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更新時間:2025/6/13 16:59:32關(guān)注度:1322
關(guān)鍵詞標(biāo)簽:E5555 hydrobromide
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CAS No. : 474550-69-1
MCE 國際站:Atopaxar hydrobromide
產(chǎn)品活性:Atopaxar (E5555) hydrobromide 是一種高效、有口服活性活性的,選擇性的,可逆的凝血酶受體蛋白酶激活受體-1 (PAR-1) 拮抗劑。Atopaxar hydrobromide 是一種抗血小板劑,能干擾血小板信號。Atopaxar hydrobromide 可用于動脈粥樣硬化血栓性疾病的研究。
研究領(lǐng)域:GPCR/G Protein
作用靶點(diǎn):Protease-Activated Receptor (PAR)
In Vitro: 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 inhibits human platelet aggregation induced by thrombin or TRAP in a concentration-dependent manner.
Atopaxar hydrobromide 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; 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.
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