsA
    Antiviral activity against cyclosporine A-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay
    Antiviral activity against cyclosporine A-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay
    [PMID: 20176894]
    Huh-7 EC50
    455 nM
    Compound: CsA
    Antiviral activity against Hepatitis C virus genotype 2a JFH-1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis
    Antiviral activity against Hepatitis C virus genotype 2a JFH-1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis
    10.1039/C1MD00227A
    Huh-7 CC50
    5.62 μM
    Compound: CsA
    Antiviral activity against Hepatitis C virus infected in human Huh7ET cells assessed as inhibition of viral replication after 72 hrs by luciferase reporter gene assay
    Antiviral activity against Hepatitis C virus infected in human Huh7ET cells assessed as inhibition of viral replication after 72 hrs by luciferase reporter gene assay
    [PMID: 19933795]
    Jurkat IC50
    > 10 μM
    Compound: CsA
    Cytotoxicity against human Jurkat cells after 4 days by MTT assay
    Cytotoxicity against human Jurkat cells after 4 days by MTT assay
    [PMID: 22984987]
    Jurkat EC50
    0.005 μM
    Compound: CsA
    Antiinflammatory activity in human Jurkat cells assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay
    Antiinflammatory activity in human Jurkat cells assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay
    [PMID: 19933795]
    Jurkat IC50
    1.4 nM
    Compound: 1
    Inhibition of NFAT activation in PMA/ionomycin-stimulated human Jurkat T cells incubated for 30 mins prior to PMA/ionomycin stimulation measured after 5 hrs by luciferase reporter gene assay
    Inhibition of NFAT activation in PMA/ionomycin-stimulated human Jurkat T cells incubated for 30 mins prior to PMA/ionomycin stimulation measured after 5 hrs by luciferase reporter gene assay
    [PMID: 23964991]
    Jurkat IC50
    1.9 μM
    Compound: CsA
    Immunosuppressive activity in human Jurkat cells assessed as reduction in PHA + PMA-induced IL-2 production after 48 hrs by ELISA
    Immunosuppressive activity in human Jurkat cells assessed as reduction in PHA + PMA-induced IL-2 production after 48 hrs by ELISA
    [PMID: 30579802]
    Jurkat IC50
    11 nM
    Compound: 1; CyA
    Immunosuppressive activity in human PMA/ionomycin stimulated Jurkat T cells assessed as suppression of IL2 production pretreated with cells followed by PMA/ionomycin stimulation measured after 13 hrs by ELISA
    Immunosuppressive activity in human PMA/ionomycin stimulated Jurkat T cells assessed as suppression of IL2 production pretreated with cells followed by PMA/ionomycin stimulation measured after 13 hrs by ELISA
    [PMID: 27647370]
    Jurkat IC50
    12 nM
    Compound: CsA
    The compound was tested in vitro for inhibition of IL-2 release stimulated with PMA/ionomycin by Jurkat cells.
    The compound was tested in vitro for inhibition of IL-2 release stimulated with PMA/ionomycin by Jurkat cells.
    [PMID: 7473543]
    Jurkat IC50
    2 nM
    Compound: CsA
    Immunosuppressive activity was measured by inhibition of the IL-2 production in Jurkat cells.
    Immunosuppressive activity was measured by inhibition of the IL-2 production in Jurkat cells.
    [PMID: 14643337]
    K562/R7 IC50
    0.7 μM
    Compound: cyclosporin A
    Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay
    Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay
    [PMID: 25634041]
    KB IC50
    0.6 μM
    Compound: CSA (cyclosporin A)
    Inhibitory activity against KB cell line after 72 h of drug exposure
    Inhibitory activity against KB cell line after 72 h of drug exposure
    [PMID: 15481991]
    KB 3-1 IC50
    1.5 μM
    Compound: CSA (cyclosporin A)
    Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure
    Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure
    [PMID: 15481991]
    L929 IC50
    29.9 μM
    Compound: Cyclosporin A
    Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    [PMID: 34597896]
    L929 IC50
    30 μM
    Compound: cyclosporin A
    Cytotoxicity against mouse L929 cells after 3 days by MTS assay
    Cytotoxicity against mouse L929 cells after 3 days by MTS assay
    [PMID: 25985195]
    L929 IC50
    33.9 μM
    Compound: cyclosporine A
    Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay
    Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay
    [PMID: 24171478]
    L929 IC50
    33.9 μM
    Compound: 2
    Cytotoxicity against mouse L929 cells after 72 hrs
    Cytotoxicity against mouse L929 cells after 72 hrs
    [PMID: 22320402]
    LLC-PK1 IC50
    0.7 μM
    Compound: Cyclosporin a
    Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
    Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
    [PMID: 12699389]
    LLC-PK1 IC50
    0.8 μM
    Compound: Cyclosporin a
    Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
    Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
    [PMID: 12699389]
    LLC-PK1 IC50
    4.8 μM
    Compound: Cyclosporin a
    Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
    Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
    [PMID: 12699389]
    Lymphocyte IC50
    0.054 μM
    Compound: CsA
    Immunosuppressive activity in peripheral blood lymphocytes isolated from two individuals assessed as proliferation using [methyl-3H]thymidine by mixed lymphocyte reaction assay
    Immunosuppressive activity in peripheral blood lymphocytes isolated from two individuals assessed as proliferation using [methyl-3H]thymidine by mixed lymphocyte reaction assay
    [PMID: 21171614]
    Lymphocyte IC50
    0.054 μM
    Compound: CsA
    Immunosuppressive activity in lymphocytes by mixed lymphocyte reaction assay
    Immunosuppressive activity in lymphocytes by mixed lymphocyte reaction assay
    [PMID: 20064721]
    Lymphocyte IC50
    0.2 μg/mL
    Compound: Cyclosporin A
    Immunosuppressive activity in human lymphocytes by mixed lymphocyte reaction assay
    Immunosuppressive activity in human lymphocytes by mixed lymphocyte reaction assay
    [PMID: 3373220]
    Lymphocyte EC50
    60 nM
    Compound: 1, CSA
    Immunosuppressive activity in lymphocytes (unknown origin) by mixed lymphocyte reaction assay
    Immunosuppressive activity in lymphocytes (unknown origin) by mixed lymphocyte reaction assay
    [PMID: 24831536]
    Lymphocyte IC50
    89 nM
    Compound: CsA
    Immunosuppressive activity in lymphocytes by MLR assay
    Immunosuppressive activity in lymphocytes by MLR assay
    [PMID: 24900866]
    MDCK-II IC50
    25.6 μM
    Compound: Cyclosporine A
    Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry
    Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry
    [PMID: 27393949]
    MT4 IC50
    > 0.83 μM
    Compound: Cs
    Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay
    Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay
    [PMID: 18212100]
    MT4 EC50
    450 nM
    Compound: 1, CsA
    Antiviral activity against HIV1 3B infected in human MT4 cells coinfected with HTLV1 assessed as reduction in virus-induced cytopathogenicity after 4 days by MTT assay
    Antiviral activity against HIV1 3B infected in human MT4 cells coinfected with HTLV1 assessed as reduction in virus-induced cytopathogenicity after 4 days by MTT assay
    [PMID: 23849880]
    MT4 CC50
    5608 nM
    Compound: CSA
    Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by cell-titer glo assay
    Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by cell-titer glo assay
    [PMID: 30074795]
    PBMC EC50
    0.0031 μM
    Compound: CsA
    Antiinflammatory activity in human PBMC assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay
    Antiinflammatory activity in human PBMC assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay
    [PMID: 19933795]
    PBMC IC50
    0.056 μM
    Compound: Cs
    Antiproliferative activity against mouse PBMC with MLR assessed as inhibition of [3H]thymidine incorporation after 18 hrs
    Antiproliferative activity against mouse PBMC with MLR assessed as inhibition of [3H]thymidine incorporation after 18 hrs
    [PMID: 18212100]
    PBMC IC50
    3 nM
    Compound: CsA
    Immunosuppressive activity in human PBMC isolated from two individuals assessed as inhibition of proliferation using [3H]thymidine by mixed lymphocyte reaction assay
    Immunosuppressive activity in human PBMC isolated from two individuals assessed as inhibition of proliferation using [3H]thymidine by mixed lymphocyte reaction assay
    10.1039/C1MD00227A
    RD CC50
    > 10 μM
    Compound: CsA
    Cytotoxicity against human RD cells after 24 hrs by WST-1 assay
    Cytotoxicity against human RD cells after 24 hrs by WST-1 assay
    [PMID: 26564266]
    RD EC50
    3.66 μM
    Compound: CsA
    Antiviral activity against EV71 infected in RD cells after 24 hrs by luciferase assay
    Antiviral activity against EV71 infected in RD cells after 24 hrs by luciferase assay
    [PMID: 26564266]
    Splenocyte CC50
    > 2.5 μM
    Compound: CsA
    Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
    Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
    [PMID: 35104138]
    Splenocyte IC50
    0.01 μg/mL
    Compound: Cyclosporine A
    Antiproliferative activity against concanavalin A-stimulated BALB/c mouse splenocytes after 72 hrs by AlamarBlue assay
    Antiproliferative activity against concanavalin A-stimulated BALB/c mouse splenocytes after 72 hrs by AlamarBlue assay
    [PMID: 23167554]
    Splenocyte IC50
    0.01 μM
    Compound: CsA
    Immunosuppressive activity in splenocytes assessed as inhibition of concanavalin A-induced proliferation after 48 hrs by [3H]thymidine incorporation assay
    Immunosuppressive activity in splenocytes assessed as inhibition of concanavalin A-induced proliferation after 48 hrs by [3H]thymidine incorporation assay
    [PMID: 19481938]
    Splenocyte EC50
    0.03 μM
    Compound: Cyclosporine A
    Immunosuppressive activity in BALB/c mouse splenocyte assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 48 hrs by MTT assay
    Immunosuppressive activity in BALB/c mouse splenocyte assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 48 hrs by MTT assay
    [PMID: 36596229]
    Splenocyte IC50
    0.03 μM
    Compound: CsA
    Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of concanavalin A induced T-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis
    Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of concanavalin A induced T-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis
    [PMID: 35104138]
    Splenocyte IC50
    0.04 μM
    Compound: CsA
    Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated before concanavalin A stimulation for 48 hrs followed by [3H]-thymidine additio
    Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated before concanavalin A stimulation for 48 hrs followed by [3H]-thymidine additio
    [PMID: 31253536]
    Splenocyte IC50
    0.04 μM
    Compound: CsA
    Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by concanavalin A stimulation and [3H]-thymidine addition f
    Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by concanavalin A stimulation and [3H]-thymidine addition f
    [PMID: 30500185]
    Splenocyte IC50
    0.07 μM
    Compound: CsA
    Immunosuppressive activity in splenocytes assessed as inhibition of LPS-induced proliferation after 48 hrs by [3H]thymidine incorporation assay
    Immunosuppressive activity in splenocytes assessed as inhibition of LPS-induced proliferation after 48 hrs by [3H]thymidine incorporation assay
    [PMID: 19481938]
    Splenocyte IC50
    0.1 μM
    Compound: Cyclosporin A
    Immunosupressive activity in OVA323-339 peptide-stimulated OT-2 T cell receptor transgenic mouse splenocytes assessed as inhibition of T cell proliferation after 3 days by MTT assay
    Immunosupressive activity in OVA323-339 peptide-stimulated OT-2 T cell receptor transgenic mouse splenocytes assessed as inhibition of T cell proliferation after 3 days by MTT assay
    [PMID: 25537268]
    Splenocyte IC50
    0.3 μM
    Compound: Cyclosporine A
    Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation incubated for 48 hrs by MTT assay
    Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation incubated for 48 hrs by MTT assay
    [PMID: 33544615]
    Splenocyte IC50
    0.32 μM
    Compound: CsA
    Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of LPS induced B-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis
    Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of LPS induced B-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis
    [PMID: 35104138]
    Splenocyte IC50
    0.4 μM
    Compound: CsA
    Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated before LPS stimulation for 48 hrs followed by [3H]-thymidine addition for 8 hrs by beta-sc
    Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated before LPS stimulation for 48 hrs followed by [3H]-thymidine addition for 8 hrs by beta-sc
    [PMID: 31253536]
    Splenocyte IC50
    0.4 μM
    Compound: CsA
    Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by LPS stimulation and [3H]-thymidine addition for 8 hrs measured afte
    Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by LPS stimulation and [3H]-thymidine addition for 8 hrs measured afte
    [PMID: 30500185]
    Splenocyte CC50
    0.88 μM
    Compound: CsA
    Cytotoxicity against splenocytes after 48 hrs by MTT assay
    Cytotoxicity against splenocytes after 48 hrs by MTT assay
    [PMID: 19481938]
    Splenocyte CC50
    1.2 μM
    Compound: CsA
    Cytotoxicity against BALB/c mouse splenocytes assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
    Cytotoxicity against BALB/c mouse splenocytes assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
    [PMID: 31253536]
    Splenocyte CC50
    1.2 μM
    Compound: CsA
    Cytotoxicity against BALB/c mouse splenocytes after 48 hrs by CCK-8 assay
    Cytotoxicity against BALB/c mouse splenocytes after 48 hrs by CCK-8 assay
    [PMID: 30500185]
    Splenocyte IC50
    10 nM
    Compound: Cyclosporine A
    Immunosuppressive activity in human splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay
    Immunosuppressive activity in human splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay
    [PMID: 19827831]
    Splenocyte IC50
    10.15 μM
    Compound: CsA
    Cytotoxicity against BALB/c mouse splenocyte assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay
    Cytotoxicity against BALB/c mouse splenocyte assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay
    [PMID: 33973788]
    Splenocyte IC50
    17 nM
    Compound: Cyclosporine A
    Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay
    Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay
    [PMID: 19827831]
    Splenocyte IC50
    30 nM
    Compound: 1, CsA
    Immunosuppressant activity in mouse splenocytes by mixed-leukocyte reaction assay
    Immunosuppressant activity in mouse splenocytes by mixed-leukocyte reaction assay
    [PMID: 23017885]
    Splenocyte CC50
    7.33 μM
    Compound: CsA
    Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 35678710]
    T cell line IC50
    26 nM
    Compound: CsA
    Antiproliferative activity against Con A-induced BALB/c mouse T cell after 48 hrs by CCK8 assay
    Antiproliferative activity against Con A-induced BALB/c mouse T cell after 48 hrs by CCK8 assay
    [PMID: 32822186]
    T cell line CC50
    9.8 μM
    Compound: CsA
    Cytotoxicity against BALB/c mouse T cell assessed as reduction in cell viability after 48 hrs by CCK8 assay
    Cytotoxicity against BALB/c mouse T cell assessed as reduction in cell viability after 48 hrs by CCK8 assay
    [PMID: 32822186]
    T-cell IC50
    > 10000 nM
    Compound: CSA
    Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting
    Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting
    [PMID: 14593182]
    T-cell IC50
    0.011 μM
    Compound: CsA
    Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay
    Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay
    [PMID: 22984987]
    T-cell IC50
    0.03 μM
    Compound: CsA
    Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay
    Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay
    [PMID: 35678710]
    T-cell IC50
    0.04 μg/mL
    Compound: cyclosporin A
    Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay
    Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay
    [PMID: 14738397]
    T-cell IC50
    0.06 μM
    Compound: CsA
    Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of anti-CD3/anti-CD28-stimulated cell proliferation after 72 hrs by MTT assay
    Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of anti-CD3/anti-CD28-stimulated cell proliferation after 72 hrs by MTT assay
    [PMID: 21131104]
    T-cell IC50
    0.07 μM
    Compound: CsA
    Immunosuppressive activity in lymph node T cell assessed as inhibition of ConA-stimulated cell proliferation after 72 hrs by MTT assay
    Immunosuppressive activity in lymph node T cell assessed as inhibition of ConA-stimulated cell proliferation after 72 hrs by MTT assay
    [PMID: 22300886]
    T-cell IC50
    0.08 μM
    Compound: Cyclosporin A
    Inhibition of ConA-induced cell proliferation of BALB/c mouse T-lymphocytes assessed as reduction in [3H]thymidine incorporation incubated for 48 hrs by beta scintillation counting method
    Inhibition of ConA-induced cell proliferation of BALB/c mouse T-lymphocytes assessed as reduction in [3H]thymidine incorporation incubated for 48 hrs by beta scintillation counting method
    [PMID: 28294615]
    T-cell IC50
    0.2 μM
    Compound: CsA
    Immunosuppressant activity in human T lymphocytes assessed as inhibition of anti-human CD3 and anti-human CD28 monoclonal antibody-induced T lymphocyte proliferation incubated for 72 hrs by FACS analysis
    Immunosuppressant activity in human T lymphocytes assessed as inhibition of anti-human CD3 and anti-human CD28 monoclonal antibody-induced T lymphocyte proliferation incubated for 72 hrs by FACS analysis
    [PMID: 31181920]
    T-cell IC50
    0.34 μM
    Compound: cyclosporin A
    Inhibition of PHA-induced human T cell proliferation after 24 hrs by MTT assay
    Inhibition of PHA-induced human T cell proliferation after 24 hrs by MTT assay
    [PMID: 11678649]
    T-cell CC50
    13.78 μM
    Compound: CsA
    Cytotoxicity against lymph node T cell after 24 hrs by MTT assay
    Cytotoxicity against lymph node T cell after 24 hrs by MTT assay
    [PMID: 22300886]
    T-cell IC50
    14 nM
    Compound: cyclosporin A
    Immunosuppressive activity in BALB/c/C57BL/6 mouse T cells assessed as inhibition of alloantigen-induced cell proliferation after 96 hrs by measuring [3H]thymidine uptake by mixed lymphocyte reaction assay
    Immunosuppressive activity in BALB/c/C57BL/6 mouse T cells assessed as inhibition of alloantigen-induced cell proliferation after 96 hrs by measuring [3H]thymidine uptake by mixed lymphocyte reaction assay
    [PMID: 21456524]
    T-cell CC50
    15.82 μM
    Compound: CsA
    Cytotoxicity against BALB/c mouse T cells after 48 hrs by MTT assay
    Cytotoxicity against BALB/c mouse T cells after 48 hrs by MTT assay
    [PMID: 21131104]
    T-cell IC50
    2.12 μM
    Compound: csa
    Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of ConA-induced T cell proliferation incubated 24 hrs post ConA-induction for 72 hrs by MTT assay
    Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of ConA-induced T cell proliferation incubated 24 hrs post ConA-induction for 72 hrs by MTT assay
    [PMID: 22727369]
    T-cell IC50
    32 nM
    Compound: CSA
    Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method
    Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method
    [PMID: 14593182]
    T-cell CC50
    4.5 μM
    Compound: Cyclosporin A
    Cytotoxic activity against BALB/c mouse T-lymphocytes assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxic activity against BALB/c mouse T-lymphocytes assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 28294615]
    T-cell IC50
    550 nM
    Compound: CsA
    Immunosuppressive activity in concanavalin A-activated T cell assessed as inhibition of lymphoproliferation after 3 days by beta-scintillation counting
    Immunosuppressive activity in concanavalin A-activated T cell assessed as inhibition of lymphoproliferation after 3 days by beta-scintillation counting
    [PMID: 19502058]
    T-cell EC50
    6.4 nM
    Compound: CsA
    Immunosuppressive activity in human PBMC assessed as inhibition of anti-human CD3-induced T-cell proliferation after 4 days by CellTrace violet cell proliferation dye based FACS analysis
    Immunosuppressive activity in human PBMC assessed as inhibition of anti-human CD3-induced T-cell proliferation after 4 days by CellTrace violet cell proliferation dye based FACS analysis
    [PMID: 28075591]
    T-cell IC50
    74 nM
    Compound: CSA
    Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method
    Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method
    [PMID: 14593182]
    Ventricular myocyte IC50
    2 μM
    Compound: Cyclosporin A
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
    [PMID: 22761000]
    Vero CC50
    > 50 μM
    Compound: Cyclosporine
    Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
    Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
    10.1101/2020.03.20.999730
    Vero IC50
    ≤ 0.5 μM
    Compound: Cs
    Antiviral activity against Dengue virus 1 infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay
    Antiviral activity against Dengue virus 1 infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay
    [PMID: 19451286]
    Vero IC50
    5.82 μM
    Compound: Cyclosporine
    Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
    Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
    10.1101/2020.03.20.999730
    Vero IC50
    8 μM
    Compound: Cs
    Antiviral activity against West Nile virus infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay
    Antiviral activity against West Nile virus infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay
    [PMID: 19451286]
    體外研究
    (In Vitro)

    Cyclosporin A 能夠與 T 細(xì)胞中的親環(huán)素結(jié)合[1]。
    Cyclosporin A 通過形成 Cyclophilin-Cyclosporin A 復(fù)合物來抑制神經(jīng)鈣蛋白[2]。
    Cyclosporin A 抑制受刺激細(xì)胞中的神經(jīng)鈣蛋白,IC50 值為 7 nM[3]。
    Cyclosporin A 抑制 NF-AT 的核轉(zhuǎn)位[4]。Cyclosporin A 通過阻止 MTP 打開對(duì)線粒體產(chǎn)生影響,IC50 為 39 nM[5]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    體內(nèi)研究
    (In Vivo)

    Cyclosporin A 可用于構(gòu)建尿毒癥模型,在雄性 Wistar 大鼠 (體重140-200 g,年齡 5-6 周) 中,靜脈給予 Cyclosporin A (10 mg/kg) 后的藥代動(dòng)力學(xué)參數(shù)顯示,曲線下面積為 27.3 μg·h/mL,半衰期為 6.9 小時(shí),分布容積為 3.7 L/kg[9]

    誘導(dǎo)尿毒癥[10][11]
    致病原理
    Cyclosporin A 給藥通過刺激轉(zhuǎn)化生長因子 β (TGF-β) 信號(hào)通路誘導(dǎo) III 型膠原蛋白間質(zhì)沉積和纖維化,同時(shí)通過調(diào)節(jié)基質(zhì)金屬肽酶 9 抑制細(xì)胞外基質(zhì) (ECM) 降解,從而導(dǎo)致細(xì)胞外基質(zhì)失衡[10]。
    具體造模方法:
    小鼠:6-8 周齡 C57BL/6 小鼠
    給藥方式:30 mg/kg • 皮下注射 • 每日給藥,共 16 周
    Note
    造模成功指標(biāo)
    代謝變化:尿素氮 (BUN) 水平↑
    組織學(xué)分析: 腎小管損傷、間質(zhì)炎癥和纖維化。
    分子變化: LOX、LOXL2、TNFα、MCP-1、(NOX)4 的 mRNA 表達(dá)&uarr,α-SMA,F(xiàn)N,COL1A、MCP-1蛋白表達(dá)&uarr。
    相關(guān)產(chǎn)品: /
    拮抗產(chǎn)品Lipoxygenase, general (HY-P2976); Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11) (HY-P990107)

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    1202.61

    Formula

    C62H111N11O12

    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    環(huán)孢霉素A;環(huán)孢素A;環(huán)孢多肽A;環(huán)孢靈;賽斯平;環(huán)孢素

    結(jié)構(gòu)分類
    初始來源

    the fungus Beauveria nivea.

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲(chǔ)存方式

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMSO 中的溶解度 : 62.5 mg/mL (51.97 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

    Ethanol 中的溶解度 : 50 mg/mL (41.58 mM; 超聲助溶)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 0.8315 mL 4.1576 mL 8.3152 mL
    5 mM 0.1663 mL 0.8315 mL 1.6630 mL
    查看完整儲(chǔ)備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
    儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí),請?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請?jiān)?個(gè)月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn):

    請根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑: 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 2.62 mg/mL (2.18 mM); 懸濁液; 超聲助溶

    • 方案 二

      請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.08 mg/mL (1.73 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.08 mg/mL的均勻懸濁液,懸濁液可用于口服和腹腔注射。

      1 mL 工作液為例,取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。

    以下溶解方案,請直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請依序添加每種溶劑: Corn Oil

      Solubility: 20 mg/mL (16.63 mM); 澄清溶液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請輸入動(dòng)物實(shí)驗(yàn)的基本信息:

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
    請輸入您的動(dòng)物體內(nèi)配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上,請謹(jǐn)慎選擇該方案。
    請確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.90%

    參考文獻(xiàn)
    Cell Assay
    [3]

    Immunosuppressive agents are dissolved in ethanol at concentrations 1000-fold more than the concentration desired for cell treatments. Cells (106) are suspended in 1 mL of complete medium in microcentrifuge tubes; 1 μL of ethanol or of the ethanolic solution of Cyclosporin A is added, and the cells are incubated at 37°C for 1 hr. Cells are washed twice with 1 mL of PBS on ice and lysed in 50 μL of hypotonic buffer containing 50 mM Tris (pH 7.5); 0.1 mM EGTA; 1 mM EDTA; 0.5 mM dithiothreitol; and 50 μg of phenylmethylsulfonyl fluoride, 50 μg of soybean trypsin inhibitor, 5 μg of leupeptin, and 5 μg of Kiker 52G per mL. Lysates are subjected to three cycles of freezing in liquid nitrogen followed by thawing at 30°C and then are centrifuged at 4°C for 10 min at 12,000×g.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [6]

    Rats are immunized on day 0 i.p. with 0 5 mL and mice i.v. with 0 2 mL of a 10% suspension of washed sheep erythrocytes (SE). To elicit a secondary response, mice are boosted 8-11 weeks after the primary immunization with an i.v. injection of 0-2 mL of 0 25% washed SE (107 cells). For prolonged treatment the animals receive on the average 45 mg/kg cyclosporin A daily in the food during 13 weeks. These rats are immunized 5 days before killing.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
    儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí),請?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 0.8315 mL 4.1576 mL 8.3152 mL 20.7881 mL
    5 mM 0.1663 mL 0.8315 mL 1.6630 mL 4.1576 mL
    10 mM 0.0832 mL 0.4158 mL 0.8315 mL 2.0788 mL
    15 mM 0.0554 mL 0.2772 mL 0.5543 mL 1.3859 mL
    20 mM 0.0416 mL 0.2079 mL 0.4158 mL 1.0394 mL
    25 mM 0.0333 mL 0.1663 mL 0.3326 mL 0.8315 mL
    30 mM 0.0277 mL 0.1386 mL 0.2772 mL 0.6929 mL
    40 mM 0.0208 mL 0.1039 mL 0.2079 mL 0.5197 mL
    DMSO 50 mM 0.0166 mL 0.0832 mL 0.1663 mL 0.4158 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    產(chǎn)品名稱:
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