cholecalciferol (Vitamin D3)
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||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.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03402698||Completed||Vitamin D Deficiency||Children''s Memorial Health Institute Poland|Nutropharma Ltd.||January 9 2018||Not Applicable|
|NCT02839239||Completed||Infant Colic||Biocare Copenhagen A/S|Lviv National Medical University||December 9 2016||Not Applicable|
|NCT01120600||Completed||Osteoporosis||Merck Sharp & Dohme Corp.||June 9 2010||Phase 3|
|NCT03588884||Recruiting||Secondary Hyperparathyroidism Due to Renal Causes|Vitamin D Deficiency|CKD Stage 3|CKD Stage 4||OPKO Ireland Global Holdings Ltd.||June 8 2018||Phase 4|
|NCT03070483||Recruiting||Hypertension|Vitamin D Deficiency||Loyola University||January 8 2018||Phase 2|
|NCT00887432||Recruiting||Prostate Adenocarcinoma||Roswell Park Cancer Institute|National Cancer Institute (NCI)||April 8 2009||Not Applicable|
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