Cerivastatin sodium(Synonyms: 西立伐他汀钠)

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Cerivastatin sodium (Synonyms: 西立伐他汀钠) 纯度: 99.84%

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。

Cerivastatin sodium(Synonyms: 西立伐他汀钠)

Cerivastatin sodium Chemical Structure

CAS No. : 143201-11-0

规格 价格 是否有货 数量
10 mM * 1 mL in Water ￥3600 In-stock
5 mg ￥3400 In-stock
10 mg ￥5750 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

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生物活性

Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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/Cip1 mRNA 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

481.53

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°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0767 mL 10.3836 mL 20.7671 mL
5 mM 0.4153 mL 2.0767 mL 4.1534 mL
10 mM 0.2077 mL 1.0384 mL 2.0767 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°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Denoyelle C, et al. Cerivastatin, an inhibitor of HMG-CoA reductase, inhibits the signaling pathways involved in the invasiveness and metastatic properties of highly invasive breast cancer cell lines: an in vitro study. Carcinogenesis. 2001 Aug;22(8):1139-48.

    [2]. Stein E, et al. Cerivastatin, a New Potent Synthetic HMG Co-A Reductase Inhibitor: Effect of 0.2 mg Daily in Subjects With Primary Hypercholesterolemia. J Cardiovasc Pharmacol Ther. 1997 Jan;2(1):7-16.

    [3]. Furberg CD, et al. Withdrawal of cerivastatin from the world market. Curr Control Trials Cardiovasc Med. 2001;2(5):205-207.

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