Prasugrel

Catalog No.S1258 Synonyms: CS-747, LY640315

Prasugrel Chemical Structure

Molecular Weight(MW): 373.44

Prasugrel is a thienopyridine ADP receptor (P2Y12) antagonist, used for the reduction of thrombotic cardiovascular events.

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Biological Activity

Description Prasugrel is a thienopyridine ADP receptor (P2Y12) antagonist, used for the reduction of thrombotic cardiovascular events.
Targets
P2Y12 receptor [1]
In vitro

Prasugrel is a novel orally active thienopyridine with faster, higher and more reliable inhibition of platelet aggregation than clopidogrel reflecting its metabolism in vivo to an active metabolite with selective P2Y(12) antagonistic activity. [1]

In vivo Prasugrel shows platelet inhibition that was 8.2 times more potent than clopidogrel in WT mice. [1] Prasugrel (3 and 10 mg/kg) dose-relatedly and significantly reduces thrombus-mediated cerebral infarction 24 hours after the irradiation in rat models of cerebral and peripheral arterial occlusive diseases. Prasugrel (0.3-3 mg/kg) reduces incidence, total area, and total number of cerebral infarcts in a dose-related manner 24 hours after the vascular injury in an embolic infarction rats model. Prasugrel (0.03-3 mg/kg/day) administered from the day before the lauric acid injection for 11 successive days inhibits the progression of the disease in a dose-related manner in rats with lauric acid-induced peripheral arterial occlusive diseases. [2] Prasugrel administrated in dogs (0.03-0.3 mg/kg/day) and monkeys (0.1 and 0.3 mg/kg/day) once a day for 14 days results in potent, dose-related and cumulative inhibition of ADP-induced platelet aggregation. Prasugrel (0.1-1 mg/kg/day, p.o.) significantly prolongs the time to arterial occlusion and increases the duration of arterial patency in a rat model of electrically-induced arterial thrombosis. [3]

Protocol

Solubility (25°C)

In vitro DMSO 30 mg/mL (80.33 mM)
Ethanol 7 mg/mL (18.74 mM)
Water Insoluble

* 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.

Chemical Information

Molecular Weight 373.44
Formula

C20H20FNO3S

CAS No. 150322-43-3
Storage powder
Synonyms CS-747, LY640315

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03027934 Not yet recruiting Diabetes Mellitus CirQuest Labs, LLC February 28, 2017 Phase 4
NCT02978040 Not yet recruiting Coronary Artery Disease|STEMI - ST Elevation Myocardial Infarction University Hospital Inselspital, Berne February 2017 Phase 4
NCT03016611 Not yet recruiting Acute Coronary Syndrome|STEMI Sheba Medical Center February 2017 Phase 4
NCT02866175 Not yet recruiting Atrial Fibrillation Daiichi Sankyo Inc.|European Cardiovascular Research Institute|Kompetenznetz Vorhofflimmern e.V.|Chiltern International Inc. February 2017 Phase 3
NCT02944123 Recruiting Acute Coronary Syndrome Dong-A University September 2016 Phase 3
NCT02507323 Withdrawn Cardiovascular Disease Yochai Birnbaum|AstraZeneca|Baylor College of Medicine February 2016 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID