西立伐他汀钠  ≥98%

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包装规格:5mg 10mg 25mg in glass bottle
产品描述:基本信息 产品编号: C10861 产品名称: Cerivastatin sodium CAS: 143201-11-0   储存条件 粉末 -20℃ 四年     分子式: C26H33FNNaO5 溶于液体 -80℃ 六个月 分子量 481.53 -20℃ 一个月 化学名:  sodium,(E,3R,5S)-7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-di(propan-2-yl)pyridin-3-yl]-3,5-dihydroxyhept-6-enoate Solubility (25°C):   体外:   DMSO   Ethanol   Water 100mg/mL(207.67mM;ultrasonic and warming and heat to 60°C) 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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.0767mL 10.3836mL 20.7671mL 5mM 0.4153mL 2.0767mL 4.1534mL 10mM 0.2077mL 1.0384mL 2.0767mL   生物活性 产品描述 一种合成的降脂剂,是一种高效,耐受性好,口服活性的HMG-CoA还原酶抑制剂,Ki为1.3nM/L。 靶点 Ki: 1.3nM/L (HMG-CoA reductase) 体外研究 Cerivastatin (5-50ng/mL; 3 days; MDA-MB-231 cells) treatment induces a dose-dependent decrease in cell proliferation of MDA-MB-231 cells (up to 40% inhibition at 25ng/mL). Cerivastatin (25ng/mL; 18-36 hours; MDA-MB-231 cells) treatment induces an arrest of the cell cycle in G 1/S phase after 36 h treatment. This arrest is not observed for a shorter incubation time (18 h). Cerivastatin (25ng/mL; 18 hours; MDA-MB-231 cells) treatment induces a marked increase in the level of p21Waf1/Cip1. Cerivastatin (25ng/mL; 12 hours; MDA-MB-231 cells) treatment increases the p21 transcript in MDA-MB-231 cells. Cerivastatin (10-25ng/mL; 18 hours) inhibits invasion of MDA-MB-231 cells through Matrigel Cerivastatin (25ng/mL; 18-36 hours) delocalizes RhoA and Ras from the membrane to the cytosol and induces morphological changes. Cerivastatin (25ng/mL; 4-36 hours) induces inactivation of NFκB, in a RhoA inhibition-dependent manner, resulting in a decrease in urokinase and metalloproteinase-9 expression, and concomitantly increases IκB Cell Proliferation Assay   Cell Line: MDA-MB-231 cells Concentration: 5ng/mL, 10ng/mL, 25ng/mL, 50ng/mL Incubation Time: 3 days Result: Induced a dose-dependent decrease in cell proliferation of MDA-MB-231 cells.   Cell Cycle Analysis   Cell Line: MDA-MB-231 cells Concentration: 25ng/mL Incubation Time: 18 hours, 36 hours Result: Induced a cell cycle block in G 1/S phase.   Western Blot Analysis   Cell Line: MDA-MB-231 cells Concentration: 25ng/mL Incubation Time: 18 hours Result: Induced a marked increase in the level of p21Waf1/Cip1.   RT-PCR   Cell Line: MDA-MB-231 cells Concentration: 25ng/mL Incubation Time: 12 hours Result: Increased p21Waf1/Cip1 mRNA levels. 体内研究 Cerivastatin is well absorbed, reaching maximal plasma levels in 1-3 hours following oral dosing. In the circulation, Cerivastatin is highly bound to plasma proteins (99.5%), with an elimination half-life of 2-4 hours. Cerivastatin is metabolized predominantly in the liver to three polar metabolites. Two of these metabolites are active, but to a lesser extent compared to parent drug, and the third metabolite is inactive. Plasma concentrations of all metabolites are substantially lower than those of the parent drug. Elimination of metabolites is via the urine (20-25%) and feces (66-73%), while essentially no parent compound is excreted
保存条件:-20℃