Calcitriol | CAS:32222-06-3

Chemscene社は、高品質な低分子化合物を提供しているメーカーです。
Chemscene社のCalcitriol(CAS:32222-06-3)をご紹介します。

※本製品は研究用です。研究用以外には使用できません。

Name:Calcitriol; 1,25-Dihydroxyvitamin D3
Cat. No. :CS-0388
CAS No. :32222-06-3
Formula:C27H44O3
M. Wt. : 416.64
Solubility:DMSO

Calcitriol is the most active metabolite of vitamin D. Many of the effects of Calcitriol are mediated by its interaction with the vitamin D receptor (VDR).IC50 & Target: Vitamin D receptor (VDR)[1]In Vitro: In parathyroid cells, Calcitriol acts through the vitamin D receptor (VDR) to inhibit PTH mRNA expression. In normal dog parathyroid glands, culture with Calcitriol (10-10 to 10-7 M) for 24 h produces a dose-dependent inhibitory effect on the progression of cells into the cell cycle and into apoptosis. Even a low Calcitriol concentration (10-11 and 10-10 M) reduces the progression to the S phase and to apoptosis. As the Calcitriol concentration is increased from 10-9 to 10-8M, a further suppression of cells entering the cell cycle and apoptosis is observed. Moreover, a significant correlation (r=0.95, P[1]. Calcitriol binds to the vitamin D receptor (VDR), a member of the steroid receptor superfamily to regulate gene expression in all tissues of the body. In addition to its actions on calcium and bone homeostasis, Calcitriol also exhibits anti-proliferative and pro-differentiation activities indicating its potential use in the prevention and treatment of multiple cancers, including breast cancer (BCa). Calcitriol inhibits the growth of both estrogen receptor-positive (ER+) and ER-negative human BCa cell lines by regulating many molecular pathways. Calcitriol reduces the invasive and metastatic potential of several BCa cells. Calcitriol evokes significant anti-inflammatory actions in several cancer cells including BCa cells. Calcitriol also mediates actions that would be especially effective in ER+ BCa[2].In Vivo: Combinations of Calcitriol with aromatase inhibitors or the analog EB1089 with all-trans-retinoic acid exhibit enhanced inhibition of the growth of MCF-7 xenografts. Calcitriol also exhibits potent anti-angiogenic activity that could contribute to its actions to inhibit invasion and metastasis[2]. Body-weight of HFD-fed animals become different as it gradually but noticeably decreased in Calcitriol group (150 IU/kg/day, p.o.) compared with controls after 12 weeks of treatment (11.4% versus 30.2%, p[3].

Krishnan AV, et al. Equivalent anticancer activities of dietary vitamin D and calcitriol in an animal model of breast cancer: Importance of mammary CYP27B1 for treatment and prevention. J Steroid Biochem Mol Biol. 2013 Jul;136:289-95. Canalejo A, et al. The in vitro effect of calcitriol on parathyroid cell proliferation and apoptosis. J Am Soc Nephrol. 2000 Oct;11(10):1865-72. Alkharfy KM, Al-Daghri NM, Yakout SM, Ahmed M.Calcitriol Attenuates Weight-Related Systemic Inflammation and Ultrastructural Changes of the Liver in a Rodent Model.Basic Clin Pharmacol Toxicol. 2012 Aug 21. Chen B, et al. Effects of 1,25-dihydroxyvitamin D3 in an ovalbumin-induced allergic rhinitis model. Int Immunopharmacol. 2017 Jun;47:182-189.