Simvastatin
作者：齊岳
發(fā)布時(shí)間：2023-08-30
09:00:49
點(diǎn)擊數(shù)：
產(chǎn)品名稱：Simvastatin
產(chǎn)品描述：
| 結(jié)構(gòu)類型 | 天然產(chǎn)物 > 萜類 |
| 產(chǎn)品描述 | Simvastatin is a HMG-CoA Reductase Inhibitor. The mechanism of action of simvastatin is as a Hydroxymethylglutaryl-CoA Reductase Inhibitor. |
| 靶點(diǎn)活性 | HMG-CoA reductase:0.1-0.2 nM(Ki) |
| 體外活性 | 給高膽固醇飲食喂養(yǎng)的兔子每天口服4 mg Simvastatin13周,使膽固醇誘導(dǎo)的總膽固醇量、LDL膽固醇以及HDL膽固醇增加恢復(fù)到正常水平.在含有0.25%膽固醇飲食喂養(yǎng)的兔子體內(nèi),6 mg/kg Simvastatin增加LDL受體依賴性結(jié)合,也使肝臟LDL受體數(shù)量增加.Simvastatin口服給藥抑制放射性乙酸鹽轉(zhuǎn)化為膽固醇,IC50為0.2 mg/kg. |
| 體內(nèi)活性 | Simvastatin抑制小鼠L-M cell(成纖維細(xì)胞)（IC50=19.3 nM）,大鼠H4II E細(xì)胞(肝臟)（IC50=13.3 nM）膽固醇合成,并且能夠抑制人類Hep G2細(xì)胞(肝臟)中膽固醇合成,IC50值為15.6 nM。 |
| 激酶實(shí)驗(yàn) | For assessment of Akt protein kinase activity in vitro, substrate (2 μg histone H2B or 25 μg eNOS peptide) is incubated with Akt immunoprecipitated from cell lysate using goat polyclonal anti-Akt1 antibody. Kinase reactions are initiated following the addition of reaction components to a final concentration of ATP (50 μM) containing 10 μCi of 32P-γATP, dithiotreitol (1 mM), HEPES buffer (20 mM, pH 7.4), MnCl2 (10 mM), MgCl2 (10 mM). After incubation for 30 min at 30°C, phosphorylated histone H2B is visualized after SDS-PAGE (15%) and autoradiography. To estimate the extent of 32P incorporation into eNOS peptides, each reaction mixture is measured by spotting onto phosphocellulose disc filter and the amount of phosphate incorporated is measured by Cerenkov counting. The wild-type peptide sequence is 1174-RIRTQSFSLQERHLRGAVPWA-1194, and the mutant eNOS peptide is identical except that serine 1179 is substituted by alanine. |
| 別名 | 辛伐他汀, MK-0733, MK 733 |
| 分子量 | 418.57 |
| 分子式 | C25H38O5 |
| CAS No. | 79902-63-9 |
存儲(chǔ)
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: 31.4 mg/mL (75 mM)
DMSO: 20.9 mg/mL (50 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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