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Tacalcitol
- PRI 2191 - 1α,24-Dihydroxycholecalciferol
Axon 2516
CAS:
57333-96-7
Purity:
98%
- Soluble in DMSO
- MF: C27H44O3
- MW: 416.64
Description
Tacalcitol (PRI-2191) is a vitamin D receptor (VDR) agonist and active vitamin D3 analog. It activates VDR-dependent transcriptional programs linked to differentiation, calcium regulation and antiproliferative signaling.
VDR signaling regulates mineral homeostasis, immune modulation, keratinocyte biology and tumor-cell differentiation. Tacalcitol is useful for studying vitamin D receptor pharmacology and comparing calcemic versus antiproliferative effects of vitamin D analogs.
Key Features
- Vitamin D receptor agonist
- Reported EC50: 7 nM for VDR activation
- Vitamin D3 metabolite analog with antiproliferative activity
- Reported lower calcemic and toxicity profile than calcitriol in comparative studies
Applications
- VDR nuclear receptor pharmacology
- Keratinocyte and dermatology research
- Cancer cell differentiation and proliferation studies
- Calcium and vitamin D signaling assays
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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