来沙骨化醇 T15745

Product Introduction
Bioactivity


英文名: Lexacalcitol

描述: Lexacalcitol is over 100 times more active than 1alpha,25-dihydroxyvitamin D3 [1alpha,25-(OH)2D3], as judged by in vitro antiproliferative and cell differentiating assays.

体外活性: KH1060 was not an effective competitor of C24 oxidation of 1alpha,25-(OH)2D3. KH 1060 inhibited PBMC proliferation and decreased TNF-alpha levels in IBD patients and this effect was synergistic with anti-TNF-alpha. KH1060 metabolism could be blocked by the cytochrome P450 inhibitor, ketoconazole. Certain hydroxylated metabolites of KH1060 retained significant biological activity in vitamin D-dependent reporter gene systems. VDR protein levels were significantly increased by PBMC treatment with KH 1060 or anti-TNF-alpha or their combination in ulcerative colitis (UC) patients, and decreased in Crohn's disease (CD) patients, treating the cells with KH 1060. A synergistic inhibition was registered combining KH 1060 and anti-TNF, at well-defined concentrations. 0.1 nM KH 1060 produced a significant decrease in TNF-alpha levels, determined by ELISA, although less remarkable than in the presence of anti-TNF.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: KH 1060 | KH-1060 | Lexacalcitol

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途