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Catalog No.
PAR-1 antagonist,potent and orally active
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
In stock
Evaluation Sample
In stock
In stock
In stock
In stock
In stock

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Vorapaxar is a potent PAR1 inhibitor and antiplatelet that was completed in phase III clinical trial[1].

PAR1 is one of the 4 thrombin receptor types that belong to G-protein coupled receptors super family[1]. By binding to thrombin, the N-terminal at the arginine 41 and serine 42 bond of PAR1 on platelet surface can be enzymatically cleaved, resulting in the activation of platelet and subsequent hemostasis process[1].

Vorapaxar is an ethyl-carbamate molecule that derived from natural himbacine and has been determined to be a selective PAR 1 inhibitor through direct binding[2]. In human plasma enriched with platelets, Vorapaxar was able to inhibit the aggregation of platelet with an IC50 value of 47 nM[2]. In addition, vorapaxar is able to inhibitthe platelet aggregation that triggered by the addition of thrombin receptor activating peptide with an IC50 value of 25 nM[2]. At the same time, however, vorapaxar does not interfere thrombin’s enzymatic activity on fibrin formation or thromboxane A2 receptors-induced platelet aggregation, as was demonstrated by its inability to inhibit platelet aggregation that induced by the addition of 9,11-dideoxy-11R,9R-epoxymethanoprostaglandin F2R (a thromboxane mimetic) [1].

In vivo, oral administration of 0.1 mg/kg of Vorapaxar completely inhibited the platelet aggregation monkey model for 24 hrs. In phase III clinical trial that involved 26,449 patients [1], administration of vorapaxar (2.5 mg/day) reduced the occurrence of cardiovascular death or ischemic events compared with placebo group by a statistically significant 1.2%[1].

[1].  Chackalamannil S & XIA, Y. Thrombin receptor (PAR-1) antagonists as novel antithrombotic agents. Expert Opinion on Therapeutic Patents, 2006.16:493-505.
[2].  Chackalamannil S, Wang Y, Greenlee W J et al. 2008. Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity. J Med Chem, 2008,51: 3061-3064.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.618385-01-6
Solubility≥24.65mg/mL in DMSO
Chemical Nameethyl N-[(1R,3aR,4aR,6R,8aR,9S,9aS)-9-[(E)-2-[5-(3-fluorophenyl)pyridin-2-yl]ethenyl]-1-methyl-3-oxo-3a,4,4a,5,6,7,8,8a,9,9a-decahydro-1H-benzo[f][2]benzofuran-6-yl]carbamate
SDFDownload SDF
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description Vorapaxar (SCH 530348) is a potent and orally active antagonist of thrombin receptor (PAR-1) with a Ki value of 8.1 nM.
Targets PAR-1          
IC50 8.1 nM (Ki)          

Quality Control

Chemical structure