Vorapaxar-d₅  (Synonyms: SCH 530348-d₅)

Vorapaxar-d₅ is deuterated labeled Vorapaxar (HY-10119). Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (K_i=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner^[1].

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].
Vorapaxar (SCH 530348) shows potent inhibition of thrombin-induced platelet aggregation with an IC₅₀ of 47 nM and haTRAP-induced platelet aggregation with an IC₅₀ of 25 nM. Vorapaxar (SCH 530348) inhibits thrombininduced calcium transient in human coronary artery smooth muscle cells (HCASMC) with a K_i of 1.1 nM. It also inhibits thrombin-stimulated thymidine incorporation in HCASMC with a Ki of 13 nM^[2].

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

497.61

C₂₉H₂₈D₅FN₂O₄

618385-01-6

FC1=C(C=CC=C1)C(C=N2)=CC=C2/C=C/[C@@H](C(C(C3)C4)CC[C@H]3NC(OC([2H])(C([2H])([2H])[2H])[2H])=O)C5C4C(O[C@@H]5C)=O

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]. Khoufache K, et al. PAR1 contributes to influenza A virus pathogenicity in mice. J Clin Invest. 2013 Jan;123(1):206-14.  [Content Brief]

  [3]. Kehinde O, et al. Vorapaxar: A novel agent to be considered in the secondary prevention of myocardial infarction. J Pharm Bioallied Sci. 2016 Apr-Jun;8(2):98-105.  [Content Brief]