中文名称: | 西立伐他汀钠 | ||||
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英文名称: | Cerivastatin sodium | ||||
别名: | 西立伐他汀钠;(+)-(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;西伐他汀钠盐;西立伐他汀 Cerivastatin sodium;Sodium 7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-dipropan-2-yl-pyrid in-3-yl]-3,5-dihydroxy-hept-6-enoate;Cerivastatin, SodiuM Salt;sodium,(E,3R,5S)-7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-di(propan-2-yl)pyridin-3-yl]-3,5-dihydroxyhept-6-enoate | ||||
CAS No: | 143201-11-0 | 分子式: | C26H33FNNaO5 | 分子量: | 481.53 |
CAS No: | 143201-11-0 | ||||
分子式: | C26H33FNNaO5 | ||||
分子量: | 481.53 |
基本信息
产品编号: |
C10861 |
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产品名称: |
Cerivastatin sodium |
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CAS: |
143201-11-0 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
481.53 |
-20℃ |
一个月 |
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化学名: |
sodium,(E,3R,5S)-7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-di(propan-2-yl)pyridin-3-yl]-3,5-dihydroxyhept-6-enoate |
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Solubility (25°C): |
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体外:
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DMSO |
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Ethanol |
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Water |
100mg/mL(207.67mM;ultrasonic and warming and heat to 60°C) |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.0767mL |
10.3836mL |
20.7671mL |
5mM |
0.4153mL |
2.0767mL |
4.1534mL |
10mM |
0.2077mL |
1.0384mL |
2.0767mL |
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 |
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 |
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 |
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 |
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 )