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143201-11-0

中文名稱 西立伐他汀鈉
英文名稱 Cerivastatin sodium
CAS 143201-11-0
分子式 C26H35FNNaO5
MDL 編號 MFCD00865716
分子量 483.56
MOL 文件 143201-11-0.mol
143201-11-0 結(jié)構(gòu)式 143201-11-0 結(jié)構(gòu)式

基本信息

中文別名
西立伐他汀鈉
(+)-(3R,5S,6E)-7-[4-(4-氟苯基)-2,6-二異丙基-5-甲氧甲基-吡啶-3-基]-3,5-二羥基-6-庚烯酸單鈉鹽
英文別名
BAYCOL
CERIVASTATIN
Rivastatin, Baycol, Lipobay
6-Heptenoic acid, 7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-bis(1-methylethyl)-3-pyridinyl]-3,5-dihydroxy-, monosodium salt, (3R,5S,6E)-
6-Heptenoic acid, 7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-bis(1-methylethyl)-3-pyridinyl]-3,5-dihydroxy-, monosodium salt, [S-[R*,S*-(E)]]-
BAY-w 6228
Cerivastatin sodium
Sodium 7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-dipropan-2-yl-pyrid in-3-yl]-3,5-dihydroxy-hept-6-enoate
所屬類別
原料藥:調(diào)節(jié)血脂藥

物理化學(xué)性質(zhì)

熔點197-199°C
比旋光度D20 +24.1° (c = 1 in ethanol)
儲存條件Hygroscopic, Store under Inert atmosphere -20°C Freezer
溶解度H2O:≥5mg/mL
形態(tài)粉末
顏色白色至棕褐色
旋光度 (Optical Rotation)[α]/D +18 to +26° in ethanol
水溶解性H2O: ≥5mg/mL
穩(wěn)定性吸濕性
CAS 數(shù)據(jù)庫143201-11-0(CAS DataBase Reference)

安全數(shù)據(jù)

危險性符號(GHS)有害 (GHS07)
GHS07
警示詞警告
WGK Germany3
西立伐他汀鈉價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2025/12/22HY-109523西立伐他汀鈉
Cerivastatin sodium
143201-11-01 mg536元
2025/12/22HY-109523西立伐他汀鈉
Cerivastatin sodium
143201-11-05mg1180元
2025/12/22HY-109523西立伐他汀鈉
Cerivastatin sodium
143201-11-010 mM * 1 mLin DMSO1250元

常見問題列表

生物活性
Cerivastatin sodium 是一種合成的降脂劑,是一種高效,耐受性好,口服活性的 HMG-CoA 還原酶抑制劑,Ki 為 1.3 nM/L。Cerivastatin sodium 可降低低密度脂蛋白膽固醇水平。Cerivastatin sodium 還主要通過 RhoA 抑制作用來抑制 MDA-MB-231 細(xì)胞的增殖和侵襲,具有抗癌作用。
靶點

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

體外研究

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).
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).
Cerivastatin (25 ng/mL; 18 hours; MDA-MB-231 cells) treatment induces a marked increase in the level of p21 Waf1/Cip1 .
Cerivastatin (25 ng/mL; 12 hours; MDA-MB-231 cells) treatment increases the p21 transcript in MDA-MB-231 cells.
Cerivastatin (10-25 ng/mL; 18 hours) inhibits invasion of MDA-MB-231 cells through Matrigel.
Cerivastatin (25 ng/mL; 18-36 hours) delocalizes RhoA and Ras from the membrane to the cytosol and induces morphological changes.
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.

Cell Proliferation Assay

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

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

Cell Line: MDA-MB-231 cells
Concentration: 25 ng/mL
Incubation Time: 18 hours
Result: Induced a marked increase in the level of p21 Waf1/Cip1 .

RT-PCR

Cell Line: MDA-MB-231 cells
Concentration: 25 ng/mL
Incubation Time: 12 hours
Result: Increased p21 Waf1/Cip1 mRNA levels.
體內(nèi)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.

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