Calcifediol monohydrate

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Chemical Structure| 63283-36-3 同义名 : 25-hydroxy Vitamin D3 monohydrate
CAS号 : 63283-36-3
货号 : A443037
分子式 : C27H46O3
纯度 : 99%+
分子量 : 418.652
MDL号 : MFCD08600001
存储条件:

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(119.43 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate), a major circulating metabolite of vitamin D3, is a potent VDR inhibitor. Calcifediol in either liposomes or ethanolic solution has no effect on the release of the proinflammatory cytokine KC from Pseudomonas-infected murine epithelial cells. Treatment of infected, human bronchial 16-HBE cells with Calcifediol liposomes results in a significant reduction in bacterial survival[2]. The safer pharmacokinetic of the recent modified-release (MR) formulation of calcifediol was effective in replenishing 25(OH)D levels with minimal impact on vitamin D catabolism and fibroblast-growth factor-23 (FGF-23) activation[3]. The inhibitory effects induced by VDR overexpression could be reversed by the VDR inhibitor, calcifediol[4]. Extended-release calcifediol (ERC) is an orally administered prohormone of active vitamin D (1,25-dihydroxyvitamin D [1,25D]) designed to safely and sufficiently increase serum total 25-hydroxyvitamin D (25D) to reduce elevated parathyroid hormone (PTH) in patients with non-dialysis-chronic kidney disease (ND-CKD)[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.39mL

0.48mL

0.24mL

11.94mL

2.39mL

1.19mL

23.89mL

4.78mL

2.39mL

参考文献

[1]Castoldi A, Herr C, et al. Calcifediol-loaded liposomes for local treatment of pulmonary bacterial infections. Eur J Pharm Biopharm. 2017 Sep;118:62-67.

[2]Castoldi A, Herr C, Niederstraßer J, Labouta HI, Melero A, Gordon S, Schneider-Daum N, Bals R, Lehr CM. Calcifediol-loaded liposomes for local treatment of pulmonary bacterial infections. Eur J Pharm Biopharm. 2017 Sep;118:62-67

[3]Galassi A, Bellasi A, Ciceri P, Pivari F, Conte F, Cozzolino M. Calcifediol to treat secondary hyperparathyroidism in patients with chronic kidney disease. Expert Rev Clin Pharmacol. 2017 Oct;10(10):1073-1084

[4]Zheng W, Duan B, Zhang Q, Ouyang L, Peng W, Qian F, Wang Y, Huang S. Vitamin D-induced vitamin D receptor expression induces tamoxifen sensitivity in MCF-7 stem cells via suppression of Wnt/β-catenin signaling. Biosci Rep. 2018 Dec 7;38(6):BSR20180595

[5]Cozzolino M, Ketteler M. Evaluating extended-release calcifediol as a treatment option for chronic kidney disease-mineral and bone disorder (CKD-MBD). Expert Opin Pharmacother. 2019 Dec;20(17):2081-2093