Atopaxar
Names
Biological Activity
[Description]:
Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease[1][2].
[Related Catalog]:
[Target]
PAR-1[1]
[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 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.) prolongs the time to occlusion by 1.8-fold and 2.4-fold, respectively, compared with controls[2]. Atopaxar does not prolong bleeding time in guinea pigs at the highest tested dosage of 1000 mg/kg[2]. Animal Model: Guinea pigs, photo-chemically-induced thrombosis (PIT) model[2] Dosage: Oral administration Administration: 10 mg/kg, 30 mg/kg, 100 mg/kg Result: At 30 and 100 mg/kg prolonged the time to occlusion by 1.8-fold and 2.4-fold, respectively, compared with controls.
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C29H38FN3O5
[ Molecular Weight ]:
527.62800
[ Exact Mass ]:
527.28000
[ PSA ]:
84.32000
[ LogP ]:
4.89230