Calcitriol (Synonyms: 1,25-Dihydroxyvitamin D3)

Name: Calcitriol
Brand: MedChemExpress
SKU: HY-10002
Rating: 5.0 (50 reviews)

Cat. No.: HY-10002 Purity: 99.94%: FAQs
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Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist.

For research use only. We do not sell to patients.

Calcitriol Chemical Structure

CAS No. : 32222-06-3

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Based on 50 publication(s) in Google Scholar

Other Forms of Calcitriol:

48 Publications Citing Use of MCE Calcitriol

Proliferation Assay

: Calcitriol purchased from MedChemExpress. 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 MedChemExpress. 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.

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Biological Activity
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Description

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

IC₅₀ & Target

Human Endogenous Metabolite

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]

In Vitro

Calcitriol exerts antiproliferative effects on cervical cancer cells in vitro. Cells decrease by 12.8% when treated with 100 nM Calcitriol for 6 days, compare with control. Inhibition of cell proliferation becomes more pronounced with the increase in Calcitriol concentration. The decrease is 26.1% and 31.6% for 200 and 500 nM Calcitriol, respectively. Treatment with Calcitriol for 72 h induces an evident accumulation of cells in the G1 phase, with approximately 66.18% in 200 nM and 78.10% in 500 nM, compare with the control (24.36%). Calcitriol treatment significantly decreases HCCR-1 protein expression compare with the control in a time- and dose-dependent manner^[1]. Calcitriol significantly increases ERα mRNA in a dose dependent manner with an EC₅₀ of 9.8×10^-9 M^[2].

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

In Vivo

Chronic treatment with Calcitriol (150 ng/kg per day for 4.5 months) improves the relaxations (pD₂: 6.30±0.09, E_max: 68.6±3.9% in Calcitriol-treated OVX, n=8). Renal blood flow in OVX rats is reduced in both kidneys, and the flow is restored by Calcitriol treatment. The increased expression of COX-2 and Thromboxane-prostanoid (TP) receptor in OVX rat renal arteries is reduced by chronic calcitriol administration^[3]. High- and low-dose Calcitriol treatment significantly decreases the systolic blood pressure (SBP) in the fructose-fed rats by 14±4 and 9±4 mmHg, respectively, at Day 56. High-dose Calcitriol treatment (20 ng/kg per day) significantly increases serum ionized calcium level (1.44±0.05 mmol/L) compare with the other groups^[4].

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

Clinical Trial

Molecular Weight

416.64

Formula

C₂₇H₄₄O₃

CAS No.

32222-06-3

Appearance

Solid

Color

White to off-white

SMILES

C=C1[C@H](C[C@@H](C/C1=C/C=C2[C@]3([C@@](C)([C@H](CC3)[C@@H](CCCC(C)(O)C)C)CCC/2)[H])O)O

Structure Classification

Others

Initial Source

Endogenous metabolite

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility

In Vitro:

DMSO : 110 mg/mL (264.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 100 mg/mL (240.02 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	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
10 mM	0.2400 mL	1.2001 mL	2.4002 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.75 mg/mL (6.60 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (6.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.75 mg/mL (6.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.75 mg/mL (6.60 mM); Clear solution
Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (6.60 mM); Clear solution
Protocol 6

Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 7

Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 8

Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 9

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: 0.55 mg/mL (1.32 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*The compound is unstable in solutions, freshly prepared is recommended.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (282 KB) SDS (644 KB)

COA (252 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Wang G, et al. Calcitriol Inhibits Cervical Cancer Cell Proliferation Through Downregulation of HCCR1 Expression. Oncol Res. 2014;22(5-6):301-9. [Content Brief]

[2]. Santos-Martínez N, et al. Calcitriol restores antiestrogen responsiveness in estrogen receptor negative breast cancer cells: a potential new therapeutic approach. BMC Cancer. 2014 Mar 29;14:230. [Content Brief]

[3]. Dong J, et al. Calcitriol restores renovascular function in estrogen-deficient rats through downregulation of cyclooxygenase-2 and the thromboxane-prostanoid receptor. Kidney Int. 2013 Jul;84(1):54-63. [Content Brief]

[4]. Chou CL, et al. Beneficial effects of calcitriol on hypertension, glucose intolerance, impairment of endothelium-dependent vascular relaxation, and visceral adiposity in fructose-fed hypertensive rats. PLoS One. 2015 Mar 16;10(3):e0119843. [Content Brief]

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.
References	[1]. Wang G, et al. Calcitriol Inhibits Cervical Cancer Cell Proliferation Through Downregulation of HCCR1 Expression. Oncol Res. 2014;22(5-6):301-9. [Content Brief] [2]. Santos-Martínez N, et al. Calcitriol restores antiestrogen responsiveness in estrogen receptor negative breast cancer cells: a potential new therapeutic approach. BMC Cancer. 2014 Mar 29;14:230. [Content Brief] [3]. Dong J, et al. Calcitriol restores renovascular function in estrogen-deficient rats through downregulation of cyclooxygenase-2 and the thromboxane-prostanoid receptor. Kidney Int. 2013 Jul;84(1):54-63. [Content Brief] [4]. Chou CL, et al. Beneficial effects of calcitriol on hypertension, glucose intolerance, impairment of endothelium-dependent vascular relaxation, and visceral adiposity in fructose-fed hypertensive rats. PLoS One. 2015 Mar 16;10(3):e0119843. [Content Brief]

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent	Concentration Solvent Mass	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

Calcitriol Related Classifications

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.

Keywords:

Calcitriol32222-06-31,25-Dihydroxyvitamin D3Drug MetaboliteVD/VDREndogenous MetaboliteVitamin DVitamin D receptorInhibitorinhibitorinhibit

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Calcitriol (Synonyms: 1,25-Dihydroxyvitamin D3)

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