cholecalciferol (Vitamin D3)

For research use only.

Catalog No.S4063 Synonyms: Cholecalciferol, Colecalciferol

1 publication

cholecalciferol (Vitamin D3)  Chemical Structure

CAS No. 67-97-0

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.

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10mM (1mL in DMSO) EUR 127 In stock
EUR 95 In stock
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Selleck's cholecalciferol (Vitamin D3) has been cited by 1 publication

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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]


Kinase Assay:[1]
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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 the mammalian 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 is calculated by dividing the value at maximal activation by the value at the no ligand data point.
Cell Research:[3]
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  • 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.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: CYP27B1 (−/−) mice
  • Dosages: ~10.0 mg/kg
  • Administration: Oral
    (Only for Reference)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 384.64


CAS No. 67-97-0
Storage powder
in solvent
Synonyms Cholecalciferol, Colecalciferol

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04641663 Not yet recruiting Dietary Supplement: Multi-target Dietary Supplement (MTDS) Aging|Age-related Cognitive Decline Douglas Boreham|McMaster University|Northern Ontario School of Medicine January 4 2021 Not Applicable
NCT04579315 Not yet recruiting Other: Intervention group; NNRD group Chronic Kidney Disease(CKD)|Hyperphosphatemia|Blood Pressure Bo Feldt-Rasmussen|Rigshospitalet Denmark November 3 2020 Not Applicable
NCT04315818 Not yet recruiting -- Rheumatoid Arthritis Assiut University September 2020 --
NCT04428359 Completed Drug: Measles-Mumps-Rubella Vaccine|Drug: Vit D Verruca Viral B.P. Koirala Institute of Health Sciences|Nepal Health Research Council June 1 2020 Not Applicable
NCT04007614 Not yet recruiting Other: Questionnaire Contraception|Macro-progestins Assistance Publique - Hôpitaux de Paris April 2020 --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID