Atopaxar


CAS No. : 751475-53-3

(Synonyms: E5555; ER-172594-00)

751475-53-3
Price and Availability of CAS No. : 751475-53-3
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Cat. No. : HY-18200
M.Wt: 527.63
Formula: C29H38FN3O5
Purity: >98 %
Solubility: DMSO : 50 mg/mL (ultrasonic)
Introduction of 751475-53-3 :

Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar, an antiplatelet agent, interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease[1][2]. IC50 & Target:PAR-1[1] In Vitro: Atopaxar (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 IC50 of 0.019 μM[2].
Atopaxar inhibits human platelet aggregation induced by thrombin or TRAP in a concentration-dependent manner[2].
Atopaxar does not inhibit PRP (platelet-rich plasma) aggregation induced by ADP, U46619, collagen, and PAR-4ap, up to a concentration of 20 μM[2].
In Vivo: Atopaxar (30-100 mg/kg; p.o.) causes a dose-dependent prolongation of the time to occlusion of the femoral artery in photochemically-induced thrombosis (PIT) guinea pigs model[2].
Atopaxar does not prolong bleeding time in guinea pigs at the highest tested dosage of 1000 mg/kg[2].

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