143201-11-0
基本信息
(+)-(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
CERIVASTATIN
Rivastatin, Baycol, Lipobay
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
物理化学性质
| 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 | 粉末 |
| 颜色 | 白色至棕褐色 |
| 旋光性 (optical activity) | [α]/D +18 to +26° in ethanol |
| 稳定性 | 吸湿性 |
| CAS 数据库 | 143201-11-0(CAS DataBase Reference) |
安全数据
| WGK Germany | 3 |
常见问题列表
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
.
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. |
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.