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Cerivastatin sodium
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cerivastatin sodium图片
CAS NO:143201-11-0
包装与价格:
包装价格(元)
10 mM * 1 mL in Water电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
西立伐他汀钠
产品介绍
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。
生物活性

Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally activeHMG-CoA reductaseinhibitor, with aKiof 1.3 nM/L. Cerivastatin sodium reduces low-density lipoproteincholesterollevels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly byRhoAinhibition, and has anti-cancer effect[1][2].

IC50& Target

Ki: 1.3 nM/L (HMG-CoA reductase)[1][2][3]

体外研究
(In Vitro)

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)[1].
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)[1].
Cerivastatin (25 ng/mL; 18 hours; MDA-MB-231 cells) treatment induces a marked increase in the level of p21Waf1/Cip1[1].
Cerivastatin (25 ng/mL; 12 hours; MDA-MB-231 cells) treatment increases the p21 transcript in MDA-MB-231 cells[1].
Cerivastatin (10-25 ng/mL; 18 hours) inhibits invasion of MDA-MB-231 cells through Matrigel[1].
Cerivastatin (25 ng/mL; 18-36 hours) delocalizes RhoA and Ras from the membrane to the cytosol and induces morphological changes[1].
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[1].

Cell Proliferation Assay[1]

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[1]

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[1]

Cell Line:MDA-MB-231 cells
Concentration:25 ng/mL
Incubation Time:18 hours
Result:Induced a marked increase in the level of p21Waf1/Cip1.

RT-PCR[1]

Cell Line:MDA-MB-231 cells
Concentration:25 ng/mL
Incubation Time:12 hours
Result:Increased p21Waf1/Cip1mRNA levels.
体内研究
(In Vivo)

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[2].

分子量

481.53

性状

Solid

Formula

C26H33FNNaO5

CAS 号

143201-11-0

中文名称

西立伐他汀钠

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
In Vitro: 

H2O : 100 mg/mL(207.67 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.0767 mL10.3836 mL20.7671 mL
5 mM0.4153 mL2.0767 mL4.1534 mL
10 mM0.2077 mL1.0384 mL2.0767 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (protect from light, stored under nitrogen)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。