Atopaxar

Atopaxar Chemische Eigenschaften,Einsatz,Produktion Methoden

• Definition

  ChEBI: Atopaxar is an aromatic ketone.

• Biologische Aktivität

  Atopaxar (E5555) is a potent, orally active, selective, reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. It can be used in the study of atherothrombotic diseases and interferes with platelet signaling..

• in vitro

  Atopaxar inhibits haTRAP (high-affinity thrombin receptor activating peptide) binding to PAR-1 on human platelet membranes in a concentration-dependent manner, with an IC ₅₀ of 0.019 μM. < br/> Atopaxar inhibits human platelet aggregation induced by thrombin or TRAP in a concentration-dependent manner.
  Atopaxar does not inhibit PRP (platelet-rich plasma) aggregation induced by ADP, U46619, collagen, and PAR-4ap, up to a concentration of 20 μM.
  

• in vivo

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

  < td class="col1 fwb"> Result:

  Animal Model:	Guinea pigs, PIT model
  Dosage:	Oral administration
  Administration:	10 mg/kg, 30 mg/kg, 100 mg/kg
  Prolonged the time to occlusion by 1.8-fold and 2.4-fold at 30 mg/kg and 100 mg/kg, respectively, compared with controls.

• target

  PAR-1

Atopaxar Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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