Catalog No.S1466 Synonyms: RO215535, Topitriol
Molecular Weight(MW): 416.64
Calcitriol is a nonselective vitamin D receptor activator/agonist(VDRA), exhibiting a 10-fold higher vitamin D receptor (VDR) binding affinity(IC50=0.4 nM) than the selective VDRA paricalcitol.
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|Description||Calcitriol is a nonselective vitamin D receptor activator/agonist(VDRA), exhibiting a 10-fold higher vitamin D receptor (VDR) binding affinity(IC50=0.4 nM) than the selective VDRA paricalcitol.|
Calcitriol is a potent inhibitor of PHA-induced lymphocyte proliferation, achieving 70% inhibition of tritiated thymidine incorporation after 72 h in culture. Calcitriol suppresses interleukin-2 (IL-2) production by PHA-stimulated peripheral blood mononuclear cells in a concentration-dependent fashion.  Calcitriol increases the concentration of intracellular calcium ([Ca2+]i) within 5 s by mobilizing calcium from the endoplasmic reticulum and the formation of inositol 1,4, 5-trisphosphate and diacylglycerol.  Calcitriol can inhibit the proliferation and promote the differentiation of human prostate adenocarcinoma cells. Calcitriol causes a selective decrease in the secreted levels of type IV collagenases (MMP-2 and MMP-9).  Calcitriol has antiproliferative activity in squamous cell carcinoma and prostatic adenocarcinoma and enhances the antitumor activity of platinum-based agents. Calcitriol prior to paclitaxel significantly reduces clonogenic survival compared with either agent alone in the murine squamous cell carcinoma and PC-3 cells.  Calcitriol is a potent anti-proliferative agent in a wide variety of malignant cell types. Calcitriol effects are associated with an increase in G0/G1 arrest, induction of apoptosis and differentiation, modulation of expression of growth factor receptors. Calcitriol potentiates the antitumor effects of many cytotoxic agents and inhibits motility and invasiveness of tumor cells and formation of new blood vessels. 
-  Rigby WF, et al. J Clin Invest, 1984, 74(4), 1451-1455.
-  Le Mellay V, et al. J Biol Chem, 1997, 272(18), 11902-11907.
-  Schwartz GG, et al. Cancer Epidemiol Biomarkers Prev, 1997, 6(9), 727-732.
|In vitro||DMSO||83 mg/mL (199.21 mM)|
|Ethanol||83 mg/mL (199.21 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02962102||Not yet recruiting||Critically Ill|Acute Kidney Injury||David Leaf|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|Brigham and Womens Hospital||February 2017||Phase 2|
|NCT01561222||Not yet recruiting||Chronic Kidney Disease Stage 1|Chronic Kidney Disease Stage 2||Taixing Peoples Hospital||July 2015||Phase 4|
|NCT02410005||Active, not recruiting||Diabetic Nephropathies||Weill Cornell Medical College in Qatar|Weill Medical College of Cornell University|Hamad Medical Corporation||October 2014||Phase 2|Phase 3|
|NCT02224144||Active, not recruiting||End Stage Renal Disease|Kidney Transplantation|Bone Loss|Fractures|Vascular Calcifications||Columbia University|Satellite Healthcare||August 2014||Phase 2|
|NCT02061384||Active, not recruiting||Male Infertility|Klinefelters Syndrome|Y-chromosome Microdeletions||University of Washington||August 2014||Phase 2|
|NCT02186665||Completed||Plaque Psoriasis||Galderma||July 2014||Phase 4|
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