Rosuvastatin-₁₃C,d₃ sodium  (Synonyms: ZD 4522-₁₃C,d₃ sodium; X-Plended-₁₃C,d₃ sodium; Crestor-₁₃C,d₃ sodium)

Rosuvastatin-¹³C,d₃ sodium is ¹³C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC₅₀ of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC₅₀ of 195 nM^[2]. Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels^[1][2][3].

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Rosuvastatin Sodium (10 mg/kg, intraperitoneal) prolonges QTc in conscious and unrestraines guinea pigs from 201±1 to 210±2 ms^[3].
Rosuvastatin (20 mg/kg/day, for 2 weeks) significantly reduces very low-density lipoproteins Sodium (VLDL) in diabetes mellitus rats induced by Streptozocin^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

507.53

C₂₁¹³CH₂₄D₃FN₃NaO₆S

O=C(O[Na])C[C@H](O)C[C@H](O)/C=C/C1=C(C(C)C)N=C(N([13C]([2H])([2H])[2H])S(=O)(C)=O)N=C1C2=CC=C(C=C2)F

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [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.  [Content Brief]

  [3]. Plante I, et al. Rosuvastatin blocks hERG current and prolongs cardiac repolarization. J Pharm Sci. 2012 Feb;101(2):868-78.  [Content Brief]

  [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.  [Content Brief]

  [5]. Carswell C.I., et al. Rosuvastatin. Drugs, 2002. 62(14): p. 2075-85; discussion 2086-7.  [Content Brief]