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编 号:F306449
分子式:C22H28FN3O6S
分子量:481.54
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生物活性:
Rosuvastatin (ZD 4522) 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.

体内研究:
Rosuvastatin (10 mg/kg, intraperitoneal) prolonges QTc in conscious and unrestraines guinea pigs from 201±1 to 210±2 ms. Rosuvastatin (20 mg/kg/day, for 2 weeks) significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin.
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