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Vorapaxar

Catalog No. T7013Cas No. 618385-01-6
Alias SCH 530348, MK-5348

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

Vorapaxar

Vorapaxar

Purity: 99.93%
Catalog No. T7013Alias SCH 530348, MK-5348Cas No. 618385-01-6
Vorapaxar (MK-5348) (SCH 530348) is an effective and orally active thrombin receptor (PAR-1) antagonist (Ki: 8.1 nM).
Pack SizePriceAvailabilityQuantity
1 mg$68In Stock
5 mg$148In Stock
10 mg$228In Stock
25 mg$413In Stock
50 mg$618In Stock
100 mg$879In Stock
500 mg$1,750In Stock
1 mL x 10 mM (in DMSO)$163In Stock
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Purity:99.93%
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Product Introduction

Bioactivity
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
Vorapaxar is a synthetic tricyclic 3-phenylpyridine and an orally active himbacine-based thrombin-receptor antagonist. Vorapaxar 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. Vorapaxar also has no affect on the prothrombin time (PT), partial thromboplastin time (PTT), or activated partial thromboplastin time (aPTT). Moreover, Vorapaxar 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
Vorapaxar 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 Vorapaxar 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]
AliasSCH 530348, MK-5348
Chemical Properties
Molecular Weight492.58
FormulaC29H33FN2O4
Cas No.618385-01-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: 92 mg/mL (186.8 mM)
DMSO: 92 mg/mL (186.8 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.0301 mL10.1506 mL20.3013 mL101.5064 mL
5 mM0.4060 mL2.0301 mL4.0603 mL20.3013 mL
10 mM0.2030 mL1.0151 mL2.0301 mL10.1506 mL
20 mM0.1015 mL0.5075 mL1.0151 mL5.0753 mL
50 mM0.0406 mL0.2030 mL0.4060 mL2.0301 mL
100 mM0.0203 mL0.1015 mL0.2030 mL1.0151 mL

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