中文名称: | 西立伐他汀 | ||||
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英文名称: | Cerivastatin | ||||
别名: | (3R,5S,6E)-7-[4-(4-Fluorophenyl)-2,6-diisopropyl-5-(methoxymethyl)-3-pyridyl]-3,5-dihydroxy-6-heptenoic acid | ||||
CAS No: | 145599-86-6 | 分子式: | C26H34FNO5 | 分子量: | 459.55 |
CAS No: | 145599-86-6 | ||||
分子式: | C26H34FNO5 | ||||
分子量: | 459.55 |
基本信息
产品编号: |
C10862 |
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产品名称: |
Cerivastatin |
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CAS: |
145599-86-6 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
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分子量 |
459.55 |
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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。 |
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靶点 |
Ki: 1.3nM/L (HMG-CoA reductase) |
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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 |
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Cell Line: |
MDA-MB-231 cells |
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Concentration: |
5ng/mL, 10ng/mL, 25ng/mL, 50ng/mL |
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Incubation Time: |
3 days |
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Result: |
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: |
MDA-MB-231 cells |
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Concentration: |
25ng/mL |
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Incubation Time: |
18 hours, 36 hours |
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Result: |
Induced a cell cycle block in G 1/S phase. |
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Western Blot Analysis |
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Cell Line: |
MDA-MB-231 cells |
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Concentration: |
25ng/mL |
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Incubation Time: |
18 hours |
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Result: |
Induced a marked increase in the level of p21Waf1/Cip1 |
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RT-PCR |
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Cell Line: |
MDA-MB-231 cells |
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Concentration: |
25ng/mL |
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Incubation Time: |
12 hours |
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Result: |
Increased p21Waf1/Cip1 mRNA levels. |
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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 |
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
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
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )