Art. -Nr.: HY-10002

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Calcitriol

(Synonyms: 1,25-Dihydroxyvitamin D3)

76 Cited Publications

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

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Reinheit: 99.94%
CAS. Nr.: 32222-06-3
Formel: C₂₇H₄₄O₃
Molecular Weight:416.64

Speicherung:

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

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

Calcitriol Chemical Structure

CAS. Nr.: 32222-06-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (76)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
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Biologische Aktivität

Beschreibung

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

IC₅₀ & Target

Human Endogenous Metabolite

Alle Endogenous Metabolite Isoform-spezifische Produkte anzeigen :

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	EC₅₀	3.52 nM Compound: (1alpha 25-(OH)2D3	Effect on VDR transcriptional activity in human Caco-2 cells in presence of 5% fetal calf serum Effect on VDR transcriptional activity in human Caco-2 cells in presence of 5% fetal calf serum	[PMID: 18054230]
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]
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]
COS-1	IC₅₀	0.8 nM Compound: 1, calcitriol	Displacement of 1-alpha, 25-(OH)[3H]D3 from human VDR expressed in COS1 cells Displacement of 1-alpha, 25-(OH)[3H]D3 from human VDR expressed in COS1 cells	[PMID: 17924616]
COS-7	EC₅₀	5 x 10^-10 M 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]
CV-1	ED₅₀	0.4 μM Compound: 1	Effect on VDR-mediated transcriptional activity in CV1 cells transfected with human recombinant VDR Effect on VDR-mediated transcriptional activity in CV1 cells transfected with human recombinant VDR	[PMID: 15615534]
CV-1	ED₅₀	0.7 nM Compound: 1, calcitriol	Activity on human VDR-mediated transcription of osteocalcin VDRE fused to thymidine kinase promoter/growth hormone reporter gene in CV1 cells Activity on human VDR-mediated transcription of osteocalcin VDRE fused to thymidine kinase promoter/growth hormone reporter gene in CV1 cells	[PMID: 17149880]
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	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	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 x 10^-9 M 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]
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	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]
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	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]
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]
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	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	EC₅₀	2 x 10^-9 M 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 x 10^-9 M 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 x 10^-9 M 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 x 10^-9 M 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]
HL-60	EC₅₀	3 x 10^-9 M 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	1 nM Compound: 1, 1alpha,25-(OH)2D3, calcitriol	Induction of human HL60 differentiation assessed as cells reducing nitro blue tetrazolium Induction of human HL60 differentiation assessed as cells reducing nitro blue tetrazolium	[PMID: 21902235]
HL-60	ED₅₀	130 nM Compound: 1a,25(OH)2D3 (125D)	Inhibition of colony formation assays on HL-60 cells Inhibition of colony formation assays on HL-60 cells	[PMID: 10893309]
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	ED₅₀	2 x 10^-9 M 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	2.7 x 10^-9 M Compound: 1	Ability to induce differentiation of human promyelocyte HL-60 cells into monocytes. Ability to induce differentiation of human promyelocyte HL-60 cells into monocytes.	[PMID: 12139448]
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 x 10^-9 M 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	ED₅₀	4.0 x 10^-9 M Compound: 1	Induced differentiation of human promyelocyte HL-60 cells into monocytes Induced differentiation of human promyelocyte HL-60 cells into monocytes	[PMID: 9804706]
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]
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]
Keratinocyte	ED₅₀	7 nM Compound: 1, calcitriol	Antiproliferative activity against murine keratinocytes Antiproliferative activity against murine keratinocytes	[PMID: 17149880]
Keratinocyte	IC₅₀	27.3 nM Compound: 1, calcitriol	Antiproliferative activity against human keratinocyte assessed as inhibition of [3H]TdR uptake Antiproliferative activity against human keratinocyte assessed as inhibition of [3H]TdR uptake	[PMID: 16630723]
Keratinocyte	IC₅₀	80 nM Compound: 1, calcitriol	Antiproliferative activity against mouse keratinocytes Antiproliferative activity against mouse keratinocytes	[PMID: 17924616]
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	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	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	EC₅₀	3.28 x 10^-9 M 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^-8 M 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	ED₅₀	380 nM Compound: 1a,25(OH)2D3 (125D)	Inhibition of colony formation assays on MCF-7 cells Inhibition of colony formation assays on MCF-7 cells	[PMID: 10893309]
MCF7	ED₅₀	61 nM Compound: 1 (1,25D3, calcitriol)	In vitro activity on human breast adenocarcinoma cell line MCF-7 proliferation In vitro activity on human breast adenocarcinoma cell line MCF-7 proliferation	[PMID: 11000014]
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	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	ED₅₀	2.7 nM Compound: 1 (1,25D3, calcitriol)	In vitro inhibition of phytohemagglutininin-induced stimulation of human peripheral blood mononuclear cells proliferation In vitro inhibition of phytohemagglutininin-induced stimulation of human peripheral blood mononuclear cells proliferation	[PMID: 11000014]
PBMC	IC₅₀	1 x 10^-9 M 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^-8 M 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]
PE	IC₅₀	100 nM Compound: calcitriol	Tested for growth inhibitory potency on murine keratinocyte cell line PE Tested for growth inhibitory potency on murine keratinocyte cell line PE	10.1016/S0960-894X(00)80115-8
RWLeu4	IC₅₀	6.0 x 10^-9 M Compound: calcitriol	Inhibitory concentration required against proliferation or inducing differentiation in the human chronic myelogenous leukemia cell line RWLeu4 Inhibitory concentration required against proliferation or inducing differentiation in the human chronic myelogenous leukemia cell line RWLeu4	10.1016/S0960-894X(00)80115-8
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]
T-cell	IC₅₀	5.0 x 10^-11 M Compound: 1	Concentration to inhibit T-cell activation in Murine MLR Concentration to inhibit T-cell activation in Murine MLR	10.1016/S0960-894X(00)80117-1
THP-1	EC₅₀	1 x 10^-8 M 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^-8 M 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]
U-937	IC₅₀	1.0 x 10^-8 M Compound: 1	Concentration to inhibit cell proliferation in U 937 cells Concentration to inhibit cell proliferation in U 937 cells	10.1016/S0960-894X(00)80117-1
U-937	IC₅₀	2.0 x 10^-9 M Compound: 1 alpha-25(OH)2D3	Compound was tested in vitro to inhibit proliferation of U 937 human histiolytic lymphoma cells Compound was tested in vitro to inhibit proliferation of U 937 human histiolytic lymphoma cells	10.1016/S0960-894X(00)80126-2

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 32222-06-3
Appearance Solid
Molecular Weight 416.64
Formel C₂₇H₄₄O₃
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
Synonyms

1,25-Dihydroxyvitamin D3
Structure Classification
- Others
Initial Source
- Endogenous metabolite
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

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

Publications (76)

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Journal Impact Factor

Nature

Peripheral immune-inducer dendritic cells drive early-life allergic inflammation. [Abstract]

2026 Apr;652(8112):1308-1317. PMID: 41741647
Cell

A microbial amino-acid-conjugated bile acid, tryptophan-cholic acid, improves glucose homeostasis via the orphan receptor MRGPRE. [Abstract]

2025 Aug 21;188(17):4530-4548.e25. PMID: 40446798
Nat Commun

Vitamin D supplementation ameliorates ductular reaction, liver inflammation and fibrosis in mice by upregulating TXNIP in ductular cells. [Abstract]

2025 May 13;16(1):4420. PMID: 40360509
Acta Pharm Sin B

A novel mesenchymal stem cell-based regimen for acute myeloid leukemia differentiation therapy. [Abstract]

2023 Jul;13(7):3027-3042. PMID: 37521858

Calcitriol purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Jul;13(7):3027-3042. [Abstract]

U937 cells were cultured alone or incubated with MSC in the presence or absence of 1,25D3 (8 nmol/L) for 48 h. The differentiation markers CD14 and CD11b and phagocytosis activity in U937 cells were measured by flow cytometry.
Nat Chem Biol

Structures of the ADGRG2-Gs complex in apo and ligand-bound forms. [Abstract]

2022 Nov;18(11):1196-1203. PMID: 35982227
Theranostics

Vitamin D binding protein (VDBP) hijacks twist1 to inhibit vasculogenic mimicry in hepatocellular carcinoma. [Abstract]

2024 Jan 1;14(1):436-450. PMID: 38164156

Calcitriol purchased from MedChemExpress. Usage Cited in: Theranostics. 2024 Jan 1;14(1):436-450. [Abstract]

Western blot analysis of VDBP protein expression level in MHCC-97H cells with Matrigel 3D culture treated with 1,25-hydroxy vitamin D3 for 48 h.
Cancer Lett

Loss of Nrf2 aggravates ionizing radiation-induced intestinal injury by activating the cGAS/STING pathway via Pirin. [Abstract]

2024 Sep 2:217218. PMID: 39233044
J Cachexia Sarcopenia Muscle

The Effects of Vitamin D on Muscle Strength Are Influenced by Testosterone Levels. [Abstract]

2025 Feb;16(1):e13733. PMID: 39957010

Calcitriol purchased from MedChemExpress. Usage Cited in: J Cachexia Sarcopenia Muscle. 2025 Feb;16(1):e13733. [Abstract]

Mice were administered i.p. with calcipotriol (60 μg/kg body weight, three times a week) or vehicle alone or in combination.
Proc Natl Acad Sci U S A

Progesterone activates GPR126 to promote breast cancer development via the Gi pathway. [Abstract]

2022 Apr 12;119(15):e2117004119. PMID: 35394864
Cell Commun Signal

BRD4/nuclear PD-L1/RelB circuit is involved in the stemness of breast cancer cells. [Abstract]

2023 Nov 3;21(1):315. PMID: 37924094
Acta Pharmacol Sin

Activating BK channels ameliorates vascular smooth muscle calcification through Akt signaling. [Abstract]

2022 Mar;43(3):624-633. PMID: 34163023
Brain Behav Immun

Alteration of intestinal mucosal immunity and metabolites in mice exposed to chronic restraint stress. [Abstract]

2025 Aug 23:130:106090. PMID: 40854440
J Transl Med

Vitamin D attenuates the progression of pulmonary fibrosis via inhibiting thymidine kinase 1/PFKFB3-driven glycolysis. [Abstract]

2026 Apr 22;24(1):571. PMID: 42021376
J Transl Med

Calcitriol increases MBNL1 expression and alleviates myotonic dystrophy phenotypes in HSALR mouse models. [Abstract]

2022 Dec 12;20(1):588. PMID: 36510245
Biomed Pharmacother

The intervention effect of zuogui pill on chronic kidney disease-mineral and bone disorder regulatory factor. [Abstract]

2018 Oct:106:54-60. PMID: 29957466
Stem Cell Res Ther

Transcriptomic and proteomic sequencing unveils the role of vitamin D and metabolic flux shifts in the induction of human hepatic organoids. [Abstract]

2024 Dec 18;15(1):478. PMID: 39696644
Cell Death Discov

Cathelicidin hCAP18/LL-37 promotes cell proliferation and suppresses antitumor activity of 1,25(OH)2D3 in hepatocellular carcinoma. [Abstract]

2022 Jan 17;8(1):27. PMID: 35039485
Ecotoxicol Environ Saf

Calcitriol alleviates noise-induced hearing loss by regulating the ATF3/DUSP1 signalling pathway. [Abstract]

2024 Aug 24:284:116906. PMID: 39182283
Antioxid Redox Signal

Role of Nox4 in High Calcium-Induced Renal Oxidative Stress Damage and Crystal Deposition. [Abstract]

2022 Jan;36(1-3):15-38. PMID: 34435888
J Bone Miner Res

Osteoblastic STAT3 is Crucial for Orthodontic Force Driving Alveolar Bone Remodeling and Tooth Movement. [Abstract]

2023 Jan;38(1):214-227. PMID: 36370067
Front Immunol

Vitamin D3 deficiency induced intestinal inflammatory response of turbot through nuclear factor-κB/inflammasome pathway, accompanied by the mutually exclusive apoptosis and autophagy. [Abstract]

2022 Sep 8:13:986593. PMID: 36159807
Biochem Pharmacol

Calcitriol protects against diabetic kidney disease by alleviating ferroptosis in renal tubular epithelial cells via JUN/ATF3 pathway. [Abstract]

2026 Sep;251(Pt 1):118089. PMID: 42167448
World J Gastroenterol

Calcitriol attenuates liver fibrosis through hepatitis C virus nonstructural protein 3-transactivated protein 1-mediated TGF β1/Smad3 and NF-κB signaling pathways. [Abstract]

2023 May 14;29(18):2798-2817. PMID: 37274069
Cells

The TLR10-Vitamin D Axis Facilitates Osteogenic Differentiation of Mesenchymal Stem Cells In Vitro. [Abstract]

2026 Apr 15;15(8):697. PMID: 42041566
CNS Neurosci Ther

Vitamin D3 Attenuates Neuropathic Pain via Suppression of Mitochondria-Associated Ferroptosis by Inhibiting PKCα/NOX4 Signaling Pathway. [Abstract]

2024 Sep;30(9):e70067. PMID: 39328008
Nutrients

1,25-Dihydroxyvitamin D3 Provides Benefits in Vitiligo Based on Modulation of CD8+ T Cell Glycolysis and Function. [Abstract]

2023 Nov 6;15(21):4697. PMID: 37960350
J Nutr Biochem

1,25(OH)2D3 protected against LPS-induced acute lung injury through modulation of gut microbiota. [Abstract]

2025 May 20:109970. PMID: 40403854
J Nutr Biochem

Effects of vitamin D status on cutaneous wound healing through modulation of EMT and ECM. [Abstract]

2024 Aug 8:109733. PMID: 39127309
J Nutr Biochem

1,25-(OH)2D3 promotes hair growth by inhibiting NLRP3/IL-1β and HIF-1α/IL-1β signaling pathways. [Abstract]

2024 Jun 25:109695. PMID: 38936782
Int J Mol Sci

Application of Novel Transcription Factor Machine Learning Model and Targeted Drug Combination Therapy Strategy in Triple Negative Breast Cancer. [Abstract]

2023 Aug 31;24(17):13497. PMID: 37686305
Eur J Pharmacol

Piezo1 activation mediates stiffness-induced aortic medial calcification: Pharmacological evidence from agonist and antagonist studies. [Abstract]

2025 Dec 13:1011:178465. PMID: 41391237
Int Immunopharmacol

VDR activation ameliorates intermittent hypoxia-related cognitive impairment by upregulating TREM2 transcription. [Abstract]

2025 Sep 23:166:115543. PMID: 40991996
mBio

The vitamin D receptor is essential for the replication of pseudorabies virus. [Abstract]

2024 Oct 30:e0213724. PMID: 39475231
Int Immunopharmacol

The VDR/FFAR2 axis mitigates sepsis-induced lung injury by suppressing macrophage lipid peroxidation. [Abstract]

2024 Oct 16;143(Pt 2):113328. PMID: 39418731
Eur J Pharmacol

A network pharmacology-based method to explore the therapeutic effect of honokiol on diabetes with comorbid depression in mice. [Abstract]

2024 May 14:176642. PMID: 38754538
Int Immunopharmacol

Vitamin D attenuates DNCB-induced atopic dermatitis-like skin lesions by inhibiting immune response and restoring skin barrier function. [Abstract]

2023 Sep:122:110558. PMID: 37393836
Int Immunopharmacol

Effects of 1,25-dihydroxyvitamin D3 in an ovalbumin-induced allergic rhinitis model. [Abstract]

2017 Jun;47:182-189. PMID: 28412624

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.
Cancers (Basel)

In Vivo and In Vitro Enhanced Tumoricidal Effects of Metformin, Active Vitamin D3, and 5-Fluorouracil Triple Therapy against Colon Cancer by Modulating the PI3K/Akt/PTEN/mTOR Network. [Abstract]

2022 Mar 17;14(6):1538. PMID: 35326689
Biochem J

Calcitriol increases frataxin levels and restores mitochondrial function in cell models of Friedreich Ataxia. [Abstract]

2021 Jan 15;478(1):1-20. PMID: 33305808
iScience

MYCT1 attenuates renal fibrosis and tubular injury in diabetic kidney disease. [Abstract]

2023 Aug 12;26(9):107609. PMID: 37664593
J Lipid Res

Acylation derivatization based LC-MS analysis of 25-hydroxyvitamin D from finger-prick blood. [Abstract]

2019 May;60(5):1058-1064. PMID: 30902903
J Photoch Photobio B

2022: 1-9.
Biochim Biophys Acta Mol Cell Res

TSLP-induced collagen type-I synthesis through STAT3 and PRMT1 is sensitive to calcitriol in human lung fibroblasts. [Abstract]

2021 Sep;1868(10):119083. PMID: 34147561
Cell Signal

Nuclear import of NLS- RARα is mediated by importin α/β. [Abstract]

2020 May;69:109567. PMID: 32036017
J Endocrinol Invest

1α,25(OH)2D3 alleviates perfluorooctane sulfonic acid-induced oxidative injury through the Nrf2-ARE pathway via VDR in Sertoli cells. [Abstract]

2025 Jul 19. PMID: 40682728
Med Oncol

Vitamin D3 and its active form calcitriol suppress erythroleukemia through upregulation of CHAC1 and downregulation of NOTCH1. [Abstract]

2025 Mar 27;42(5):138. PMID: 40146328
Biochim Biophys Acta Mol Cell Biol Lipids

Control of ALOX5 expression in monocytic cells using a synthetic riboswitch. [Abstract]

2025 Jul 25;1870(7):159671. PMID: 40716698
Environ Toxicol

Calcitriol suppresses gastric cancer progression and cisplatin resistance by inhibiting glycolysis and M2 macrophage polarization through inhibition of mTOR activation. [Abstract]

2024 Feb;39(2):830-839. PMID: 37792677
Cell Transplant

1,25-Dihydroxyvitamin D3: A Positive Factor for the Osteogenic Differentiation of hPDLSCs and for the Tissue Regenerative Activity of Cell Sheets. [Abstract]

2023 Jan-Dec:32:9636897231202541. PMID: 37798942
Environ Toxicol

Transcriptional factor BRD4 promotes the stemness of esophageal cancer by activating the nuclear PD-L1/RelB axis. [Abstract]

2024 Feb;39(2):669-679. PMID: 37615218
Curr Issues Mol Biol

Exploring the Molecular Mechanism of 1,25(OH)2D3 Reversal of Sorafenib Resistance in Hepatocellular Carcinoma Based on Network Pharmacology and Experimental Validation. [Abstract]

2025 Apr 29;47(5):319. PMID: 40699718
Curr Issues Mol Biol

1α,25-Dihydroxyvitamin D3 Improves Follicular Development and Steroid Hormone Biosynthesis by Regulating Vitamin D Receptor in the Layers Model. [Abstract]

2023 May 4;45(5):4017-4034. PMID: 37232725
Mol Biol Rep

1,25(OH)₂D₃ mitigates bronchopulmonary dysplasia via modulation of the TXNIP-NLRP3-GSDMD signaling pathway. [Abstract]

2026 May 25;53(1):820. PMID: 42183898
Toxicol In Vitro

1,25-Dihydroxyvitamin D3 attenuates TGF-β1-induced airway remodeling in asthma by inhibiting IL-33 mediated by the ERK1/2 signaling pathway. [Abstract]

2026 Jun:114:106228. PMID: 41850469
Vet Microbiol

Combining metabolic and checkpoint therapy: 1,25-dihydroxyvitamin D₃ enhances the antiviral efficacy of anti-PD-1 in BVDV infection. [Abstract]

2026 Apr:315:110950. PMID: 41707390
Exp Eye Res

Topical calcitriol application promotes diabetic corneal wound healing and reinnervation through inhibiting NLRP3 inflammasome activation. [Abstract]

2021 Aug:209:108668. PMID: 34144035
PLoS One

Unveiling the mechanism of calcitriol in treating type 2 diabetes mellitus: A combined network pharmacology and in vitro approach targeting ERS-related pathways. [Abstract]

2026 Apr 16;21(4):e0347246. PMID: 41990027
J Steroid Biochem Mol Biol

Vitamin D promotes wound healing in aged skin by modulating inflammation, angiogenesis, and EMT via the Hippo pathway. [Abstract]

2025 Jun 2:252:106799. PMID: 40466431
World J Gastrointest Oncol

Role of 1,25-dihydroxyvitamin D3 in alleviating hepatic steatosis: Targeting M1 macrophage polarization in non-alcoholic fatty liver disease. [Abstract]

2025 Mar 15;17(3):102424. PMID: 40092934
Arch Virol

Calcitriol reduces Newcastle disease virus replication by modulating galectin 3 and pro-inflammatory cytokines. [Abstract]

2024 Nov 27;169(12):254. PMID: 39601906
J Steroid Biochem Mol Biol

1,25(OH)2D3 improves diabetic wound healing by modulating inflammation and promoting angiogenesis. [Abstract]

2024 May:239:106477. PMID: 38340904
Hormones (Athens)

1,25-Dihydroxyvitamin D3 alleviates hyperandrogen-induced ferroptosis in KGN cells. [Abstract]

2023 Jun;22(2):273-280. PMID: 36884209
Placenta

Vitamin D alleviates hypoxia/reoxygenation-induced injury of human trophoblast HTR-8 cells by activating autophagy. [Abstract]

2021 Aug:111:10-18. PMID: 34126416
J Steroid Biochem Mol Biol

1β,25-Dihydroxyvitamin D3: A new vitamin D metabolite in human serum. [Abstract]

2017 Oct:173:341-348. PMID: 28193495
Nutr Cancer

VDR-Mediated Inhibition of Glycolysis and Metastasis by Calcitriol in Triple-Negative Breast Cancer. [Abstract]

2025;77(10):1200-1211. PMID: 40944623
Biomed Chromatogr

Metabolic profiles of ribociclib in rat and human liver microsomes using liquid chromatography combined with electrospray ionization high-resolution mass spectrometry. [Abstract]

2020 Mar;34(3):e4783. PMID: 31899811
STAR Protoc

Protocol for multiplexed transcription factor activity detection using optimized barcoded reporters and an automated computational pipeline. [Abstract]

2025 Sep 10;6(3):104066. PMID: 40934073
Kafkas Univ Vet Fak Derg

2025 Mar 18;31(2):171-180.
Leuk Res Rep

1,25-OH2 vitamin D3 and AKT-inhibition increase glucocorticoid induced apoptosis in a model of T-cell acute lymphoblastic leukemia (ALL). [Abstract]

2018 Mar 17:9:38-41. PMID: 29892547
bioRxiv

2026 Jun 26.
Vasc Endovasc Rev

2025 Nov 29.
Res Sq

2024 May 9.
Research Square Print

2022 May.
Oxid Med Cell Longev

1,25(OH)2D3 Mitigates Oxidative Stress-Induced Damage to Nucleus Pulposus-Derived Mesenchymal Stem Cells through PI3K/Akt Pathway. [Abstract]

2022 Mar 18;2022:1427110. PMID: 35340208
Research Square Preprint

2022 Jan.
Oncotarget

Calcitriol induces cell senescence of kidney cancer through JMJD3 mediated histone demethylation. [Abstract]

2017 Oct 26;8(59):100187-100195. PMID: 29245970

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.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4002 mL

12.0008 mL

24.0015 mL

5 mM

0.4800 mL

2.4002 mL

4.8003 mL

10 mM

0.2400 mL

1.2001 mL

2.4002 mL

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

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

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].

MedChemExpress (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].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (645 KB)
- English - EN (645 KB)
- Français - FR (645 KB)
- Deutsch - DE (645 KB)
- Norwegian - NO (645 KB)
- Español - ES (645 KB)
- Swedish - SV (645 KB)
- Italian - IT (645 KB)
- Korean - KR (645 KB)
- Portuguese - PT (645 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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	12.0008 mL	24.0015 mL	60.0038 mL
	5 mM	0.4800 mL	2.4002 mL	4.8003 mL	12.0008 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	0.7500 mL
	100 mM	0.0240 mL	0.1200 mL	0.2400 mL	0.6000 mL

Keywords

Calcitriol

76 Cited Publications

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Calcitriol

MCE Bioactive Compound Library

Natural Product Library Plus

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

Publications Citing Use of MedChemExpress (MCE) Calcitriol

Alle Endogenous Metabolite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (76)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Calcitriol

MCE Bioactive Compound Library

Natural Product Library Plus

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

Publications Citing Use of MedChemExpress (MCE) Calcitriol

Alle Endogenous Metabolite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (76)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Calcitriol Related Classifications

HY-10002 Related Classifications