Vorapaxar - CAS 618385-01-6
Catalog number: B0084-458444
Category: Inhibitor
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Molecular Formula:
C29H33FN2O4
Molecular Weight:
492.58
COA:
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Targets:
Protease-Activated Receptors (PARs)
Description:
SCH-530348 is a novel antiplatelet agent undergoing development by Schering-Plough Corp for the treatment and prevention of atherothrombosis. It is currently undergoing Phase-III clinical trials for acute coronary syndrome (unstable angina/non-ST segment elevation myocardial infarction) and secondary prevention of cardiovascular events in high-risk patients.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-458444 10 mg $198 In stock
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Purity:
0.98
Synonyms:
N-[(1R,3aR,4aR,6R,8aR,9S,9aS)-9-[(1E)-2-[5-(3-Fluorophenyl)-2-pyridinyl]ethenyl]dodecahydro-1-methyl-3-oxonaphtho[2,3-c]furan-6-yl]carbamic Acid Ethyl Ester Sulfate; Sch 530348;
MSDS:
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InChIKey:
ZBGXUVOIWDMMJE-QHNZEKIYSA-N
InChI:
InChI=1S/C29H33FN2O4/c1-3-35-29(34)32-23-10-11-24-20(14-23)15-26-27(17(2)36-28(26)33)25(24)12-9-22-8-7-19(16-31-22)18-5-4-6-21(30)13-18/h4-9,12-13,16-17,20,23-27H,3,10-11,14-15H2,1-2H3,(H,32,34)/b12-9+/t17-,20+,23-,24-,25+,26-,27+/m1/s1
Canonical SMILES:
CCOC(=O)NC1CCC2C(C1)CC3C(C2C=CC4=NC=C(C=C4)C5=CC(=CC=C5)F)C(OC3=O)C
1.Synthesis of novel and potent vorapaxar analogues.
Knight E1, Robinson E1, Smoktunowicz N2, Chambers RC2, Aliev AE1, Inglis GG3, Chudasama V1, Caddick S1. Org Biomol Chem. 2016 Mar 15;14(12):3264-74. doi: 10.1039/c5ob02541a.
Vorapaxar is a first-in-class PAR-1 antagonistic drug based on the ent-himbacine scaffold. Detailed in this article are enantioselective and racemic routes to various novel vorapaxar analogues. Biological testing revealed these compounds to have moderate to excellent potencies against PAR-1 with the most potent analogue demonstrating an IC50 of 27 nM.
2.Use of thienopyridine prior to presentation with non-ST-segment elevation acute coronary syndrome and association with safety and efficacy of vorapaxar: insights from the TRACER trial.
Harskamp RE1, Clare RM2, Ambrosio G3, Held C4, Lokhnygina Y2, Moliterno DJ5, White HD6, Aylward PE7, Armstrong PW8, Mahaffey KW9, Harrington RA9, Van de Werf F10, Wallentin L4, Strony J11, Tricoci P12. Eur Heart J Acute Cardiovasc Care. 2016 Feb 19. pii: 2048872616633880. [Epub ahead of print]
BACKGROUND: Vorapaxar is effective in the prevention of secondary atherothrombotic events, although the efficacy/safety balance appears less favorable in the treatment of patients with non-ST-segment elevation (NSTE) acute coronary syndrome (ACS). We hypothesized that patients with NSTE ACS already receiving thienopyridine prior to the ACS event may show differential efficacy/safety effects with vorapaxar vs. placebo added to their standard care.
3.Efficacy and safety of vorapaxar for the prevention of adverse cardiac events in patients with coronary artery disease: a meta-analysis.
Tan G1, Chen J1, Liu M1, Yeh J1, Tang W1, Ke J1, Wu W1. Cardiovasc Diagn Ther. 2016 Apr;6(2):101-8. doi: 10.21037/cdt.2015.12.04.
BACKGROUND: Coronary artery disease (CAD) is the leading cause of morbidity and mortality worldwide. Vorapaxar, a protease-activated receptor-1 (PAR-1) antagonist, is a novel antiplatelet agent that may provide us a new way in antithrombotic therapy. Several studies had been conducted to evaluate the efficacy of vorapaxar in the treatment of CAD, but the results were inconsistent. Here a meta-analysis was made to assess the efficacy and safety of vorapaxar in reducing adverse cardiac events in patients with CAD.
4.Continued vorapaxar versus withdrawed clopidogrel both on top of low dose aspirin in patients undergoing heart surgery: A call for randomized trial.
Serebruany VL1, Kim MH2, Golukhova E3, Pya Y4, Bekbossynova M4, Cattaneo M5, Marciniak TA6. Int J Cardiol. 2016 Apr 17;215:273-276. doi: 10.1016/j.ijcard.2016.04.124. [Epub ahead of print]
Despite advanced techniques and improved clinical outcomes, the optimal antiplatelet strategy following coronary artery bypass grafting (CABG) is an unsolved mystery. Vorapaxar, a novel platelet thrombin receptor (PAR-1/4) blocker, is currently approved for post-myocardial infarction and peripheral artery disease indications on top of clopidogrel or/and aspirin. We here summarize the outcomes in patients after CABG for justification of a future vorapaxar trial. We comprehended the CABG outcomes after vorapaxar yielded from TRACER, TRA2P trials, and affiliated FDA reviews. The verified evidence suggests that composite of death, myocardial infarction and stroke occurred in 2.2% of vorapaxar vs. 8.1% placebo in TRA2P. These data were similar to the endpoint differences (5.9% after vorapaxar vs. 8.3% for placebo) in TRACER. The mortality reduction also consistently suggests vorapaxar advantage (1.7% vs. 2.5% in TRA2P, and 1.7% vs. 3.9% in TRACER).
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CAS 618385-01-6 Vorapaxar

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