西立伐他汀钠
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- CAS号:
- 143201-11-0
- 英文名:
- Cerivastatin sodium
- 英文别名:
- BAYCOL;BAY-w 6228;Rivastatin hydrate;Cerivastatin sodium;Rivastatin, Baycol, Lipobay;Cerivastatin-13C-d3 Sodium Salt;Cerivastatin sodium salt hydrate;Sodium 7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-dipropan-2-yl-pyrid in-3-yl]-3,5-dihydroxy-hept-6-enoate;(3R,5S,6E)-7-[4-(4-Fluorophenyl)-5-(MethoxyMethyl)-2,6-bis(1-Methylethyl)-3-pyridinyl]-3,5-dihydroxy-6-heptenoic Acid SodiuM Salt;(3R,5S,6E)-7-[4-(4-Fluorophenyl)-5-(methoxymethyl)-2,6-bis(1-methylethyl)-3-pyridinyl]-3,5-dihydroxy-6-heptenoic acid sodium salt hydrate
- 中文名:
- 西立伐他汀钠
- 中文别名:
- 西立伐他汀钠;西立伐他汀,钠盐;化合物 T10767;PERFEMIKER]西立伐他汀钠,98%;(+)-(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
- CBNumber:
- CB5115264
- 分子式:
- C26H35FNNaO5
- 分子量:
- 483.56
- MOL File:
- 143201-11-0.mol
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西立伐他汀钠化学性质
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熔点:
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197-199°C
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比旋光度:
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D20 +24.1° (c = 1 in ethanol)
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储存条件:
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Hygroscopic, Store under Inert atmosphere -20°C Freezer
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溶解度:
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H2O: ≥5mg/mL
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形态:
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powder
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颜色:
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white to tan
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旋光性 (optical activity):
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[α]/D +18 to +26° in ethanol
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稳定性:
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Hygroscopic
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CAS 数据库:
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143201-11-0(CAS DataBase Reference)
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西立伐他汀钠性质、用途与生产工艺
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。
Ki: 1.3 nM/L (HMG-CoA reductase)
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
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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
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Cell Line:
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MDA-MB-231 cells
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Concentration:
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5 ng/mL, 10 ng/mL, 25 ng/mL, 50 ng/mL
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Incubation Time:
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3 days
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Result:
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Induced a dose-dependent decrease in cell proliferation of MDA-MB-231 cells.
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Cell Cycle Analysis
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Cell Line:
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MDA-MB-231 cells
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Concentration:
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25 ng/mL
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Incubation Time:
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18 hours, 36 hours
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Result:
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Induced a cell cycle block in G 1/S phase.
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Western Blot Analysis
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Cell Line:
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MDA-MB-231 cells
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Concentration:
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25 ng/mL
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Incubation Time:
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18 hours
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Result:
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Induced a marked increase in the level of p21
Waf1/Cip1
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RT-PCR
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Cell Line:
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MDA-MB-231 cells
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Concentration:
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25 ng/mL
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Incubation Time:
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12 hours
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Result:
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Increased p21
Waf1/Cip1
mRNA levels.
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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.
西立伐他汀钠
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-109523 | Cerivastatin sodium | | 1 mg | 636元 |
| 2024/04/30 | HY-109523 | 西立伐他汀钠
Cerivastatin sodium | 143201-11-0 | 5mg | 1400元 |
西立伐他汀钠
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143201-11-0, 西立伐他汀钠 相关搜索:
- Pharmaceuticals
- Intermediates & Fine Chemicals
- Inhibitors
- 心脑血管类科研原料药
- C26H33FNNaO5
- 145599-86-0
- PERFEMIKER]西立伐他汀钠,98%
- 化合物 T10767
- 西立伐他汀,钠盐
- (+)-(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
- 143201-11-0
- Cerivastatin-13C-d3 Sodium Salt
- Rivastatin hydrate
- Cerivastatin sodium salt hydrate
- (3R,5S,6E)-7-[4-(4-Fluorophenyl)-5-(methoxymethyl)-2,6-bis(1-methylethyl)-3-pyridinyl]-3,5-dihydroxy-6-heptenoic acid sodium salt hydrate
- (3R,5S,6E)-7-[4-(4-Fluorophenyl)-5-(MethoxyMethyl)-2,6-bis(1-Methylethyl)-3-pyridinyl]-3,5-dihydroxy-6-heptenoic Acid SodiuM Salt
- Rivastatin, Baycol, Lipobay
- Sodium 7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-dipropan-2-yl-pyrid in-3-yl]-3,5-dihydroxy-hept-6-enoate
- Cerivastatin sodium
- BAY-w 6228
- 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)]]-
- 6-Heptenoic acid, 7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-bis(1-methylethyl)-3-pyridinyl]-3,5-dihydroxy-, monosodium salt, (3R,5S,6E)-
- BAYCOL