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Immunology & Inflammation
Antineoplastic and Immunosuppressive Antibiotics inhibitor
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Immunology & Inflammation related inhibitor
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phosphatase inhibitor
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Complement System inhibitor
Cyclosporin A
僅限科研使用
Cyclosporin A
別名: Cyclosporine A, Cyclosporine, Ciclosporin, CsA,NSC 290193 中文名稱：環(huán)孢菌素A
Cyclosporin A, 一種非極性環(huán)寡肽，是一種免疫抑制劑，與親環(huán)素結(jié)合，隨后抑制calcineurin，無細胞試驗中IC50為7 nM，廣泛用于預(yù)防器官移植反應(yīng)中的排斥反應(yīng),并已用于在灌注的3D近端小管模型上測試其毒性作用。Cyclosporin A?(NSC 290193) 可用于誘導(dǎo)肝移植慢性排斥反應(yīng)動物模型。
Cyclosporin A Chemical Structure
CAS: 59865-13-3
產(chǎn)品質(zhì)控
批次：
純度：
99.98%
99.98
常與Cyclosporin A一起在實驗中被使用的化合物
Cyclosporin A和Diquafosol Tetrasodium聯(lián)合治療可顯著改善干眼癥的客觀體征和癥狀。
Eom Y, et al. J Ocul Pharmacol Ther. 2022 Dec;38(10):682-694.
Cyclosporin A和Rapamycin對大鼠實驗性自身免疫性葡萄膜視網(wǎng)膜炎(EAU)具有完全抑制作用。
CyclosporinA和Nifedipine通過增加成纖維細胞和膠原密度引起大鼠牙齦過度生長。
Spoildorio LC, et al. J Periodontal Res. 2002 Jun;37(3):192-5.
Cyclosporin A和Dexamethasone可減少前列環(huán)素(PGI2)釋放并增加纖溶酶原激活物抑制劑1(PAI-1)分泌。
Huang LQ, et al. Blood Coagul Fibrinolysis. 1995 Jul;6(5):438-45.
Cyclosporin A和Selumetinib組合在結(jié)直腸癌患者來源的腫瘤外植體(PDTX)模型中表現(xiàn)出腫瘤生長抑制和腫瘤消退。
Spreafico A, et al. Clin Cancer Res. 2013 Aug 1;19(15):4149-62.
Cyclosporin A相關(guān)產(chǎn)品
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| human K562/R7 cells | Function assay | 1 μM | 72 h | 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, IC50=0.7 μM | 25634041 |
| MDCK2 | Function assay | 10 uM | 40 mins | Inhibition of human wild type Pgp expressed in MDCK2 cells assessed as calcein-AM accumulation at 10 uM after 40 mins. | 17964170 |
| C2C12 | Function assay | 0.1 ug/ml | 3 days | Inhibition of hexose-6-phosphate dehydrogenase-induced cell differentiation in mouse C2C12 cells assessed as myosin heavy chain fluorescence at 0.1 ug/ml for 3 days. | 20081855 |
| HCT116 | Function assay | 10 uM | 30 mins | Modulation of BCRP in human HCT116 cells assessed as intracellular accumulation of mitoxantrone at 10 uM after 30 mins by flow-cytometry. | 21488686 |
| 2008 | Function assay | 10 uM | 30 mins | Inhibition of human MRP1 expressed in 2008 cells at 10 uM preincubated for 30 mins prior to calcein AM addition measured every 60 secs up to 90 mins by calcein AM accumulation assay. | 23017888 |
| A2780adr | Function assay | 10 uM | 30 mins | Inhibition of human P-gp overexpressed in doxorubicin resistant A2780adr cells at 10 uM preincubated for 30 mins prior to calcein AM addition measured every 60 secs up to 90 mins by calcein AM accumulation assay. | 23017888 |
| HL60 | Function assay | 5 uM | 40 mins | Inhibition of Ca2+-induced mitochondrial permeability transition in human HL60 cells at 5 uM after 40 mins relative to control. | 23026083 |
| Saos2 | Function assay | 5 uM | 3 hrs | Inhibition of p-gp in doxorubicin-resistant human Saos2 cells assessed as increase in doxorubicin uptake at 5 uM after 3 hrs by flow cytometric analysis. | 24720452 |
| Saos2 | Function assay | 5 uM | 2 hrs | Inhibition of p-gp in doxorubicin-resistant human Saos2 cells assessed as increase in intracellular doxorubicin retention at 5 uM after 2 hrs by flow cytometric analysis. | 24720452 |
| Saos2 | Function assay | 5 uM | 2 to 3 hrs | Inhibition of p-gp in doxorubicin-resistant human Saos2 cells assessed as intracellular doxorubicin distribution in nuclei at 5 uM after 2 to 3 hrs by laser scanning confocal microscopic analysis. | 24720452 |
| A2780 | Function assay | 5 uM | 40 mins | Inhibition of Pgp-mediated drug efflux in adriamycin-resistant human A2780 cells assessed as increase in intracellular adriamycin level at 5 uM after 40 mins by flow cytometry analysis. | 24900323 |
| A2780 | Function assay | 5 uM | 1 hr | Inhibition of Pgp-mediated drug efflux in adriamycin-resistant human A2780 cells assessed as increase in adriamycin uptake at 5 uM after 1 hr by flow cytometry analysis. | 24900323 |
| A2780 | Function assay | 5 uM | 8 hrs | Inhibition of Pgp-mediated drug efflux in adriamycin-resistant human A2780 cells assessed as increase in adriamycin uptake at 5 uM after 8 hrs by flow cytometry analysis. | 24900323 |
| T-cells | Antiinflammatory assay | 0.01 to 100 nM | 2 days | Antiinflammatory activity in LLO118 TCR transgenic mouse IL-2-competent CD4-positive T cells assessed as inhibition of LLO (190 to 205)-induced IL-2 production at 0.01 to 100 nM for 2 days by flow cytometric analysis. | 24900866 |
| Th17 | Antiinflammatory assay | 10 to 100 nM | 2 days | Antiinflammatory activity in LLO118 TCR transgenic mouse Th17 cells assessed as inhibition of IL-17 production at 10 to 100 nM for 2 days by flow cytometric analysis. | 24900866 |
| Th1 | Antiinflammatory assay | 100 nM | 2 days | Antiinflammatory activity in LLO118 TCR transgenic mouse Th1 cells assessed as inhibition of IFN-gamma production at 100 nM for 2 days by flow cytometric analysis. | 24900866 |
| CD1 | Function assay | 0.1 to 10 uM | 30 mins | Inhibition of taurolithocholate acid 3-sulfate-induced necrosis in CD1 mouse pancreatic acinar cells at 0.1 to 10 uM after 30 mins by propidium iodide staining based confocal microscopic analysis. | 26950392 |
| Flp-InTM-293 | Function assay | 25 uM | 30 mins | Inhibition of ABCC2 (unknown origin) expressed in human Flp-InTM-293 cells assessed as inhibition of calcein-AM efflux at 25 uM measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry. | 27393949 |
| hamster BHK21 | Function assay | 25 uM | 30 mins | Inhibition of human ABCC1 expressed in hamster BHK21 cells assessed as inhibition of calcein-AM efflux at 25 uM measured after 30 mins by flow cytometry. | 27393949 |
| MDCK2 | Function assay | 25 uM | 30 mins | Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux at 25 uM measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry. | 27393949 |
| NH3T3 | Function assay | 2.5 uM | 30 mins | Inhibition of human ABCB1 expressed in mouse NH3T3 cells assessed as inhibition of calcein-AM efflux at 2.5 uM measured after 30 mins by flow cytometry. | 27393949 |
| MDA435/LCC6MDR | Function assay | 1 uM | 5 days | Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 1 uM measured after 5 days by Cell Titer 96 Aqueous assay (Rvb = 139.3 +/- 7.5 nM), IC50 = 0.0018 μM. | 27750197 |
| K562R | Function assay | 5 uM | 1 hr | Inhibition of P-gp in doxorubicin-resistant human K562R cells assessed as rhodamine efflux by measuring ratio of mean fluorescence intensity in presence and absence of compound at 5 uM incubated for 1 hr by flow cytometry. | 27753480 |
| HCT15 | Function assay | 0.4 to 6.3 ug/mL | Modulation of P-gp in human HCT15 cells assessed as increase in DINIB-induced cytotoxicity at 0.4 to 6.3 ug/mL. | 11754602 | |
| UO31 | Function assay | 0.4 to 6.3 ug/mL | Modulation of P-gp in human UO31 cells assessed as increase in DINIB-induced cytotoxicity at 0.4 to 6.3 ug/mL. | 11754602 | |
| CAKI1 | Function assay | 0.4 to 6.3 ug/mL | Modulation of P-gp in human CAKI1 cells assessed as increase in DINIB-induced cytotoxicity at 0.4 to 6.3 ug/mL. | 11754602 | |
| HCT15 | Function assay | 10 uM | Inhibition of MDR1 in human HCT15 cells assessed as calcein-AM efflux at 10 uM by fluorescence assay. | 21348461 | |
| mouse L5178 cells | Function assay | 20 mins | Inhibition of human ABCB1-mediated rhodamine 123 efflux in mouse L5178 cells expressing human MDR1 after 20 mins by FACS analysis, IC50=0.65 μM | 21341745 | |
| KB/MDR cell | Function assay | 72 h | Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure, IC50=1.5 μM | 15481991 | |
| human MDA435/LCC6MDR cells | Cytotoxic?assay | 72h | Cytotoxicity against human MDA435/LCC6MDR cells expressing MDR after 72 hrs， IC50=2.8 μM | 22320402 | |
| human Huh5-2 cells | Cytotoxic?assay | 3 days | Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay , CC50=6 μM | 18625766 | |
| human HuH6 cells | Cytotoxic?assay | 3 days | Cytotoxicity against human HuH6 cells after 3 days by MTT assay, CC50=7 μM | 18625766 | |
| human Huh-9-13 cells | Cytotoxic?assay | 3 days | Cytotoxicity against human Huh-9-13 cells after 3 days by MTT assay， CC50=7 μM | 18625766 | |
| african green monkey Vero cells | Function assay | 24 h | 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, IC50=8 μM | 19451286 | |
| human LCC-6 cells | Cytotoxic?assay | 72 h | Cytotoxicity against human LCC-6 cells after 72 hrs, IC50=8.3 μM | 22320402 | |
| human Huh-Mono cells | Cytotoxic?assay | 3 days | Cytotoxicity against human Huh-Mono cells after 3 days by MTT assay， CC50=24 μM | 18625766 | |
| mouse L929 cells | Cytotoxic?assay | 3 days | Cytotoxicity against mouse L929 cells after 3 days by MTS assay, IC50=30 μM | 25985195 | |
| human MDA435/LCC6MDR cells | Function assay | 5 days | Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing paclitaxel resistance measured as cell survival after 5 days by MTS assay, EC50=0.032 μM. | 25985195 | |
| mouse T cells | Function assay | 4 days | Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay, ic50=11 nM | 22984987 | |
| human splenocytes | Function assay | 4 days | Immunosuppressive activity in human splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay, IC50=10 nM | 19827831 | |
| human Jurkat cells | Function assay | 1 h | 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, EC50=5 nM | 19933795 | |
| human PBMC | Function assay | 1 h | 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, EC50=3.1 nM | 19933795 | |
| PMBC | Function assay | 72 hrs | Effect on proliferation of human peripheral blood mononuclear cells (PMBC) at 72 hr using MTT assay, IC50 = 8.97 μM. | 15203163 | |
| A2780 | Function assay | 30 mins | Inhibition of human Pgp in A2780 cells after 30 mins by Hoechst 33342 assay, IC50 = 1.41254 μM. | 18083034 | |
| A2780 | Function assay | 30 mins | Inhibition of human Pgp in A2780 cells after 30 mins by calcein AM assay, IC50 = 1.41254 μM. | 18083034 | |
| Huh-9-13 | Antiviral assay | 3 days | Antiviral activity against BILN 2061-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 0.004 μM. | 19104013 | |
| Huh-9-13 | Antiviral assay | 3 days | Antiviral activity against compound-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 0.35 μM. | 19104013 | |
| Huh-9-13 | Antiviral assay | 3 days | Antiviral activity against 2'-C-methyl-2'-fluoro-cytidine-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 0.4 μM. | 19104013 | |
| Huh-9-13 | Antiviral assay | 3 days | Antiviral activity against VX 950-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 0.49 μM. | 19104013 | |
| Huh-9-13 | Antiviral assay | 3 days | Antiviral activity against R479-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 1.98 μM. | 19104013 | |
| Huh-9-13 | Antiviral assay | 3 days | Antiviral activity against cyclosporine-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 3.85 μM. | 19104013 | |
| HuH7 | Antiviral assay | 48 hrs | 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, EC50 = 0.21 μM. | 20176894 | |
| HuH7 | Antiviral assay | 48 hrs | 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, EC50 = 3.39 μM. | 20176894 | |
| T-cells | Immunosuppressive assay | 72 hrs | 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, IC50 = 0.06 μM. | 21131104 | |
| T-cells | Cytotoxicity assay | 48 hrs | Cytotoxicity against BALB/c mouse T cells after 48 hrs by MTT assay, CC50 = 15.82 μM. | 21131104 | |
| T-cells | Immunosuppressive assay | 96 hrs | 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, IC50 = 0.014 μM. | 21456524 | |
| L929 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse L929 cells after 72 hrs, IC50 = 33.9 μM. | 22320402 | |
| CCRF-CEM/VCR1000 | Function assay | 240 secs | Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis, IC50 = 0.10233 μM. | 22452412 | |
| mouse lymph node cells | Immunosuppressive assay | 72 hrs | Immunosuppressive activity in anti-CD3/anti-CD8 co-stimulated Balb/c mouse lymph node cells assessed as inhibition of cell proliferation after 72 hrs by ELISA, IC50 = 0.07 μM. | 22494616 | |
| mouse lymph node cells | Cytotoxicity assay | 48 hrs | Cytotoxicity against Balb/c mouse lymph node cells after 48 hrs by MTT assay, CC50 = 10.1 μM. | 22494616 | |
| HEK293 | Function assay | 5 mins | 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, Ki = 1.2 μM. | 22541068 | |
| HEK293 | Function assay | 5 mins | 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, IC50 = 1.3 μM. | 22541068 | |
| HEK293 | Function assay | 5 mins | 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, Ki = 36 μM. | 22541068 | |
| HEK293 | Function assay | 5 mins | 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, IC50 = 37 μM. | 22541068 | |
| T-cells | Immunosuppressive assay | 24 hrs | 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, IC50 = 2.12 μM. | 22727369 | |
| RPMI1788 | Immunosuppressive assay | 6 days | Immunosuppressive activity in human RPMI1788 cells cocultured with human PBMC assessed as inhibition of [3H]thymidine incorporation incubated for 6 days prior to [3H]thymidine addition measured after 18 hrs by liquid scintillation counting, IC50 = 0.054 μM. | 23347804 | |
| MT4 | Antiviral assay | 4 days | 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, EC50 = 0.45 μM. | 23849880 | |
| A2780Adr | Function assay | 30 mins | 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, IC50 = 0.99 μM. | 23851114 | |
| 2008 | Function assay | 30 mins | 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, IC50 = 2.81 μM. | 23851114 | |
| Jurkat T | Function assay | 30 mins | 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, IC50 = 0.0014 μM. | 23964991 | |
| MDA435/LCC6 | Cytotoxicity assay | 3 days | Cytotoxicity against human MDA435/LCC6 cells assessed as growth inhibition after 3 days by MTS assay, IC50 = 2.8 μM. | 24171478 | |
| MDA435/LCC6MDR | Cytotoxicity assay | 3 days | Cytotoxicity against human MDA435/LCC6MDR cells assessed as growth inhibition after 3 days by MTS assay, IC50 = 8.3 μM. | 24171478 | |
| L929 | Cytotoxicity assay | 3 days | Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay, IC50 = 33.9 μM. | 24171478 | |
| A2780adr | Function assay | up to 90 mins | 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, IC50 = 0.92 μM. | 24184213 | |
| 2008 | Function assay | up to 90 mins | 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, IC50 = 2.7 μM. | 24184213 | |
| NCI/ADR-RES | Function assay | 20 mins | Inhibition of human P-glycoprotein expressed in NCI/ADR-RES cells assessed as reduction of calcein-AM transport after 20 mins by fluorescence assay. | 24992153 | |
| A2780adr | Function assay | 90 mins | 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, IC50 = 0.919 μM. | 25855895 | |
| T spleen cells | Cytotoxicity assay | 72 hrs | Cytotoxicity against ICR mouse T spleen cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.01 μM. | 26564266 | |
| B spleen cells | Cytotoxicity assay | 72 hrs | Cytotoxicity against ICR mouse B spleen cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.04 μM. | 26564266 | |
| RD | Antiviral assay | 24 hrs | Antiviral activity against EV71 infected in RD cells after 24 hrs by luciferase assay, EC50 = 3.66 μM. | 26564266 | |
| A2780/ADR | Function assay | 30 mins | 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, IC50 = 1.41 μM. | 27100033 | |
| A2780/ADR | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A2780/ADR cells overexpressing ABCB1 assessed as reduction in cell viability after 72 hrs by MTT assay, GI50 = 8.63 μM. | 27100033 | |
| A2780 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 72 hrs by MTT assay, GI50 = 8.94 μM. | 27100033 | |
| Jurkat T | Immunosuppressive assay | 13 hrs | 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, IC50 = 0.011 μM. | 27647370 | |
| A2780/ADR | Function assay | 30 mins | 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, IC50 = 1.21 μM. | 27676469 | |
| HuH7 | Antiviral assay | 72 hrs | Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells after 72 hrs by luciferase reporter gene assay, EC50 = 0.17 μM. | 28075591 | |
| HepaRG | Antiviral assay | 16 hrs | Antiviral activity against HBV infected in human HepaRG cells assessed as reduction in viral infection after 16 hrs, IC50 = 0.2 μM. | 28383274 | |
| replicon 2A cells | Function assay | 72 hrs | Inhibition of mTOR signaling pathway in (unknown origin) in sub-genomic replicon 2A cells assessed as reduction in phosphorylated rps6 protein levels up to 400 nM after 72 hrs by Western blot analysis. | 28442256 | |
| A2780adr | Function assay | 30 mins | Inhibition of ABCB1 in human A2780adr cells assessed as reduction in calcein AM levels preincubated for 30 mins followed by calcein AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay, IC50 = 1.21 μM. | 28471656 | |
| H69AR | Function assay | 30 mins | Inhibition of ABCC1 in human H69AR cells assessed as reduction in calcein AM levels preincubated for 30 mins followed by calcein AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay, IC50 = 2.97 μM. | 28471656 | |
| A2780/ADR | Function assay | 30 mins | Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured at 60 secs interval for 60 mins by fluorescence assay, IC50 = 1.21 μM. | 28841513 | |
| H69AR | Function assay | 30 mins | Inhibition of ABCC1 in human H69AR cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured at 60 secs interval for 60 mins by fluorescence assay, IC50 = 3.53 μM. | 28841513 | |
| C57BL/6 mouse lymph node cells | Immunosuppressive assay | 24 hrs | Immunosuppressive activity in C57BL/6 mouse lymph node cells after 24 hrs by MTT assay, IC50 = 0.5 μM. | 29871844 | |
| HuH7 | Antiviral assay | 3 days | Antiviral activity against HCV genotype 2a infected in human HuH7 cells after 3 days by dual-glo luciferase reporter gene assay, EC50 = 0.773 μM. | 30074795 | |
| MT4 | Cytotoxicity assay | 4 to 5 days | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by cell-titer glo assay, CC50 = 5.608 μM. | 30074795 | |
| mouse mammary carcinoma cell line EMT6/AR 1.0 | Function assay | Reversal effect on the accumulation of [3H]- daunorubicin in mouse mammary carcinoma cell line EMT6/AR 1.0, IC50=0.44 μM | 10098671 | ||
| KB cell | Function assay | Inhibitory activity against KB cell line after 72 h of drug exposure, IC50=0.6 μM | 15481991 | ||
| LLC-PK1 epithelial cells | Function assay | Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay， IC50=0.7 μM | 12699389 | ||
| A2780/ADR cells | Function assay | Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay， IC50=1.41254 μM | 17890094 | ||
| guinea pig ventricular myocytes | Function assay | Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes, IC50=2 μM | 22761000 | ||
| human Caco2 cells | Function assay | nhibition of P-gp in human Caco2 cells assessed as reduction in digoxin efflux, IC50=2.9 μM | 23382458 | ||
| leukemia CEM cells | Function assay | Inhibitory activity against Human MDR1 P-Glycoprotein ABC Transporter using leukemia CEM cells, IC50=3.4 μM | 12361387 | ||
| human HeLa cells | Function assay | Antiviral activity against HPV-18 infected in human HeLa cells assessed as inhibition of viral replication after 7 days， TC50=4.6 μM | 18212100 | ||
| human 2008 cells | Function assay | Inhibition of human MRP1 in human 2008 cells, IC50=4.78 μM | 18707884 | ||
| human HuH7 cells | Cytotoxic?assay | Cytotoxicity against human HuH7 cells assessed as release of lactate dehydrogenase, IC50=5.81 μM | 20943390 | ||
| human HeLa cells | Cytotoxic?assay | Cytotoxicity against human HeLa cells, TC50=8.3 μM | 18212100 | ||
| MDCK cells | Cytotoxic?assay | Cytotoxicity against MDCK cells, TC50=9.9 μM | 18212100 | ||
| rat H42E cells | Cytotoxic?assay | Cytotoxicity against rat H42E cells assessed as intracellular ATP level, TC50=42 μM | 19502058 | ||
| CK1 cells | Function assay | Antiviral activity against HPV-33 infected in CK1 cells assessed as inhibition of viral replication after 7 days, TC50=0.3 μM | 18212100 | ||
| HEK293 cells | Function assay | Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells assessed as protein-mediated pitavastatin uptake， Ki=0.2 μM | 22587986 | ||
| human PBMC | Proliferation assay | Antiproliferative activity against human PBMC, IC50=12 nM | 15679309 | ||
| human T-cell | Function assay | In vitro inhibitory activity against human T-cell production of lymphokine IL-2, IC50=8.1 nM | 7537331 | ||
| Jurkat cells | Function assay | Immunosuppressive activity was measured by inhibition of the IL-2 production in Jurkat cells, IC50=2 nM | 14643337 | ||
| HepG2 cells | Function assay | Inhibition of liver stage Plasmodium berghei infection in HepG2 cells, IC50=1.65 nM | 22586124 | ||
| Jurkat | Function assay | The compound was tested in vitro for inhibition of IL-2 release stimulated with PMA/ionomycin by Jurkat cells., IC50 = 0.012 μM. | 7473543 | ||
| mouse spleen cells | Function assay | The compound was tested in vitro for inhibition of proliferation in BDF1 mouse spleen cells stimulated with concanavalin A (ConA)., IC50 = 0.04 μM. | 7473543 | ||
| Sf9 | Function assay | inhibition of Verapamil stimulated ATP hydrolysis in membranes from MDR1-expressing Sf9 cells, Ki = 0.02 μM. | 7514263 | ||
| LLC-PK1 | Function assay | transepithelial transport (basal to apical) in MDR1-expressing LLC-PK1 cells, Km = 8.4 μM. | 7681059 | ||
| HeLa | Function assay | inhibition of LTC4 uptake in membrane vesicle from MRP1-expressing HeLa cells, Ki = 5 μM. | 7961706 | ||
| Caco-2 | Function assay | transepithelial transport (basal to apical) in Caco-2 cells, Km = 3.8 μM. | 8842452 | ||
| spleen | Function assay | Effect of compound on IL-2 production from alloantigen-stimulated mouse spleen cells, IC50 = 0.01 μM. | 8893839 | ||
| COS | Function assay | inhibition of Taurocholate uptake in ASBT-expressing COS cells, Ki = 24 μM. | 9458785 | ||
| LLC-PK1 | Function assay | inhibition of Doxorubicin transepithelial transport (basal to apical) (Digoxin: 0.8 uM) in MDR1-expressing LLC-PK1 cells, IC50 = 3.66 μM. | 9914792 | ||
| CEM/VLB100 | Function assay | inhibition of Calcein-AM efflux in CEM/VLB100 cells, Ki = 1.8 μM. | 10198227 | ||
| HEK | Function assay | inhibition of BMG uptake in membrane vesicles from Mrp2-expressing HEK cells, Ki = 10 μM. | 10421658 | ||
| HEK | Function assay | inhibition of BMG uptake in membrane vesicles from MRP2-expressing HEK cells, Ki = 21 μM. | 10421658 | ||
| HeLa | Function assay | inhibition of Taurocholate uptake in NTCP-expressing HeLa cells, IC50 = 1 μM. | 10565843 | ||
| LLC-PK1 | Function assay | inhibition of LTC4 uptake in membrane vesicles from MRP2-expressing LLC PK1 cells, Ki = 4.7 μM. | 10570049 | ||
| Sf9 | Function assay | inhibition of Taurocholate uptake in membrane vesicles from Bsep-expressing Sf9 cells, Ki = 0.3 μM. | 10648470 | ||
| Caco-2 | Function assay | inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells, IC50 = 1.3 μM. | 10820137 | ||
| CEM/VLB100 | Function assay | inhibition of Calcein-AM efflux (Calcein-AM: 0.25 uM) in CEM/VLB100 cells, IC50 = 3.41 μM. | 10891114 | ||
| Sf9 | Function assay | inhibition of ATPase in membrane vesicle from BCRP-expressing Sf9 cells, Ki = 0.5 μM. | 11437380 | ||
| NIH-3T3-G185 | Function assay | inhibition of Daunorubicin efflux in NIH-3T3-G185 cells, IC50 = 1.4 μM. | 11716514 | ||
| NIH-3T3-G185 | Function assay | inhibition of Calcein-AM efflux in NIH-3T3-G185 cells, IC50 = 1.7 μM. | 11716514 | ||
| NIH-3T3-G185 | Function assay | inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells, IC50 = 1.7 μM. | 11716514 | ||
| NIH-3T3-G185 | Function assay | inhibition of LDS-751 efflux in NIH-3T3-G185 cells, IC50 = 1.8 μM. | 11716514 | ||
| NIH-3T3-G185 | Function assay | inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells, IC50 = 2.1 μM. | 11716514 | ||
| NIH-3T3-G185 | Function assay | inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells, IC50 = 2.4 μM. | 11716514 | ||
| NIH-3T3-G185 | Function assay | inhibition of JC-1 efflux in NIH-3T3-G185 cells, IC50 = 4.3 μM. | 11716514 | ||
| MDA-435/LCC6 and MDA-435/LCC6-MDRI | Function assay | Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%., EC50 = 0.5 μM. | 11784143 | ||
| MDA-435/LCC6 | Function assay | Effect on reversal of [3H]- VBL accumulation in MDA-435/LCC6 (Pgp-negative) cells., EC50 = 0.6 μM. | 11784143 | ||
| MDA-435/LCC6 and MDA-435/LCC6-MDRI | Function assay | Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%, EC50 = 0.6 μM. | 11784143 | ||
| MDA435/LCC6 MDR1 | Function assay | reversal of Vinblastine accumulation (Vinblastine: 0.005 uM) in MDA435/LCC6 MDR1 cells, EC50 = 0.6 μM. | 11784143 | ||
| MDA-435/LCC6 (Pgp-negative) | Function assay | Effect on reversal of DOX accumulation in MDA-435/LCC6 (Pgp-negative) cells., EC50 = 0.7 μM. | 11784143 | ||
| MDA-435/LCC6 | Growth inhibitory assay | Growth inhibitory activity on MDA-435/LCC6 (Pgp-positive) human breast cancer cells., IC50 = 1 μM. | 11784143 | ||
| MDA-435/LCC6-MDRI | Growth inhibitory assay | Growth inhibitory activity on MDA-435/LCC6-MDRI (Pgp-negative) human breast cancer cells., IC50 = 1.1 μM. | 11784143 | ||
| BTI-TN5B1-4 | Function assay | ATP hydrolysis in membrane fraction from High Five (BTI-TN5B1-4) cells, Km = 0.17 μM. | 11785684 | ||
| Jurkat | Function assay | Inhibition of production of IL-2 secretion in Jurkat cells, IC50 = 0.007 μM. | 11881984 | ||
| Jurkat | Function assay | Inhibition of production of beta-galactosidase IL-2 RGA in Jurkat cells, IC50 = 0.008 μM. | 11881984 | ||
| LLC-PK1 | Function assay | increase in Vinblastine intracellular accumulation in MDR1-expressing LLC-PK1 cells, Ki = 1.3 μM. | 11961113 | ||
| LLC-PK1 | Function assay | increase in Calcein-AM intracellular accumulation in MDR1-expressing LLC-PK1 cells, Ki = 4.66 μM. | 11961113 | ||
| MDCK | Function assay | inhibition of Digoxin transepithelial transport (basal to apical) in MDR1-expressing MDCK cells, Ki = 2.18 μM. | 12134945 | ||
| MDCK | Function assay | inhibition of Vinblastine transepithelial transport (basal to apical) in MRP2-expressing MDCK cells, Ki = 8.11 μM. | 12134946 | ||
| LLC-PK1 | Function assay | increase in Calcein-AM intracellular accumulation in mdr1b-expressing LLC-PK1 cells, Ki = 3.5 μM. | 12235267 | ||
| LLC-PK1 | Function assay | increase in Calcein-AM intracellular accumulation in mdr1a-expressing LLC-PK1 cells, Ki = 3.65 μM. | 12235267 | ||
| HL-60 | Function assay | Inhibitory activity against Human formylpeptide receptor (FPR) of human leukemia HL-60 cells, IC20 = 3.6 μM. | 12361388 | ||
| High Five cells | Function assay | inhibition of Taurochenodeoxycholate uptake(CsA 30uM, 30 % of control) in membrane vesicles prepared from High Five cells infected with the ABCB11 baculovirus, Ki = 9.5 μM. | 12404239 | ||
| MDCKII | Function assay | inhibition of Cerivastatin uptake in OATP2-expressing MDCKII cells, Ki = 0.238 μM. | 12538813 | ||
| Caco-2 | Function assay | transepithelial transport of digoxin (basal to apical) in Caco-2 cells, Ki = 0.35 μM. | 12636153 | ||
| SK-E2 | Function assay | increase in bodipy intracellular accumulation (Bodipy: 0.2 uM) in SK-E2 cells (expressing BSEP), IC50 = 7.5 μM. | 12739759 | ||
| SK-E2 | Function assay | increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP), IC50 = 7.8 μM. | 12739759 | ||
| HEK293 | Function assay | inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cells, Ki = 0.2 μM. | 14530907 | ||
| T-cells | Function assay | Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method, IC50 = 0.032 μM. | 14593182 | ||
| T-cells | Function assay | Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method, IC50 = 0.074 μM. | 14593182 | ||
| mouse spleen cells | Cytotoxicity assay | Cytotoxicity against BALB/c mouse spleen cells, CC50 = 1.35 μM. | 17081761 | ||
| MDCK2 | Function assay | Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells, IC50 = 9.34 μM. | 17664327 | ||
| HEK293 | Function assay | Inhibition of cross-linking of human Pgp TM1 L65R/TM6 L339C/TM7 F728 mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 0.5 μM. | 17848563 | ||
| HEK293 | Function assay | Inhibition of cross-linking of human Pgp TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 0.6 μM. | 17848563 | ||
| HEK293 | Function assay | Inhibition of cross-linking of human Pgp TM3T199R/TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 1.1 μM. | 17848563 | ||
| HEK293 | Function assay | Inhibition of cross-linking of human Pgp TM6 F343R/TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 11 μM. | 17848563 | ||
| HEK293 | Function assay | Inhibition of cross-linking of human Pgp TM5 I306R/TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 15 μM. | 17848563 | ||
| Caco-2 | Function assay | Inhibition of P-glycoprotein-mediated [3H]vinblastine transport in human Caco-2 cells, EC50 = 45.5 μM. | 18524592 | ||
| A2780 | Function assay | Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay, IC50 = 1.41254 μM. | 18678495 | ||
| A2780/ADR | Function assay | Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay, IC50 = 1.4 μM. | 19250834 | ||
| C2C12 | Function assay | Inhibition of serum withdrawal-induced cell differentiation in mouse C2C12 cells assessed as myosin heavy chain expression. | 20081855 | ||
| mouse spleen cells | Function assay | Inhibition of serine palmitoyltransferase in mouse spleen cells. | 21456524 | ||
| Sf21 | Function assay | Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50 = 0.5 μM. | 21965623 | ||
| Sf21 | Function assay | Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50 = 0.6 μM. | 21965623 | ||
| T-cells | Function assay | Inhibition of CD4 expression in human CD4+ T cells, IC50 = 8.97 μM. | 22101135 | ||
| HEK293 | Function assay | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, Ki = 1.3 μM. | 22541068 | ||
| HEK293 | Function assay | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, IC50 = 1.4 μM. | 22541068 | ||
| MDA435/LCC6MDR | Function assay | Modulation of p-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversal of paclitaxel resistance, EC50 = 0.032 μM. | 24171478 | ||
| mouse | Function assay | Inhibition of human MDR1 expressed in mouse L5178 cells assessed as increase in intracellular accumulation of rhodamine 123 by FACSCalibur flow cytometry, IC50 = 0.67 μM. | 24900226 | ||
| mouse lymph node cells | Function assay | Inhibition of PI3K-gamma in mouse lymph node cells assessed as inhibition of ConA-stimulated T cell proliferation, IC50 = 0.57 μM. | 26720154 | ||
| MDCK2 | Function assay | 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, IC50 = 25.6 μM. | 27393949 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells. | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells. | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells. | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells. | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells. | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells. | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells. | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells. | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells. | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells. | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells. | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells. | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells. | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells. | 29435139 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Cyclosporin A, 一種非極性環(huán)寡肽，是一種免疫抑制劑，與親環(huán)素結(jié)合，隨后抑制calcineurin，無細胞試驗中IC50為7 nM，廣泛用于預(yù)防器官移植反應(yīng)中的排斥反應(yīng),并已用于在灌注的3D近端小管模型上測試其毒性作用。Cyclosporin A?(NSC 290193) 可用于誘導(dǎo)肝移植慢性排斥反應(yīng)動物模型。 | ||
|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | 在T細胞中，Cyclosporin A與親環(huán)蛋白(免疫親和素)結(jié)合[1]，形成親環(huán)蛋白-Cyclosporin A復(fù)合體，其結(jié)合并抑制鈣調(diào)磷酸酶。[2]Cyclosporin A 抑制鈣調(diào)磷酸酶，IC50 是7 nM[3]，隨后阻斷NF-AT核轉(zhuǎn)運。 [4]Cyclosporin A通過抑制MTP(線粒體通透性轉(zhuǎn)換孔)的開放而影響線粒體，IC50 是39 nM。[5] |
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|---|---|---|---|---|
| 激酶實驗 | 磷酸酶試驗 | |||
| 純化的牛腦鈣調(diào)磷酸酶和鈣調(diào)蛋白是購買的。含純化酶的反應(yīng)混合物包含100 nM 鈣調(diào)磷酸酶，100 nM 鈣調(diào)蛋白，以及5 μM 32P-標(biāo)記磷酸化多肽，60 μl (總體積) 試驗緩沖液包含20 mM Tris (pH 8)，100 mM NaCI，6 mM MgCl2，0.5 mM 二硫蘇糖醇， 每毫升0.1毫克牛血清白蛋白，以及0.1 mM CaCl2或5 mM EGTA。含細胞裂解物的反應(yīng)混合物包含20 μl of未稀釋裂解物， 5 μM 32P-標(biāo)記的磷酸肽，和40 μl 試驗緩沖液。反應(yīng)混合物包含50 μM 多肽412或413和/或 500 nM岡田酸，一種磷酸酶1和2A的特異性抑制劑; 500 nM 岡田酸足以抑制Ca2+-不依賴性磷酸酶，而更高濃度時也會部分抑制Ca2+-依賴性的活性。30°C下培育15分鐘，加入0.5 ml包含5% 三氯乙酸的100 mM 磷酸鉀緩沖液(pH 7.0)終止反應(yīng)。Dowex陽離子交換色譜分離無機磷酸鹽，用閃爍計數(shù)測定數(shù)量。 | ||||
| 細胞實驗 | 細胞系 | Jurkat細胞(無性繁殖J77) | ||
| 濃度 | ~100 nM | |||
| 孵育時間 | 1小時 | |||
| 方法 | 免疫抑制劑以細胞治療濃度的1000倍溶于乙醇。細胞(106)懸浮于微量離心管1ml完全培養(yǎng)基中；1 μl乙醇或者Cyclosporin A乙醇溶液加入反應(yīng)液中，細胞在37°C下培育1小時。細胞在冰浴下用1ml PBS洗兩次，在50μl低滲緩沖液中裂解，緩沖液每毫升包含50 mM Tris (pH 7.5); 0.1 mM EGTA; 1 mM EDTA; 0.5 mM二硫蘇糖醇; 以及50 微克苯甲基磺酰氯，50 微克胰蛋白酶抑制劑，5微克亮抑酶肽，和5 微克抑肽酶。裂解液用液氮冷凍，再在30°C下融化，循環(huán)3次，隨后在 4°C下以12,000×g離心10分鐘。 |
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| 實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | PMID |
| Western blot | Phospho-AKT1 / AKT1 / PTEN / Phospho-BAD / BAD / Procaspase-3 Cyp-D / AIF / β-actin IL-8 / MCP-1 Actin / Smac β-actin / FIPV-N |
|
12644839 | |
| Growth inhibition assay | NPC death |
|
20181586 | |
| IHC | Th22 / Th17 / Th1 / M1 / Th2 Tregs / Bregs / pDCs / M2 Ki 67 / Fas-FasL IFN-γ / TNF-α WT-PCLS / FXRKO-PCLS |
|
30916387 | |
| Immunofluorescence | Human gingival fibroblast cells Human gingival fibroblast cells Calcein Rhod-Dex / Calcein cadherin-9 / vimentin |
|
27857765 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | Cyclosporin A是一種免疫抑制劑，小鼠，大鼠，和荷蘭豬經(jīng)非腸道給藥或者口服給藥都有效[6]，臨床上用于器官移植中預(yù)防免疫排斥。[7] |
|
|---|---|---|
| 動物實驗 | Animal Models | 大鼠 |
| Dosages | 45毫克/千克 | |
| Administration | 口服 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06366685 | Not yet recruiting | Esophageal Cancer|Exercise Training|Psychotherapy|Rehabilitation |
Mengmeng Yuan|Anhui Medical University |
May 1 2024 | Not Applicable |
| NCT06320561 | Not yet recruiting | Stroke |
Vrije Universiteit Brussel|University Ghent|Research Foundation Flanders |
May 2024 | -- |
| NCT05702931 | Not yet recruiting | Hyperglycemia|Renal Transplant Complication Primary Non-Function|Diabetes |
Rigshospitalet Denmark|Aarhus University Hospital|Odense University Hospital |
April 1 2024 | Phase 4 |
| NCT06052761 | Recruiting | Child in Hospital |
Adiyaman University |
February 10 2024 | Not Applicable |
化學(xué)信息&溶解度
| 分子量 | 1202.61 | 分子式 | C62H111N11O12 |
| CAS號 | 59865-13-3 | SDF | Download Cyclosporin A SDF |
| Smiles | CCC1C(=O)N(CC(=O)N(C(C(=O)NC(C(=O)N(C(C(=O)NC(C(=O)NC(C(=O)N(C(C(=O)N(C(C(=O)N(C(C(=O)N(C(C(=O)N1)C(C(C)CC=CC)O)C)C(C)C)C)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)CC(C)C)C)C | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 100 mg/mL ( (83.15 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 100 mg/mL (83.15 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
技術(shù)支持
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* 必填項
常見問題及建議解決方法
問題 1:
What is the difference between S2286 (cyclosporin A) and S1514 (cyclosporin)?
回答：
Cyclosporine is a mixture of Cyclosporine A, derivatives of Cyclosporine A, salts of Cyclosporine A. Cyclosporine A is an especially useful Cyclosporine component.
Tags: buy Cyclosporin A | Cyclosporin A supplier | purchase Cyclosporin A | Cyclosporin A cost | Cyclosporin A manufacturer | order Cyclosporin A | Cyclosporin A distributor
