(3S,5R)-Rosuvastatin

Modify Date: 2024-01-03 18:00:18

(3S,5R)-Rosuvastatin Structure
(3S,5R)-Rosuvastatin structure
Common Name (3S,5R)-Rosuvastatin
CAS Number 1242184-42-4 Molecular Weight 481.53800
Density 1.368±0.06 g/cm3 Boiling Point N/A
Molecular Formula C22H28FN3O6S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of (3S,5R)-Rosuvastatin


(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].

 Names

Name rosuvastatin
Synonym More Synonyms

 (3S,5R)-Rosuvastatin Biological Activity

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
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.

 Chemical & Physical Properties

Density 1.368±0.06 g/cm3
Molecular Formula C22H28FN3O6S
Molecular Weight 481.53800
Exact Mass 481.16800
PSA 149.30000
LogP 3.48250
Water Solubility Very slightly soluble (0.17 g/L) (25 ºC)

 Synonyms

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