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编 号：F364342
分子式：C29H39BrFN3O5
分子量：608.54
分子式：C29H39BrFN3O5
分子量：608.54
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CAS No: 474550-69-1
产品详情
生物活性：
Atopaxar (E5555) hydrobromide is a potent, orally active, selective and reversible thrombin receptor protease-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.
体内研究：
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. Atopaxar hydrobromide does not prolong bleeding time in guinea pigs at the highest tested dosage of 1000 mg/kg.Animal Model:Guinea pigs, PIT model
Dosage:Oral administration
Administration:10 mg/kg, 30 mg/kg, 100 mg/kg
Result: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.
体外研究：
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 IC50 of 0.019 μM.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.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.
Atopaxar (E5555) hydrobromide is a potent, orally active, selective and reversible thrombin receptor protease-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.
体内研究：
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. Atopaxar hydrobromide does not prolong bleeding time in guinea pigs at the highest tested dosage of 1000 mg/kg.Animal Model:Guinea pigs, PIT model
Dosage:Oral administration
Administration:10 mg/kg, 30 mg/kg, 100 mg/kg
Result: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.
体外研究：
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 IC50 of 0.019 μM.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.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.
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