Eldecalcitol

Eldecalcitol is a derivative of the vitamin D3 receptor agonist and vitamin D3 active metabolite calcitriol (Cay-71820). It induces calcium release in an in vitro bone mobilization assay using isolated mouse calvaria when used at a concentration of 10 nM. Eldecalcitol (50 nM) reduces LPS-induced pyroptosis and increases in hydrogen peroxide and protein levels of the NOD-like receptor protein 3 (NLRP3) inflammasome, caspase-1, and IL-1beta in primary human gingival fibroblasts. Eldecalcitol (0.4 nM) induces apoptosis and cell cycle arrest at the G0/G1 phase in, and inhibits migration of, SCC-15 and CAL 27 squamous cell carcinoma cells and decreases tumor volume in an SCC-15 mouse xenograft model when administered at a dose of 0.5 µg/kg twice per week. Eldecalcitol (0.3 µg/kg) decreases serum parathyroid hormone (PTH) levels and increases serum calcium levels, bone mineral density, and bone strength in a cynomolgus monkey model of osteoporosis induced by ovariectomy. Formulations containing eldecalcitol have been used in the treatment of osteoporosis.Formal Name: 2-(3-hydroxypropoxy)-4-methylene-5-[(2E)-2-[(1R,3aS,7aR)-octahydro-1-[(1R)-5-hydroxy-1,5-dimethylhexyl]-7a-methyl-4H-inden-4-ylidene]ethylidene]-1,3-cyclohexanediol. CAS Number: 104121-92-8. Synonyms: ED-71, 1alpha,25-dihydroxy-2beta-(3-hydroxypropoxy) Vitamin D3. Molecular Formula: C30H50O5. Formula Weight: 490.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Slightly soluble, Methanol: Slightly soluble, Water: Slightly soluble. SMILES: C=C1[C@@H](O)[C@H](OCCCO)[C@H](O)C/C1=C/C=C2CCC[C@@]3(C)[C@@]\2([H])CC[C@]3([H])[C@H](C)CCCC(C)(O)C. InChi Code: InChI=1S/C30H50O5/c1-20(9-6-15-29(3,4)34)24-13-14-25-22(10-7-16-30(24,25)5)11-12-23-19-26(32)28(27(33)21(23)2)35-18-8-17-31/h11-12,20,24-28,31-34H,2,6-10,13-19H2,1,3-5H3/b22-11+,23-12-/t20-,24-,25+,26-,27-,28-,30-/m1/s1. InChi Key: FZEXGDDBXLBRTD-AYIMTCTASA-N.