Rosuvastatin-d6

Rosuvastatin-d6 (ZD 4522-d6) is deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels[1][2][3].

Product Specifications

CAS Number

[2070009-40-2]

Product Name Alternative

ZD 4522-d6

UNSPSC

12352211

Target

Autophagy; Bacterial; HMG-CoA Reductase (HMGCR) ; Isotope-Labeled Compounds; Potassium Channel

Related Pathways

Anti-infection; Autophagy; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Others

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease; Cardiovascular Disease; Cancer

Smiles

OC(C[C@H](O)C[C@H](O)/C=C/C1=C(C(C([2H])([2H])[2H])C([2H])([2H])[2H])N=C(N(C)S(C)(=O)=O)N=C1C2=CC=C(C=C2)F)=O

Molecular Formula

C22H22D6FN3O6S

Molecular Weight

487.57

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]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.|[3]Plante I, et al. Rosuvastatin blocks hERG current and prolongs cardiac repolarization. J Pharm Sci. 2012 Feb;101 (2) :868-78.|[4]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.|[5]Carswell C.I., et al. Rosuvastatin. Drugs, 2002. 62 (14) : p. 2075-85; discussion 2086-7.