西立伐他汀钠 CAS#: 143201-11-0

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西立伐他汀钠

生物活性靶点体外研究体内研究 用途与合成方法 MSDS 西立伐他汀钠价格(试剂级) 上下游产品信息

中文名称	西立伐他汀钠
中文同义词	西立伐他汀钠;(+)-(3R,5S,6E)-7-[4-(4-氟苯基)-2,6-二异丙基-5-甲氧甲基-吡啶-3-基]-3,5-二羟基-6-庚烯酸单钠盐;西立伐他汀,钠盐;化合物 T10767;PERFEMIKER]西立伐他汀钠,98%
英文名称	Cerivastatin sodium
英文同义词	BAYCOL;6-Heptenoic acid, 7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-bis(1-methylethyl)-3-pyridinyl]-3,5-dihydroxy-, monosodium salt, (3R,5S,6E)-;6-Heptenoic acid, 7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-bis(1-methylethyl)-3-pyridinyl]-3,5-dihydroxy-, monosodium salt, [S-[R*,S*-(E)]]-;BAY-w 6228;Cerivastatin sodium;Sodium 7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-dipropan-2-yl-pyrid in-3-yl]-3,5-dihydroxy-hept-6-enoate;Rivastatin, Baycol, Lipobay;(3R,5S,6E)-7-[4-(4-Fluorophenyl)-5-(MethoxyMethyl)-2,6-bis(1-Methylethyl)-3-pyridinyl]-3,5-dihydroxy-6-heptenoic Acid SodiuM Salt
CAS号	143201-11-0
分子式	C26H35FNNaO5
分子量	483.56
EINECS号
相关类别	心脑血管类科研原料药;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals
Mol文件	143201-11-0.mol
结构式

西立伐他汀钠 性质

西立伐他汀钠 用途与合成方法

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 Cycle Analysis

Western Blot Analysis

RT-PCR

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.

安全信息

MSDS信息

西立伐他汀钠 价格(试剂级)

西立伐他汀钠 上下游产品信息