Product Description: Rosuvastatin-d6 (ZD 4522-d6) is deuterium labeled Rosuvastatin. 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[1][2][3].
Applications: Metabolism-sugar/lipid metabolism
Formula: C22H22D6FN3O6S
References: [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216./[2]Watanabe, M., et al., Synthesis and biological activity of methanesulfonamide pyrimidine- and N-methanesulfonyl pyrrole-substituted 3,5-dihydroxy-6-heptenoates, a novel series of HMG-CoA reductase inhibitors. Bioorg Med Chem, 1997. 5(2): p. 437-44./[3]Plante I, et al. Rosuvastatin blocks hERG current and prolongs cardiac repolarization. J Pharm Sci. 2012 Feb;101(2):868-78./[4]Feng PF, et al. Intracellular Mechanism of Rosuvastatin-Induced Decrease in Mature hERG Protein Expression on Membrane. Mol Pharm. 2019 Apr 1;16(4):1477-1488./[5]Carswell C.I., et al. Rosuvastatin. Drugs, 2002. 62(14): p. 2075-85; discussion 2086-7.
CAS Number: 2070009-40-2
Molecular Weight: 487.57
Research Area: Metabolic Disease;Cardiovascular Disease;Cancer
Target: Autophagy;Bacterial;HMG-CoA Reductase (HMGCR);Isotope-Labeled Compounds;Potassium Channel
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