Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC 50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC 50 of 195 nM. Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
性状
Solid
IC50 & Target[1][2]
IC50: 11 nM (HMG-CoA), 195 nM (hERG)
体内研究(In Vivo)
Rosuvastatin Sodium (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 Sodium (VLDL) in diabetes mellitus rats induced by Streptozocin. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
ClinicalTrial
参考文献
[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]. Plante I, et al. Rosuvastatin blocks hERG current and prolongs cardiac repolarization. J Pharm Sci. 2012 Feb;101(2):868-78.
溶解度数据
In Vitro: DMSO : 250 mg/mL (496.50 mM; Need ultrasonic)配制储备液