Rosuvastatin-d6 is intended for use as an internal standard for the quantification of rosuvastatin by GC- or LC-MS. Rosuvastatin is an inhibitor of HMG-CoA reductase (IC50 = 5 nM).1 It inhibits cholesterol synthesis in isolated rat hepatocytes with an IC50 value of 0.16 nM.2 Rosuvastatin (10 mg/kg) reduces plasma total cholesterol, triglyceride, LDL-C, and oxidized LDL-C levels in Ldlr-/- mice fed a high-fat diet.3 It decreases the area of aortic atherosclerotic lesions in the same model. Formulations containing rosuvastatin have been used in the treatment of dyslipidemias.
1.Istvan, E.S., and Deisenhofer, J.Structural mechanism for statin inhibition of HMG-CoA reductaseScience292(5519)1160-1164(2001) 2.McTaggart, F., Buckett, L., Davidson, R., et al.Preclinical and clinical pharmacology of Rosuvastatin, a new 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitorAm. J. Cardiol.87(5A)28B-32B(2001) 3.Guo, H., Shi, Y., Liu, L., et al.Rosuvastatin inhibits MMP-2 expression and limits the progression of atherosclerosis in LDLR-deficient miceArch. Med. Res.40(5)345-351(2009)