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GPCR/G Protein Protease-activated Receptor Vorapaxar

Vorapaxar

Catalog No. T7013   CAS 618385-01-6
Synonyms: SCH 530348, MK-5348

Vorapaxar (SCH 530348) is an effective and orally active thrombin receptor (PAR-1) antagonist (Ki: 8.1 nM).

Vorapaxar, CAS 618385-01-6
Pack Size Availability Price/USD Quantity
2 mg In stock 85.00
5 mg In stock 150.00
10 mg In stock 260.00
25 mg In stock 580.00
50 mg In stock 880.00
1 mL * 10 mM (in DMSO) In stock 150.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Vorapaxar (SCH 530348) is an effective and orally active thrombin receptor (PAR-1) antagonist (Ki: 8.1 nM).
Targets&IC50 PAR-1 : 8.1nM(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]
Animal Research
Animal Model: cynomolgus monkeys
Synonyms SCH 530348 , MK-5348
Purity 99.93%
Molecular Weight 492.58
Formula C29H33FN2O4
CAS No. 618385-01-6

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 92 mg/mL (186.8 mM)

Ethanol: 92 mg/mL (186.8 mM)

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Chackalamannil S, et al. J Med Chem, 2008, 51(11), 3061-3064. 2. 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.

Related compound libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library FDA-approved Drug Library GPCR Compound Library Fluorochemical Library Anti-Cardiovascular Disease Compound Library

Related Products

Related compounds with same targets
TFLLR-NH2 2TFA(197794-83-5(free base)) Thrombin Receptor Activator for Peptide AZ3451 Thrombin Receptor Activator for Peptide Protease-Activated Receptor-4 diTFA(245443-52-1(free base)) PAR-4 Agonist Peptide, amide TFA 2-Furoyl-LIGRLO-amide TFA(729589-58-6 free base) AC264613

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