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西立伐他汀钠

西立伐他汀钠 更多供应商
公司名称: 北京百灵威科技有限公司  
联系电话: 400-666-7788 010-82848833
产品介绍: 中文名称:西立伐他汀,钠盐
英文名称:Cerivastatin, SodiuM Salt
CAS:143201-11-0
包装信息:100Mg,10Mg,5Mg 备注:化学试剂、精细化学品、医药中间体、材料中间体
公司名称: 凯试(上海)科技有限公司  
联系电话: 021-50135380
产品介绍: 英文名称:Cerivastatin, SodiuM Salt
CAS:143201-11-0
纯度:98% 备注:1500元/5mg; 1950元/10mg; 12000元/100mg
公司名称: 深圳菲斯生物科技有限公司  
联系电话: 13380397412
产品介绍: 中文名称:西立伐他汀钠
英文名称:Cerivastatin sodium
CAS:143201-11-0
纯度:99% HPLC 包装信息:10mg;25mg;50mg;100mg 备注:品牌:sinco,适用于药品研发生产和申报
公司名称: 广州爱纯医药科技有限公司  
联系电话: 18927568969 020-39119399
产品介绍: 英文名称:Cerivastatin sodium salt hydrate
纯度:98% (HPLC) 包装信息:5MG; 25MG; 100MG; 1G 备注:BR
公司名称: Cato Research Chemicals Inc.  
联系电话: +1-541-2553640
产品介绍: 英文名称:Cerivastatin, SodiuM Salt
CAS:143201-11-0
纯度:95% 包装信息:25Mg, 50Mg
西立伐他汀钠
生物活性靶点体外研究体内研究
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
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:C26H34FNO5
分子量:459.55
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
西立伐他汀钠
西立伐他汀钠 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
CAS 数据库143201-11-0(CAS DataBase Reference)
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 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.

安全信息
WGK Germany 3
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