1242184-42-4

1242184-42-4 structure

Name: (3S,5R)-Rosuvastatin
Chemical Name: rosuvastatin
CAS Number: 1242184-42-4
Molecular Formula: C₂₂H₂₈FN₃O₆S
Molecular Weight: 481.53800
Catalog: Signaling Pathways Autophagy Autophagy
Create Date: 2018-05-30 16:14:19
Modify Date: 2024-01-03 18:00:18
(3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin 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[2]. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels[3].

Name	rosuvastatin
Synonyms	(3S,5R)-Rosuvastatin Sodium Salt (3S,5R)-Rosuvastatin Rosuvastatin Acid Enantiomer

Description	(3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin 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[2]. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels[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)[1] and 195 nM (hERG)[2]
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.