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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In DMSO USD 130 In stock
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Vitamin D3  Chemical Structure

Vitamin D3 Chemical Structure
Molecular Weight: 384.64

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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.
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.


[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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Chemical Information

Molecular Weight (MW) 384.64


CAS No. 67-97-0
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms Cholecalciferol
Solubility (25°C) * In vitro DMSO 77 mg/mL (200 mM)
Water <1 mg/mL (<1 mM)
Ethanol 77 mg/mL (200 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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