SimvaSTATin 是一种 HMG-CoA 还原酶抑制剂，其作用机制是作为羟甲基戊二酰辅酶A还原酶抑制剂。

Simvastatin is a HMG-CoA Reductase Inhibitor. The mechanism of action of simvastatin is as a Hydroxymethylglutaryl-CoA Reductase Inhibitor.

给高胆固醇饮食喂养的兔子每天口服4 mg Simvastatin13周,使胆固醇诱导的总胆固醇量、LDL胆固醇以及HDL胆固醇增加恢复到正常水平.在含有0.25%胆固醇饮食喂养的兔子体内,6 mg/kg Simvastatin增加LDL受体依赖性结合,也使肝脏LDL受体数量增加.Simvastatin口服给药抑制放射性乙酸盐转化为胆固醇,IC50为0.2 mg/kg.

Simvastatin抑制小鼠L-M cell(成纤维细胞)（IC50=19.3 nM）,大鼠H4II E细胞(肝脏)（IC50=13.3 nM）胆固醇合成,并且能够抑制人类Hep G2细胞(肝脏)中胆固醇合成,IC50值为15.6 nM。

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.

79902-63-9

C25H38O5

418.57

MK-0733;MK 733;辛伐他汀

DMSO:20.9 mg/mL (50 mM)
Ethanol:31.4 mg/mL (75 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years