中文名称: 西立伐他汀
英文名称: Cerivastatin
CAS No: 145599-86-6
分子式: C26H34FNO5
分子量: 459.55
C10862 西立伐他汀 (psaitong)
包装规格:
5mg 25mg in glass bottle
产品描述:

基本信息

产品编号:

C10862

产品名称:

Cerivastatin

CAS:

145599-86-6

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C26H34FNO5

溶于液体

 

 

分子量

459.55

 

 

化学名: 

(3R,5S,6E)-7-[4-(4-Fluorophenyl)-2,6-diisopropyl-5-(methoxymethyl)-3-pyridyl]-3,5-dihydroxy-6-heptenoic acid

 

生物活性

产品描述

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1.3nM/L。

靶点

Ki: 1.3nM/L (HMG-CoA reductase)

体外研究

Cerivastatin (5-50ng/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 25ng/mL). Cerivastatin (25ng/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 (25ng/mL; 18 hours; MDA-MB-231 cells) treatment induces a marked increase in the level of p21Waf1/Cip1. Cerivastatin (25ng/mL; 12 hours; MDA-MB-231 cells) treatment increases the p21 transcript in MDA-MB-231 cells.

Cerivastatin (10-25ng/mL; 18 hours) inhibits invasion of MDA-MB-231 cells through Matrigel.

Cerivastatin (25ng/mL; 18-36 hours) delocalizes RhoA and Ras from the membrane to the cytosol and induces morphological changes.

Cerivastatin (25ng/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:

5ng/mL, 10ng/mL, 25ng/mL, 50ng/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:

25ng/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:

25ng/mL

Incubation Time:

18 hours

Result:

Induced a marked increase in the level of p21Waf1/Cip1

RT-PCR

Cell Line:

MDA-MB-231 cells

Concentration:

25ng/mL

Incubation Time:

12 hours

Result:

Increased p21Waf1/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

 

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
搜索质检报告(COA)
参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

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用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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    C8=C7/X C8: LOG(C8):