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  2. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. Drug Metabolite VD/VDR Endogenous Metabolite
  4. Calcitriol

Calcitriol  (Synonyms: 骨化三醇; 1,25-Dihydroxyvitamin D3)

目錄號: HY-10002 純度: 99.94%
COA 產(chǎn)品使用指南

Calcitriol 是活性最大的 vitamin D 代謝物，也是 vitamin D 受體 (VDR) 的激動劑。

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)

Calcitriol Chemical Structure

Calcitriol Chemical Structure

CAS No. : 32222-06-3

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Other Forms of Calcitriol:

MCE 顧客使用本產(chǎn)品發(fā)表的 46 篇科研文獻(xiàn)

WB
Proliferation Assay

    Calcitriol purchased from MCE. Usage Cited in: Int Immunopharmacol. 2017 Jun;47:182-189.  [Abstract]

    The total number of sneezing and nasal rubbing motions is significantly reduced by 1,25-(OH)2D3, n=9.

    Calcitriol purchased from MCE. Usage Cited in: Oncotarget. 2017 Oct 26;8(59):100187-100195.  [Abstract]

    Calcitriol increases the expressions of JMJD3 and p16INK4A. 786-O cells are treated with vehicle (Veh) or 100nM Calcitriol (Cal) for 48h, and untreated group as control (Con). The expressions of JMJD3 and p16INK4A are determined with western blotting.

    • 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

    Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist.

    IC50 & Target

    Human Endogenous Metabolite

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    Bone marrow cell EC50
    100 nM
    Compound: 1-alpha, 25-(OH)2D3
    Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days relative to 1-alpha, 25-(OH)2D3
    Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days relative to 1-alpha, 25-(OH)2D3
    		[PMID: 18539034]
    Bone marrow cell EC50
    2 nM
    Compound: 1-alpha, 25-(OH)2D3
    Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days
    Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days
    		[PMID: 18539034]
    BXPC-3 IC50
    21.07 μM
    Compound: 3; 1,25(OH)2D3
    Antiproliferative activity against human BxPC3 cells after 24 hrs by MTT assay
    Antiproliferative activity against human BxPC3 cells after 24 hrs by MTT assay
    		[PMID: 30193216]
    Caco-2 EC50
    223.4 nM
    Compound: 1,25(OH)2D3
    Activation of VDR in human Caco2 cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
    Activation of VDR in human Caco2 cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
    		[PMID: 27070779]
    Caco-2 IC50
    4.4 μM
    Compound: Calcitriol
    Antipoliferative activity against human Caco2 cells after 48 hrs by MTT assay
    Antipoliferative activity against human Caco2 cells after 48 hrs by MTT assay
    		[PMID: 26562542]
    Caco-2 IC50
    4.46 μM
    Compound: Calcitriol
    Antiproliferative activity against human Caco2 cells after 48 hrs by MTT assay
    Antiproliferative activity against human Caco2 cells after 48 hrs by MTT assay
    		[PMID: 29518319]
    Caco-2 EC50
    515.2 nM
    Compound: 1,25(OH)2D3
    Transactivation of VDR in human Caco2 cells after 24 hrs by luciferase reporter gene assay
    Transactivation of VDR in human Caco2 cells after 24 hrs by luciferase reporter gene assay
    		[PMID: 26367019]
    COS-7 EC50
    50 nM
    Compound: 1, 1,25-(OH)2D3
    Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay
    Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay
    		[PMID: 17904370]
    COS-7 EC50
    500 pM
    Compound: 1, 1,25-(OH)2D3
    Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assay
    Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assay
    		[PMID: 17298045]
    HaCaT EC50
    249.7 nM
    Compound: 1,25(OH)2D3
    Activation of VDR in human HaCaT cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
    Activation of VDR in human HaCaT cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
    		[PMID: 27070779]
    HaCaT EC50
    321.5 nM
    Compound: 1,25(OH)2D3
    Transactivation of VDR in human HaCaT cells after 24 hrs by luciferase reporter gene assay
    Transactivation of VDR in human HaCaT cells after 24 hrs by luciferase reporter gene assay
    		[PMID: 26367019]
    HCT-116 IC50
    0.01 nM
    Compound: 1b, calcitriol
    Cytotoxicity against human HCT116 assessed as decrease in cell count after 120 hrs
    Cytotoxicity against human HCT116 assessed as decrease in cell count after 120 hrs
    		[PMID: 22926068]
    HEK293 IC50
    > 10 μM
    Compound: 1, 1,25-VD3
    Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of transcriptional activity by luciferase and beta-galactosidase reporter gene assay
    Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of transcriptional activity by luciferase and beta-galactosidase reporter gene assay
    		[PMID: 23462715]
    HEK293 EC50
    0.003 μM
    Compound: 1, 1,25-VD3
    Agonist activity at CMX-GAL4 tagged human VDR expressed in HEK293 cells assessed as increase in transcriptional activity by luciferase reporter gene assay
    Agonist activity at CMX-GAL4 tagged human VDR expressed in HEK293 cells assessed as increase in transcriptional activity by luciferase reporter gene assay
    		[PMID: 23462715]
    HEK293 IC50
    0.1 nM
    Compound: 1; 1,25(OH)2D3
    Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with NCoR assessed as decrease in NCoR recruitment by two-hybrid assay
    Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with NCoR assessed as decrease in NCoR recruitment by two-hybrid assay
    		[PMID: 26613420]
    HEK293 EC50
    0.12 nM
    Compound: 1; 1,25(OH)2D3
    Agonist activity at VDR in human HEK293 cells assessed as transcriptional activity after 16 to 24 hrs by luciferase reporter gene assay
    Agonist activity at VDR in human HEK293 cells assessed as transcriptional activity after 16 to 24 hrs by luciferase reporter gene assay
    		[PMID: 26613420]
    HEK293 EC50
    0.6 nM
    Compound: 1; 1,25(OH)2D3
    Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with RXRalpha assessed as RXRalpha recruitment by two-hybrid assay
    Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with RXRalpha assessed as RXRalpha recruitment by two-hybrid assay
    		[PMID: 26613420]
    HEK293 EC50
    1 nM
    Compound: 1, 1,25-(OH)2D3
    Agonist activity at human VDR in HEK293 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay
    Agonist activity at human VDR in HEK293 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay
    		[PMID: 17904370]
    HEK293 EC50
    7.28 x 10-10 M
    Compound: 1,25(OH)2D3, Calcitriol
    Antiproliferative activity against NHEK cells incubated for 24 hrs by [3H]thymidine incorporation assay
    Antiproliferative activity against NHEK cells incubated for 24 hrs by [3H]thymidine incorporation assay
    		[PMID: 22404326]
    HeLa EC50
    1 nM
    Compound: calcitriol, [1alpha,25(OH)2D3]
    Transactivation of GAL4-fused VDR ligand binding domain expressed in human HeLa cells after 16 hrs by luciferase reporter gene assay
    Transactivation of GAL4-fused VDR ligand binding domain expressed in human HeLa cells after 16 hrs by luciferase reporter gene assay
    		[PMID: 22957834]
    HeLa EC50
    2.5 nM
    Compound: calcitriol, [1alpha,25(OH)2D3]
    Transactivation of full length human VDR expressed in human HeLa cells assessed as increase in CYP24 transcription after 18 hrs by luciferase reporter gene assay
    Transactivation of full length human VDR expressed in human HeLa cells assessed as increase in CYP24 transcription after 18 hrs by luciferase reporter gene assay
    		[PMID: 22957834]
    HepG2 IC50
    > 50 μM
    Compound: Calcitriol
    Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
    		[PMID: 29518319]
    HepG2 IC50
    > 50 μM
    Compound: Calcitriol
    Antipoliferative activity against human HepG2 cells after 48 hrs by MTT assay
    Antipoliferative activity against human HepG2 cells after 48 hrs by MTT assay
    		[PMID: 26562542]
    HL-60 EC50
    0.009 μM
    Compound: Calcitriol
    Agonist activity at vitamin D3 receptor in human HL-60 cells assessed as induction of cell differentiation after 96 hrs by NBT dye-based microscopic analysis
    Agonist activity at vitamin D3 receptor in human HL-60 cells assessed as induction of cell differentiation after 96 hrs by NBT dye-based microscopic analysis
    		[PMID: 26562542]
    HL-60 IC50
    0.05 μM
    Compound: 1, 1,25(OH)2D3, calcitriol
    Induction of cell differentiation of human HL60 cells incubated for 144 hrs by Wst-1 dye based assay
    Induction of cell differentiation of human HL60 cells incubated for 144 hrs by Wst-1 dye based assay
    		[PMID: 25180926]
    HL-60 EC50
    17.9 nM
    Compound: Calcitriol
    Induction of human HL60 cell differentiation after 4 days by NBT reduction assay
    Induction of human HL60 cell differentiation after 4 days by NBT reduction assay
    		[PMID: 24035340]
    HL-60 ED50
    2 nM
    Compound: 1, calcitriol, 1alpha,25-(OH)2D3
    Induction of differentiation of human HL60 promyelocytes to monocytes after 4 days by nitro blue tetrazolium reduction assay
    Induction of differentiation of human HL60 promyelocytes to monocytes after 4 days by nitro blue tetrazolium reduction assay
    		[PMID: 26206427]
    HL-60 ED50
    2 nM
    Compound: 1, calcitriol, 1alpha,25-(OH)2D3
    Induction of human HL60 cell differentiation after 4 days by NBT reduction assay
    Induction of human HL60 cell differentiation after 4 days by NBT reduction assay
    		[PMID: 22490010]
    HL-60 EC50
    2 nM
    Compound: 1, 1alpha,25-(OH)2D3, calcitriol
    Induction of differentiation of human HL60 promyelocytes into monocytes after 4 days by NBT reduction assay
    Induction of differentiation of human HL60 promyelocytes into monocytes after 4 days by NBT reduction assay
    		[PMID: 19819702]
    HL-60 EC50
    2 nM
    Compound: 1, 1alpha,25(OH)2D3, calcitriol
    Induction of differentiation of human HL-60 cells promyelocytes to monocytes after 4 days by NBT reduction assay
    Induction of differentiation of human HL-60 cells promyelocytes to monocytes after 4 days by NBT reduction assay
    		[PMID: 18722130]
    HL-60 EC50
    2 nM
    Compound: 1, calcitriol
    Induction of differention of human HL60 cells into monocytes by NBT reduction assay
    Induction of differention of human HL60 cells into monocytes by NBT reduction assay
    		[PMID: 17960924]
    HL-60 EC50
    2150 pM
    Compound: 1, 1,25-(OH)2D3
    Induction of human HL60 cell differentiation to monocytes by NBT reduction assay
    Induction of human HL60 cell differentiation to monocytes by NBT reduction assay
    		[PMID: 17298045]
    HL-60 EC50
    3 nM
    Compound: 1, Calcitriol, 1alpha,25-(OH)2D3
    Induction of human HL60 cell differentiation after 4 days by nitro blue tetrazolium reduction assay
    Induction of human HL60 cell differentiation after 4 days by nitro blue tetrazolium reduction assay
    		[PMID: 22018918]
    HL-60 ED50
    3 nM
    Compound: 1; calcitriol; 1alpha,25-(OH)2D3
    Induction of human HL60 cell differentiation assessed as differentiation from promyelocytes to monocytes by NBT assay
    Induction of human HL60 cell differentiation assessed as differentiation from promyelocytes to monocytes by NBT assay
    		[PMID: 26630444]
    HL-60 ED50
    3 nM
    Compound: 1, 1alpha,25-(OH)2D3,calcitriol
    Induction of human HL60 cell differentiation into monocytes after 4 days by NBT reduction assay
    Induction of human HL60 cell differentiation into monocytes after 4 days by NBT reduction assay
    		[PMID: 19402630]
    HL-60 EC50
    3 nM
    Compound: 1, calcitriol
    Induction of cell differentiation of human HL60 cells to monocytes by NBT reduction assay
    Induction of cell differentiation of human HL60 cells to monocytes by NBT reduction assay
    		[PMID: 19167893]
    HN12 IC50
    4.68 nM
    Compound: 1b, calcitriol
    Cytotoxicity against human HN12 assessed as decrease in cell count after 120 hrs
    Cytotoxicity against human HN12 assessed as decrease in cell count after 120 hrs
    		[PMID: 22926068]
    HN12 IC50
    553 nM
    Compound: calcitriol
    Antiproliferative activity against human HN12 cells assessed as decrease in cell number after 72 hrs by WST assay
    Antiproliferative activity against human HN12 cells assessed as decrease in cell number after 72 hrs by WST assay
    		[PMID: 24900339]
    HOS EC50
    0.01 nM
    Compound: 1alpha,25(OH)2D3
    Activity at human VDR expressed in human HOS cells transfected with pGL3-hOc, pCDNA-hVDR and phRL-TK assessed as assessed as transcriptional activation measured 24 hrs post infection by luciferase reporter gene assay
    Activity at human VDR expressed in human HOS cells transfected with pGL3-hOc, pCDNA-hVDR and phRL-TK assessed as assessed as transcriptional activation measured 24 hrs post infection by luciferase reporter gene assay
    		[PMID: 21889334]
    HOS EC50
    0.011 nM
    Compound: 1-alpha,25(OH)2D3
    Agonist activity at human VDR expressed in HOS cells co-expressing human RXR by Dual-Glo luciferase reporter gene assay
    Agonist activity at human VDR expressed in HOS cells co-expressing human RXR by Dual-Glo luciferase reporter gene assay
    		[PMID: 30446437]
    Huh-7 EC50
    0.0003 μM
    Compound: 1alpha,25-dihydroxyvitamin D3
    Agonist activity at VDR expressed in human HuH7 cells after 24 hrs by pDR3-luciferase reporter gene assay
    Agonist activity at VDR expressed in human HuH7 cells after 24 hrs by pDR3-luciferase reporter gene assay
    		[PMID: 27145071]
    Jurkat EC50
    3.936 nM
    Compound: 1,25(OH)2D3
    Activation of VDR in human Jurkat cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
    Activation of VDR in human Jurkat cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
    		[PMID: 27070779]
    L02 IC50
    0.67 μM
    Compound: Calcitriol
    Antiproliferative activity against human L02 cells after 48 hrs by MTT assay
    Antiproliferative activity against human L02 cells after 48 hrs by MTT assay
    		[PMID: 29518319]
    L02 IC50
    0.67 μM
    Compound: Calcitriol
    Cytotoxicity against human L02 cells after 48 hrs by MTT assay
    Cytotoxicity against human L02 cells after 48 hrs by MTT assay
    		[PMID: 26562542]
    L02 IC50
    48 μM
    Compound: 1; 1,25(OH)2D3
    Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 30579121]
    MCF7 IC50
    > 50 μM
    Compound: 3; 1,25(OH)2D3
    Antiproliferative activity against human MCF7 cells expressing VDR siRNA assessed as reduction in BrdU incorporation after 16 hrs by ELISA
    Antiproliferative activity against human MCF7 cells expressing VDR siRNA assessed as reduction in BrdU incorporation after 16 hrs by ELISA
    		[PMID: 30193216]
    MCF7 IC50
    11.1 μM
    Compound: 1; 1,25(OH)2D3
    Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
    		[PMID: 30579121]
    MCF7 IC50
    11.43 μM
    Compound: 3; 1,25(OH)2D3
    Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
    		[PMID: 30193216]
    MCF7 IC50
    12.5 μM
    Compound: 1alpha,25-dihydroxyvitamin D3
    Antiproliferative activity against human MCF7 cells assessed as inhibition of proliferation after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as inhibition of proliferation after 72 hrs by MTT assay
    		[PMID: 25127149]
    MCF7 EC50
    3.28 nM
    Compound: 1, 1alpha,25-(OH)2D3, 1,25D, calcitriol
    Agonist activity at VDR in human MCF7 cells assessed as transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assay
    Agonist activity at VDR in human MCF7 cells assessed as transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assay
    		[PMID: 22989379]
    MCF7 EC50
    5.2 x 10-2 μM
    Compound: 1
    Antiproliferative activity against human MCF7 cells after 72 hrs by [3H]thymidine incorporation assay
    Antiproliferative activity against human MCF7 cells after 72 hrs by [3H]thymidine incorporation assay
    		[PMID: 19739672]
    MCF7 EC50
    5.5 nM
    Compound: 1alpha,25(OH)2D3
    Agonist activity at zebrafish gal4-VDR LBD expressed in human MCF7 cells by luciferase reporter gene based transactivation assay
    Agonist activity at zebrafish gal4-VDR LBD expressed in human MCF7 cells by luciferase reporter gene based transactivation assay
    		[PMID: 22180837]
    MCF7 IC50
    5.59 μM
    Compound: Calcitriol
    Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
    		[PMID: 29518319]
    MCF7 IC50
    5.6 μM
    Compound: Calcitriol
    Antipoliferative activity against human MCF7 cells after 48 hrs by MTT assay
    Antipoliferative activity against human MCF7 cells after 48 hrs by MTT assay
    		[PMID: 26562542]
    Medulloblastoma cell GI50
    1.4 μM
    Compound: 3
    Antiproliferative activity against medulloblastoma cells derived from conditional patched knockout mouse after 48 hrs by [3H]-thymidine incorporation assay
    Antiproliferative activity against medulloblastoma cells derived from conditional patched knockout mouse after 48 hrs by [3H]-thymidine incorporation assay
    		[PMID: 30471551]
    PBMC IC50
    1 nM
    Compound: 1
    Inhibition of LPS-induced IL12/23p40 production in human PBMC after 24 hrs by ELISA
    Inhibition of LPS-induced IL12/23p40 production in human PBMC after 24 hrs by ELISA
    		[PMID: 19309155]
    PBMC IC50
    1.2 x 10-2 μM
    Compound: 1
    Inhibition of LPS-induced IL6 production in human PBMC after 24 hrs by ELISA
    Inhibition of LPS-induced IL6 production in human PBMC after 24 hrs by ELISA
    		[PMID: 19309155]
    PBMC IC50
    29 pM
    Compound: 1
    Inhibition of LPS-induced TNFalpha production in human PBMC after 24 hrs by ELISA
    Inhibition of LPS-induced TNFalpha production in human PBMC after 24 hrs by ELISA
    		[PMID: 19309155]
    PBMC IC50
    8 nM
    Compound: 1
    Inhibition of IFN-gamma production in human PBMC after 5 days by ELISA-based mixed lymphocyte reaction assay
    Inhibition of IFN-gamma production in human PBMC after 5 days by ELISA-based mixed lymphocyte reaction assay
    		[PMID: 19309155]
    PC-3 IC50
    17.2 μM
    Compound: Calcitriol
    Antipoliferative activity against human PC3 cells after 48 hrs by MTT assay
    Antipoliferative activity against human PC3 cells after 48 hrs by MTT assay
    		[PMID: 26562542]
    PC-3 IC50
    17.25 μM
    Compound: Calcitriol
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    		[PMID: 29518319]
    PC-3 IC50
    9.53 μM
    Compound: 3; 1,25(OH)2D3
    Antiproliferative activity against human PC3 cells after 24 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 24 hrs by MTT assay
    		[PMID: 30193216]
    SW480 IC50
    16.78 μM
    Compound: 78
    Anticancer activity against human SW480 cells assessed as reduction in cell proliferation incubated for 2 days by CCK-8 assay
    Anticancer activity against human SW480 cells assessed as reduction in cell proliferation incubated for 2 days by CCK-8 assay
    		[PMID: 33445154]
    T47D IC50
    1.3 nM
    Compound: calcitriol
    Antiproliferative activity against human T47D cells assessed as decrease in cell number after 72 hrs by WST assay
    Antiproliferative activity against human T47D cells assessed as decrease in cell number after 72 hrs by WST assay
    		[PMID: 24900339]
    THP-1 EC50
    1 x 10-2 μM
    Compound: 1
    Activation of VDR in human THP1 cells assessed as increase in 25-hydroxyvitamin D-24-hydroxylase mRNA expression by RT-PCR
    Activation of VDR in human THP1 cells assessed as increase in 25-hydroxyvitamin D-24-hydroxylase mRNA expression by RT-PCR
    		[PMID: 19309155]
    THP-1 EC50
    1 x 10-2 μM
    Compound: 1
    Activation of VDR in human THP1 cells assessed as increase in cathelicidin antimicrobial peptide mRNA expression by RT-PCR
    Activation of VDR in human THP1 cells assessed as increase in cathelicidin antimicrobial peptide mRNA expression by RT-PCR
    		[PMID: 19309155]
    體外研究
    (In Vitro)

    Calcitriol 對宮頸癌細(xì)胞具有體外抗增殖作用。與對照組相比，用 100 nM Calcitriol 處理 6 天后，細(xì)胞數(shù)量減少了 12.8%。隨著 Calcitriol 濃度的增加，細(xì)胞增殖的抑制作用更加明顯。200 nM 和 500 nM Calcitriol 分別減少了 26.1% 和 31.6%。用 Calcitriol 處理 72 小時(shí)后，G1 期細(xì)胞明顯聚集，200 nM 約 66.18%，500 nM 約 78.10%，而對照組則為（24.36%）。與對照組相比，則為 治療可顯著降低 HCCR-1 蛋白表達(dá)，且呈時(shí)間和劑量依賴性[1]。 Calcitriol 可顯著增加 ERα mRNA，且呈劑量依賴性，EC50 為 9.8×10-9 M[2]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    長期使用 Calcitriol 處理（每天 150 ng/kg，持續(xù) 4.5 個(gè)月）可改善松弛（骨化三醇治療的 OVX 大鼠中 pD2：6.30，Emax：68.6%）。OVX 大鼠雙腎的腎血流量均減少，Calcitriol 可恢復(fù)血流量。長期使用 Calcitriol 可降低 OVX 大鼠腎動脈中 COX-2 和血栓素-前列腺素 (TP) 受體表達(dá)的增加[3]。高劑量和低劑量 Calcitriol 治療使第 56 天的果糖喂養(yǎng)大鼠的收縮壓 (SBP) 分別顯著降低 14 和 9 mmHg。與其他組相比，高劑量 Calcitriol 治療（每天 20 ng/kg）顯著提高血清離子鈣水平[4]。

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

    416.64

    Formula

    C27H44O3
    CAS 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    骨化三醇；鈣三醇
    結(jié)構(gòu)分類
    初始來源
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式

    -20°C, protect from light, stored under nitrogen

    *該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

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

    DMSO 中的溶解度 : 110 mg/mL (264.02 mM; 超聲助溶; 吸濕的 DMSO 對產(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 : 100 mg/mL (240.02 mM; 超聲助溶)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.4002 mL 12.0009 mL 24.0017 mL
    5 mM 0.4800 mL 2.4002 mL 4.8003 mL
    查看完整儲備液配制表

    * 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備液；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

    • 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

    動物實(shí)驗(yàn)：

    請根據(jù)您的 實(shí)驗(yàn)動物和給藥方式 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，澄清的儲備液可以根據(jù)儲存條件，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： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.75 mg/mL (6.60 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.75 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 27.5 mg/mL 的澄清 DMSO 儲備液加到 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。
    • 方案 二

      請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.75 mg/mL (6.60 mM); 澄清溶液

      此方案可獲得 ≥ 2.75 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 27.5 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
    動物溶解方案計(jì)算器
    請輸入動物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動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
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

    *該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

    您所需的儲備液濃度超過該產(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。
    動物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，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: 99.94%

    參考文獻(xiàn)
    Cell Assay
    [1]

    HeLa S3 cells are plated at a density of 1,000 cells/well in 96-well plates of Dulbecco’s modified Eagle’s medium (DMEM) with 10% fetal bovine serum (FBS), treated with 1% ethanol (control) or various concentrations of Calcitriol (100, 200, and 500 nM) for 72 h. A Cell Counting Kit8 (CCK-8) is used to determine cell proliferation. At 24, 48, 72, 96, 120, and 144 h after culturing with 200 nM Calcitriol, cells are harvested for analysis. Three independent experiments are performed in quadruplicate[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Adult female Sprague-Dawley rats weighing 200 to 220g are used in this study. Rats are housed in a temperature-controlled room (~23°C) with a 12-h light/dark cycle. The animals have free access to a standard diet and water. Ovariectomy (OVX) is performed on rats. At 6 months after the surgical procedure, the OVX rats are randomly assigned to either treatment with vehicle dimethyl sulfoxide (OVX+vehicle) or Calcitriol (150 ng/kg daily, OVX+calcitriol). Calcitriol treatment is given by oral gavage and lasted or 4.5 months. Blood pressure and serum Calcitriol level are measured[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    參考文獻(xiàn)

    完整儲備液配制表

    * 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備液；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

    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 2.4002 mL 12.0009 mL 24.0017 mL 60.0043 mL
    5 mM 0.4800 mL 2.4002 mL 4.8003 mL 12.0009 mL
    10 mM 0.2400 mL 1.2001 mL 2.4002 mL 6.0004 mL
    15 mM 0.1600 mL 0.8001 mL 1.6001 mL 4.0003 mL
    20 mM 0.1200 mL 0.6000 mL 1.2001 mL 3.0002 mL
    25 mM 0.0960 mL 0.4800 mL 0.9601 mL 2.4002 mL
    30 mM 0.0800 mL 0.4000 mL 0.8001 mL 2.0001 mL
    40 mM 0.0600 mL 0.3000 mL 0.6000 mL 1.5001 mL
    50 mM 0.0480 mL 0.2400 mL 0.4800 mL 1.2001 mL
    60 mM 0.0400 mL 0.2000 mL 0.4000 mL 1.0001 mL
    80 mM 0.0300 mL 0.1500 mL 0.3000 mL 0.7501 mL
    100 mM 0.0240 mL 0.1200 mL 0.2400 mL 0.6000 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：
    Calcitriol
    目錄號：
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