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Tacalcitol
- PRI 2191 - 1α,24-Dihydroxycholecalciferol
- Soluble in DMSO
- MF: C27H44O3
- MW: 416.64
Description
Vitamine D receptor agonist (EC50 value 7 nM for VDR) and metabolite of vitamin D3 with a higher antitumor and lower calcemic activity as well as lower toxicity than Calcitriol. Tacalcitol inhibits proliferation and induces differentiation of keratinocytes. Tacalcitol (PRI 2191) promotes normal bone formation, and is a well-known inhibitor of chemical mediated inflammatory changes including dermal cellular infiltration and epidermal hyperplasia, used to treat T cell-mediated inflammatory skin diseases such as psoriasis, prurigo and vitiligo. PRI2191 enhances the antiproliferative effect of Imatinib (Axon 1394) on HL-60 cells.
Note: Axon 2516 is the stable monohydrate formulation of Tacalcitol
More Information
| Parent CAS No. | 57333-96-7 |
|---|---|
| Chemical Name | (1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R,5R)-5-hydroxy-6-methylheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol |
| MFCD | N.A. |
| Short Description | VDR agonist |
References
- J. Wietrzyk et al. Toxicity and antineoplastic effect of (24R)-1,24-dihydroxyvitamin D3 (PRI-2191). Steroids. 2004 Sep;69(10):629-35.
- A. Opolski et al. Antiproliferative activity in vitro of side-chain analogues of calcitriol against various human normal and cancer cell lines. Anticancer Res. 1999 Nov-Dec;19(6B):5217-22.
- W. Shen et al. Novel nonsecosteroidal VDR agonists with phenyl-pyrrolyl pentane skeleton. Eur J Med Chem. 2013 Nov;69:768-78.
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