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产品描述:基本信息 产品编号: I10433  产品名称: Inecalcitol CAS: 163217-09-2   储存条件 粉末 -20℃ 四年     分子式: C26H40O3 溶于液体 -80℃ 6个月 分子量 400.60 -20℃ 1个月 化学名:  19-Nor-14-epi-23-yne-1,25 dihydroxyvitamin D3 Solubility (25°C):   体外:   DMSO   Water   Ethanol   体内(现配现用):   <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 生物活性 产品描述 一种独特的维生素 D3 类似物,是一种具有口服活性维生素 D 受体 (VDR) 激动剂, Kd 为 0.53nM。Inecalcitol 可诱导细胞凋亡 (apoptosis),并具有有效的抗癌活性。 靶点 Kd: 0.53nM (vitamin D receptor (VDR)) 体外研究 Inecalcitol (0.1-10nM; 48 hours) treatment of LNCaP cells results in decreased expression of both protein and mRNA of Pim-1 in a dose-dependent manner. Inecalcitol (0.1-10nM; 48 hours) also decreases ETV1 expression levels in a dose-dependent manner. Inecalcitol (10-14 days) inhibits the growth of LNCaP and HL-60 cells with ED50 values of 4.0nM and 0.28nM, respectively. Western Blot Analysis Cell Line: LNCaP cells Concentration: 0.1nM, 1nM, 10nM Incubation Time: 48 hours Result: Resulted in decreased expression of both protein and mRNA of Pim-1 in a dose-dependent manner. 体内研究 Inecalcitol (1.3 mg/kg; i.p.; 3 times per week; for 42 days) inhibits androgen-responsive prostate cancer growth in vivo.Pharmacokinetic studies show that plasma half-life of Inecalcitol (C57Bl/6J mice; 1.3 mg/kg; i.p.) is 18.3 minutes in mice Animal Model: Male BNX nu/nu mice (8 weeks of age) injected with LNCaP cells Dosage: 1.3 mg/kg Administration: i.p.; 3 times per week; for 42 days Result: Inhibited androgen-responsive prostate cancer growth in vivo.
保存条件:-20℃ 充氮保存