RosuvastatinD3(ZD4522D3)是Rosuvastatin的一种氘代化合物。Rosuvastatin(ZD4522)是一种竞争性HMG-CoA还原酶抑制剂，IC50为11nM。Rosuvastatin有效阻断人类醚-a-go-go相关基因(hERG)电流，IC50为195nM，延迟心脏复极化，从而延长动作电位持续时间(APDs)和校正QT间期(QTc)间隔。
Rosuvastatin D3 (ZD 4522 D3) is a deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM[1]. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals[2].
[1]. 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. [2]. Carswell C.I., et al. Rosuvastatin. Drugs, 2002. 62(14): p. 2075-85; discussion 2086-7.
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