Rosuvastatin is an inhibitor of HMG-CoA reductase (IC = 5 nM). It inhibits cholesterol synthesis in isolated rat hepatocytes with an IC value of 0.16 nM. Rosuvastatin (10 mg/kg) reduces plasma total cholesterol, triglyceride, LDL-C, and oxidized LDL-C levels in Ldlr mice fed a high-fat diet. It decreases the area of aortic atherosclerotic lesions in the same model. Formulations containing rosuvastatin have been used in the treatment of dyslipidemias.
Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
IC50&Target
IC50: 11 nM (HMG-CoA), 195 nM (hERG)
体内研究
Rosuvastatin (10 mg/kg, intraperitoneal) prolonges QTc in conscious and unrestraines guinea pigs from 201±1 to 210±2 ms[1].
Rosuvastatin (20 mg/kg/day, for 2 weeks) significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin[2].
分子式
C22H28FN3O6S
分子量
481.54
CAS号
287714-41-4
中文名称
罗伐他汀;瑞舒伐他汀
运输条件
Room temperature in continental US; may vary elsewhere.