cholecalciferol (Vitamin D3)

Catalog No.S4063 Synonyms: Cholecalciferol, Colecalciferol

For research use only.

Cholecalciferol (Vitamin D3, Cholecalciferol, Colecalciferol) is a form of vitamin D, binds and activates a H305F/H397Y mutant vitamin D receptor (VDR) with EC50 of 300 nM.

cholecalciferol (Vitamin D3)  Chemical Structure

CAS No. 67-97-0

Selleck's cholecalciferol (Vitamin D3) has been cited by 2 Publications

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Biological Activity

Description Cholecalciferol (Vitamin D3, Cholecalciferol, Colecalciferol) is a form of vitamin D, binds and activates a H305F/H397Y mutant vitamin D receptor (VDR) with EC50 of 300 nM.
H305F/H397Y mutant vitamin D receptor [1]
300 nM(Kd)
In vitro

Vitamin D3 is a fat-soluble vitamin that helps your body absorb calcium and phosphorus. Vitamin D3, a precursor in the 1α,25- dihydroxyvitamin D3 biosynthetic pathway, which does not activate wild-type hVDR. It binds and activates H305F/H397Y variant hVDR ,with 70 fold activation in compare to wide-type hVDR. [1] Epidemiological studies and work on experimental animals strongly suggest a protective effect of cholecalciferol vitamin D3 (1,25(OH)2D3) against colon cancer and several other cancers. [2]

In vivo

With UV-radiation, vitamin D3 is synthesized in the skin from the precursors 7-dehydro-cholesterole and provitamin D3. In the liver, vitamin D3 is transformed to 25-hydroxyvitamin D3. Six cytochrome P450 hydroxylases can exhibit this 25-hydroxylation, with the main enzyme being CYP27A1 (25-hydroxylase). The subsequent step is a 1alpha-hydroxylation by CYP27B1 (1-hydroxylase), which produces the most active form of vitamin D3, 1,25-dihydroxyvitamin-D3. This metabolite is inactivated by a 24-hydroxylation by CYP24 (24-hydro-xylase). Vitamin D3 is used for prevention of mortality in adults. However, Vitamin D3 combines with calcium increased the risk of nephrolithiasis. [3]

Protocol (from reference)

Kinase Assay:


  • Luciferase and β-galactosidase activity assay:

    HEK293T cells are transfected with pCMXwild-type hVDR, pCMXH305F, pCMXH305Y, and pCMXH305F/H397Y. These plasmids contain the Gal4DBD (GBD) fused to the corresponding VDR ligand binding domain (GBD:LBD fusion under the control of a cytomegalovirus (CMV) promoter). The reporter plasmids are p17*4TATAluc, containing the Renilla luciferase gene under the control of four Gal4 response elements located upstream from a minimal thymidine kinase promoter, and pCMXβgal, a plasmid containing the β-galactosidase gene under the control of themammalian CMV promoter. The ligands are added to the wells at various concentrations ((0.01 μM– 100 μM) LCA and (0.01 μM–32 μM) cholecalciferol). Cells are harvested and analyzed for luciferase and β-galactosidase activity. Fold activation iscalculated by dividing the value at maximal activation by the value at the no ligand data point.

Cell Research:


  • Cell lines: MCF-7
  • Concentrations: ~ 100 nM
  • Incubation Time: ~ 96 h
  • Method:

    Vitamin D receptor (VDR)- positive MCF-7 cells in culture are stimulated with the vitamin D metabolites vitamin D3, 25-hydroxyvitamin D3 and 1,25-dihydroxyvitamin D3 for 24, 48, 72 and 96 hours in physiological andsupraphysiological concentrations. The expressions of 25-hydroxylase, 1-hydroxylase and 24-hydroxylase and their changes after stimulation are assessed by real-time PCR.

Animal Research:


  • Animal Models: CYP27B1 (−/−) mice
  • Dosages: up to 0.625 mg/kg
  • Administration: Oral

Solubility (25°C)

In vitro

DMSO 77 mg/mL
(200.18 mM)
Water Insoluble
Ethanol '77 mg/mL

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 384.64


CAS No. 67-97-0
Storage 3 years -20°C powder
2 years -80°C in solvent

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04641663 Enrolling by invitation Dietary Supplement: Multi-target Dietary Supplement (MTDS) Aging|Age-related Cognitive Decline Douglas Boreham|McMaster University|Northern Ontario School of Medicine September 3 2021 Not Applicable
NCT04010578 Not yet recruiting Dietary Supplement: MK-7 and vitamin D3|Other: Placebo Coronary Artery Disease|Carotid Artery Disease Academisch Ziekenhuis Maastricht|Horizon 2020 - European Commission August 1 2021 Not Applicable
NCT04981743 Recruiting Dietary Supplement: Nigella Sativa capsule twice daily Covid19 Ain Shams University July 21 2021 Not Applicable
NCT04775381 Recruiting Drug: Vitamin D Hypocalcemia Centre Hospitalier René Dubos June 30 2021 Phase 3
NCT04880824 Recruiting Behavioral: Prehabilitation- new form of care Frailty Syndrome Charite University Berlin Germany May 19 2021 --
NCT04315818 Not yet recruiting -- Rheumatoid Arthritis Assiut University March 2021 --

(data from, updated on 2022-01-17)

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