生物活性 | |||
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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 | |||
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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 |
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