(3R,5R)-Rosuvastatin

(3R,5R)-Rosuvastatin

• CAS Number: 1094100-06-7
• UNSPSC Description: (3R,5R)-Rosuvastatin is the (3R,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].
• Target Antigen: 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/3r-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 Weight: 481.54
• 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.
• Shipping Conditions: Room temperature
• Clinical Information: No Development Reported