Bioactivity | Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC50 of 195 nM[2]. Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels[1][2][3]. |
Target | IC50: 11 nM (HMG-CoA), 195 nM (hERG) |
In Vivo | Rosuvastatin Calcium (10 mg/kg, intraperitoneal) prolonges QTc in conscious and unrestraines guinea pigs from 201±1 to 210±2 ms[2]. Rosuvastatin (20 mg/kg/day, for 2 weeks) significantly reduces very low-density lipoproteins Calcium (VLDL) in diabetes mellitus rats induced by Streptozocin[4]. |
Name | Rosuvastatin Calcium |
CAS | 147098-20-2 |
Formula | C22H27Ca0.5FN3O6S |
Molar Mass | 500.57 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [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. [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. |