Catalog No.S8067 Synonyms: SCH 530348, MK-5348
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.
Purity & Quality Control
Choose Selective Protease-activated Receptor Inhibitors
|Description||Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.|
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. 
|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. |
|In vitro||DMSO||99 mg/mL (200.98 mM)|
|Ethanol||99 mg/mL (200.98 mM)|
* 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.
|Synonyms||SCH 530348, MK-5348|
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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|
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.