Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Cerivastatin is a highly potent, well-tolerated, and orally active HMG-CoA reductase inhibitor (Ki: 1.3 nM/L). Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition with anti-cancer effect. Cerivastatin reduces low-density lipoprotein cholesterol levels.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 15,000 | 8-10周 | ||
50 mg | ¥ 19,800 | 8-10周 | ||
100 mg | ¥ 25,500 | 8-10周 |
产品描述 | Cerivastatin is a highly potent, well-tolerated, and orally active HMG-CoA reductase inhibitor (Ki: 1.3 nM/L). Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition with anti-cancer effect. Cerivastatin reduces low-density lipoprotein cholesterol levels. |
靶点活性 | HMG-CoA reductase:1.3 nM/L (Ki) |
体外活性 | Cerivastatin (5-50 ng/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 25 ng/mL). Cerivastatin (10-25 ng/mL; 18 hours) inhibits invasion of MDA-MB-231 cells through Matrigel. Cerivastatin (25 ng/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. Cerivastatin (25 ng/mL; 18-36 hours; MDA-MB-231 cells) treatment induces an arrest of the cell cycle in the G 1/S phase after 36 h treatment. Cerivastatin (25 ng/mL; 18-36 hours) delocalizes RhoA and Ras from the membrane to the cytosol and induces morphological changes. Cerivastatin (25 ng/mL; 18 hours; MDA-MB-231 cells) treatment induces a marked increase in the level of p21Waf1/Cip1. Cerivastatin (25 ng/mL; 12 hours; MDA-MB-231 cells) treatment increases the p21 transcript in MDA-MB-231 cells. This arrest is not observed for a shorter incubation time (18 h) [1]. |
体内活性 | Cerivastatin is highly bound to plasma proteins (99.5%), with an elimination half-life of 2-4 hours. Cerivastatin is well absorbed, reaching maximal plasma levels in 1-3 hours following oral dosing. Cerivastatin is metabolized predominantly in the liver to three polar metabolites. 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 [2]. |
分子量 | 459.55 |
分子式 | C26H34FNO5 |
CAS No. | 145599-86-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Cerivastatin 145599-86-6 Others Inhibitor inhibitor inhibit