Vitamin D3

Catalog No.S4063

Vitamin D3 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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Vitamin D3  Chemical Structure

Vitamin D3 Chemical Structure
Molecular Weight: 384.64

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Product Information

  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description Vitamin D3 is a form of vitamin D, binds and activates a H305F/H397Y mutant vitamin D receptor (VDR) with EC50 of 300 nM.
Targets H305F/H397Y mutant vitamin D receptor [1]
IC50 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(Only for Reference)

Kinase Assay: [1]

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 Assay: [3]

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 Study: [2]

Animal Models CYP27B1 (−/−) mice
Formulation solidified agar
Dosages ~10.0 mg/kg
Administration Oral
Solubility 30% PEG400/0.5% Tween80/5% propylene glycol, 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.
Body Surface Area (m2)
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Ousley AM, et al. J Steroid Biochem Mol Biol, 2011, 125(3-5), 202-210.

[2] Hector D, et al. Archives of Biochemistry and Biophysics, 2011, 505(2), 226–230

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Clinical Trial Information( data from, updated on 2015-01-31)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02276755 Not yet recruiting Latent Tuberculosis Harvard School of Public Health September 2015 Phase 3
NCT01728987 Not yet recruiting Obesity University of Tromso August 2015 Phase 2
NCT02305927 Not yet recruiting HIV Wafaie Fawzi|Management and Development for Health (MDH)|  ...more Wafaie Fawzi|Management and Development for Health (MDH)|Harvard School of Public Health April 2015 Phase 3
NCT02186275 Not yet recruiting Crohns Disease St. Justines Hospital|Canadian Institutes of Health Resea  ...more St. Justines Hospital|Canadian Institutes of Health Research (CIHR) February 2015 Phase 3
NCT01858051 Not yet recruiting Hypovitaminosis D Massachusetts General Hospital|BioTech Pharmacal January 2015 Phase 3

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Chemical Information

Molecular Weight (MW) 384.64


CAS No. 67-97-0
Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms Cholecalciferol
Solubility (25°C) * In vitro DMSO 77 mg/mL (200.18 mM)
Water <1 mg/mL (<1 mM)
Ethanol 77 mg/mL (200.18 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name Cyclohexanol, 3-[(2E)-2-[(1R,3aS,7aR)-1-[(1R)-1,5-dimethylhexyl]octahydro-7a-methyl-4H-inden-4-ylidene]ethylidene]-4-methylene-, (1S,3Z)-

Research Area

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