(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].

Product Specifications

CAS Number

[1242184-42-4]

UNSPSC

12352005

Hazard Statement

H361-H373

Target

Autophagy; HMG-CoA Reductase (HMGCR) ; Potassium Channel

Type

Reference compound

Related Pathways

Autophagy; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Metabolic Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/3s-5r-rosuvastatin.html

Solubility

10 mM in DMSO

Smiles

O=C(O)C[C@@H](O)C[C@@H](O)/C=C/C1=C(C(C)C)N=C(N(C)S(=O)(C)=O)N=C1C2=CC=C(F)C=C2

Molecular Formula

C22H28FN3O6S

Molecular Weight

481.54

Precautions

P260-P280-P405-P501

References & Citations

[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.