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包装规格：5mg 25mg in glass bottle
产品描述：基本信息 产品编号： C10862 产品名称： Cerivastatin CAS: 145599-86-6   储存条件 粉末 -20℃ 四年     分子式： C26H34FNO5 溶于液体     分子量 459.55     化学名：  (3R,5S,6E)-7-[4-(4-Fluorophenyl)-2,6-diisopropyl-5-(methoxymethyl)-3-pyridyl]-3,5-dihydroxy-6-heptenoic acid   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℃

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