西立伐他汀钠

生物活性靶点体外研究体内研究西立伐他汀钠试剂级价格

西立伐他汀钠

CAS号:143201-11-0
英文名:Cerivastatin sodium
中文名:西立伐他汀钠
CBNumber:CB5115264
分子式:C26H35FNNaO5
分子量:483.56
MOL File:143201-11-0.mol

西立伐他汀钠化学性质

熔点 :197-199°C
比旋光度 :D20 +24.1° (c = 1 in ethanol)
储存条件 :Hygroscopic, Store under Inert atmosphere -20°C Freezer
溶解度 :H2O: ≥5mg/mL
形态 :powder
颜色 :white to tan
旋光性 (optical activity) :[α]/D +18 to +26° in ethanol
稳定性 :Hygroscopic
CAS 数据库 :143201-11-0(CAS DataBase Reference)

安全信息

WGK Germany :3

西立伐他汀钠性质、用途与生产工艺

生物活性 Cerivastatin sodium 是一种合成的降脂剂，是一种高效，耐受性好，口服活性的 HMG-CoA 还原酶抑制剂，Ki 为 1.3 nM/L。Cerivastatin sodium 可降低低密度脂蛋白胆固醇水平。Cerivastatin sodium 还主要通过 RhoA 抑制作用来抑制 MDA-MB-231 细胞的增殖和侵袭，具有抗癌作用。
靶点

Ki: 1.3 nM/L (HMG-CoA reductase)

体外研究

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 (25 ng/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 (25 ng/mL; 18 hours; MDA-MB-231 cells) treatment induces a marked increase in the level of p21 ^Waf1/Cip1 .
Cerivastatin (25 ng/mL; 12 hours; MDA-MB-231 cells) treatment increases the p21 transcript in MDA-MB-231 cells.
Cerivastatin (10-25 ng/mL; 18 hours) inhibits invasion of MDA-MB-231 cells through Matrigel.
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; 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:	5 ng/mL, 10 ng/mL, 25 ng/mL, 50 ng/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:	25 ng/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:	25 ng/mL
Incubation Time:	18 hours
Result:	Induced a marked increase in the level of p21 ^Waf1/Cip1 .

RT-PCR

Cell Line:	MDA-MB-231 cells
Concentration:	25 ng/mL
Incubation Time:	12 hours
Result:	Increased p21 ^Waf1/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.