Rosuvastatin Calcium  (Synonyms: Rosuvastatin hemicalcium; ZD 4522 Calcium)

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].

IC50: 11 nM (HMG-CoA), 195 nM (hERG)^[1][2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

500.57

Solid

C₂₂H₂₇Ca_0.5FN₃O₆S

147098-20-2

O=C([O-])C[[email protected]](O)C[[email protected]](O)/C=C/C1=C(C(C)C)N=C(N(C)S(=O)(C)=O)N=C1C2=CC=C(F)C=C2.[0.5Ca2+]

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [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.  [Content Brief]

  [2]. Carswell C.I., et al. Rosuvastatin. Drugs, 2002. 62(14): p. 2075-85; discussion 2086-7.  [Content Brief]

  [3]. Plante I, et al. Rosuvastatin blocks hERG current and prolongs cardiac repolarization. J Pharm Sci. 2012 Feb;101(2):868-78.  [Content Brief]

  [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.  [Content Brief]