Atopaxar (E5555) hydrobromide is a potent, orally active, selective and reversiblethrombinreceptorprotease-activated receptor-1 (PAR-1)antagonist. Atopaxar hydrobromide, an antiplatelet agent, interferes with platelet signaling. Atopaxar hydrobromide can be used for the research of atherothrombotic disease^[1][2].

PAR-1^[1]

Atopaxar hydrobromide (0.0001-10 μM; 1h) inhibits haTRAP (high-affinity thrombin receptor activating peptide) binding to PAR-1 on human platelet membranes in a concentration-dependent manner, with an IC₅₀of 0.019 μM^[2].
Atopaxar hydrobromide shows potent inhibitory effects on human platelet aggregation induced by thrombin and TRAP with IC₅₀s of 0.064 and 0.031 μM, respectively, but has no effect on platelet aggregation induced by either ADP or collagen^[2].
Atopaxar hydrobromide shows potent and selective inhibitory effects on guinea pig platelet aggregation induced by thrombin and TRAP with IC₅₀s of 0.13 and 0.097 μM, respectively^[2].

Atopaxar (30-100 mg/kg; p.o.) hydrobromide causes a dose-dependent prolongation of the time to occlusion of the femoral artery in photochemically-induced thrombosis (PIT) guinea pigs model^[2].
Atopaxar hydrobromide does not prolong bleeding time in guinea pigs at the highest tested dosage of 1000 mg/kg^[2].

608.54

C₂₉H₃₉BrFN₃O₅

474550-69-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• 1.

  Atopaxar hydrobromide (E5555) is prepared in the 0.5% methylcellulose solution^[2].