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Vorapaxar

Catalog No. T7013 CAS 618385-01-6

Synonyms: SCH 530348, MK-5348

Vorapaxar (MK-5348) (SCH 530348) is an effective and orally active thrombin receptor (PAR-1) antagonist (Ki: 8.1 nM).

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Vorapaxar, CAS 618385-01-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 68.00
5 mg	In stock	$ 148.00
10 mg	In stock	$ 228.00
25 mg	In stock	$ 413.00
50 mg	In stock	$ 618.00
100 mg	In stock	$ 879.00
500 mg	In stock	$ 1,750.00
1 mL * 10 mM (in DMSO)	In stock	$ 163.00

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Purity: 99.93%

Purity: 99.42%

Purity: 99.27%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Vorapaxar (MK-5348) (SCH 530348) is an effective and orally active thrombin receptor (PAR-1) antagonist (Ki: 8.1 nM).
Targets&IC50	PAR1:8.1 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]

Synonyms	SCH 530348, MK-5348
Molecular Weight	492.58
Formula	C29H33FN2O4
CAS No.	618385-01-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 92 mg/mL (186.8 mM)

DMSO: 92 mg/mL (186.8 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Chackalamannil S, et al. J Med Chem, 2008, 51(11), 3061-3064. 2. Tang W, Huang B, Wang J, et al. A label-free screening approach targeted protease-activated receptor 1 based on dynamic mass redistribution in living cells[J]. RSC Advances. 2017, 7(68): 43005-43013.

Citations

1. Tang W, Huang B, Wang J, et al. A label-free screening approach targeted protease-activated receptor 1 based on dynamic mass redistribution in living cells. RSC Advances. 2017, 7(68): 43005-43013

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library EMA Approved Drug Library Anti-Cancer Approved Drug Library GPCR Compound Library FDA-Approved Drug Library Immunology/Inflammation Compound Library

Related Products

Related compounds with same targets

Parmodulin 2 Trypsin PAR-4 Agonist Peptide, amide acetate TRAP-6 amide acetate PAR-2-IN-1 SCH79797 dihydrochloride Atopaxar PAR-2 Activating Peptide acetate

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Vorapaxar 618385-01-6 GPCR/G Protein Protease-activated Receptor Protease Activated Receptor (PAR) Inhibitor MK 5348 SCH530348 MK5348 SCH-530348 SCH 530348 Thrombin receptors inhibit MK-5348 inhibitor

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