Eldecalcitol

Eldecalcitol is a derivative of the vitamin D₃ receptor agonist and vitamin D₃ active metabolite calcitriol (Item No. 71820).^1,2 It induces calcium release in an in vitro bone mobilization assay using isolated mouse calvaria when used at a concentration of 10 nM.¹ 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-1β in primary human gingival fibroblasts.³ 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.⁴ 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.² Formulations containing eldecalcitol have been used in the treatment of osteoporosis.

WARNING This product is not for human or veterinary use.

1. Okano, T., Tsugawa, N., Masuda, S., et al. Regulatory activities of 2β-(3-hydroxypropoxy)-1α, 25-dihydroxyvitamin D₃, a novel synthetic vitamin D₃ derivative, on calcium metabolism. Biochem. Biophys. Res. Commun. 163(3), 1444-1449 (1989).

2. Smith, S.Y., Doyle, N., Boyer, M., et al. Eldecalcitol, a vitamin D analog, reduces bone turnover and increases trabecular and cortical bone mass, density, and strength in ovariectomized cynomolgus monkeys. Bone 57(1), 116-122 (2013).

3. Huang, C., Zhang , C., Yang, P., et al. Eldecalcitol inhibits LPS-induced NLRP3 inflammasome-dependent pyroptosis in human gingival fibroblasts by activating the Nrf2/HO-1 signaling pathway. Drug Des. Devel. Ther. 14, 4901-4913 (2020).

4. Lu, Y., Kou, Y., Gao, Y., et al. Eldecalcitol inhibits the progression of oral cancer by suppressing the expression of GPx-1. Oral Dis. 29(2), 615-627 (2023).