Vorapaxar

Catalog No.S8067 Synonyms: SCH 530348, MK-5348

Vorapaxar Chemical Structure

Molecular Weight(MW): 492.58

Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.

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Biological Activity

Description Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.
Targets
PAR-1 [1]
(Cell-free assay)
8.1 nM(Ki)
In vitro

SCH 530348 is a synthetic tricyclic 3-phenylpyridine and an orally active himbacine-based thrombin-receptor antagonist. 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, whereas it shows no inhibition of platelet aggregation induced by other agonists such as ADP, collagen and a PAR-4 agonist peptide. SCH 530348 also has no affect on the prothrombin time (PT), partial thromboplastin time (PTT), or activated partial thromboplastin time (aPTT). Moreover, SCH 530348 causes no increase in the bleeding time or in surgical bleeding compared with inactive control. SCH530348 is found to be selective for PAR-1 when tested over a number of ion channels and receptors, including PAR-4 receptor. [1]

In vivo SCH 530348 is well absorbed in rat (68%; 10 mg/kg) and in monkey (82%; 1 mg/kg) models. Tmax is observed at about 3 h in rats and 1 h in monkeys. The elimination half-life is 5.1 h in rats and 13 h in monkeys. The oral bioavailability is 33% in rats and 86% in monkeys. In preclinical studies in cynomolgus monkey platelets, oral administration of SCH 530348 at a dose greater than 0.1 mg/kg resulted in 100% inhibition of thrombin-receptor agonist peptide (TRAP)-induced platelet aggregation for 24 h with partial recovery occurring at 48 h. [1]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: cynomolgus monkeys
  • Formulation: 0.4% methyl cellulose
  • Dosages: 0.5, 0.3, 0.1, and 0.05 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 99 mg/mL (200.98 mM)
Ethanol 99 mg/mL (200.98 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 492.58
Formula

C29H33FN2O4

CAS No. 618385-01-6
Storage powder
in solvent
Synonyms SCH 530348, MK-5348

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02975583 Not yet recruiting Peripheral Artery Disease Vanderbilt University|Merck Sharp & Dohme Corp. December 2016 Phase 4
NCT02660866 Recruiting Peripheral Arterial Disease North Texas Veterans Healthcare System July 2016 Phase 4
NCT02875028 Recruiting Healthy Volunteers Medical University of Vienna June 2016 Phase 4
NCT02548650 Recruiting Myocardial Infarction|Diabetes Mellitus University of Florida|Merck Sharp & Dohme Corp. March 2016 Phase 4
NCT02545933 Recruiting Myocardial Infarction University of Florida|Merck Sharp & Dohme Corp. February 2016 Phase 4
NCT02629367 Not yet recruiting Coronary Artery Disease Inova Health Care Services January 2016 Phase 4

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Protease-activated Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID