Catalog No.S4063 Synonyms: Cholecalciferol
Molecular Weight(MW): 384.64
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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|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.|
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.  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. 
|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. |
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.
|In vitro||DMSO||77 mg/mL (200.18 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.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02563015||Recruiting||Healthy|Vitamin D Deficiency||McGill University||March 7, 2016||--|
|NCT03037593||Not yet recruiting||Gestational Diabetes||University of Minnesota - Clinical and Translational Science Institute||June 2017||Phase 1|Phase 2|
|NCT02856503||Not yet recruiting||Breast Cancer|Invasive Breast Carcinoma|Ductal Carcinoma In-situ||Eli Avisar|University of Miami||April 2017||Phase 1|Phase 2|
|NCT01968590||Not yet recruiting||Neurofibromatosis Type 1 (NF1)||University of Utah|U.S. Army Medical Research and Materiel Command|Universitätsklinikum Hamburg-Eppendorf|University of British Columbia|Childrens Hospital Medical Center, Cincinnati||March 2017||Phase 2|
|NCT02996721||Not yet recruiting||Death|Myocardial Infarction|Cerebral Vascular Accident|Heart Failure Hospitalization||Intermountain Health Care, Inc.||January 2017||Phase 4|
|NCT02786498||Not yet recruiting||Fracture||University of Maryland|McMaster University||January 2017||Phase 2|
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