Rosuvastatin calcium

Names

[ Name ]:
Rosuvastatin calcium

[Synonym ]:
Sodium (6E)-7-{4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl}-3,5-dihydroxy-6-heptenoate
Rosuvastatin Sodium
6-Heptenoic acid, 7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]-3,5-dihydroxy-, sodium salt, (6E)- (1:1)

Biological Activity

[Description]:

Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM[2]. 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[1][2][3].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> HMG-CoA Reductase (HMGCR)

Signaling Pathways >> Autophagy >> Autophagy

Research Areas >> Metabolic Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

[Target]

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

[In Vivo]

Rosuvastatin Sodium (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 Sodium (VLDL) in diabetes mellitus rats induced by Streptozocin[4].

[References]

[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.

[3]. 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.

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