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Rosuvastatin-d6

CAT: 0804-HY-17504AS1Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-17504AS1Size:1 Each
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Description
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].
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.
Shipping Conditions
Room temperature
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported