耗材描述
tcY-NH2
产品活性:tcY-NH2 ((trans-Cinnamoyl)-YPGKF-NH2) 是一种有效的 PAR4 选择性肽类拮抗剂。tcY-NH2 抑制凝血酶和 AY-NH2 诱导的血小板聚集和内皮抑素释放,可用于炎症、免疫学的研究。
产品来源: https://www.medchemexpress.cn/tcy-nh2.html
研究领域:GPCR/G Protein
作用靶点:Protease Activated Receptor (PAR)
In Vitro: tcY-NH2 (0-500 μM) inhibits AYPGKF-NH2 (10 μM)-induced platelet (obtained from male albino Sprague–Dawley rats) aggregation, with an IC50 value of 95 μM.
tcY-NH2 potently activates aorta relaxation (RA) and gastric (LM) contraction, with IC50 values of 64 μM (RA) and 1 μM (LM).
tcY-NH2 (Tc-YPGKF-NH2, 400 μM, 5 min) prevents endostatin release and platelet aggregation induced by thrombin or by AY-NH2.
tcY-NH2 (5 μM, 15 min) decreases infarct size (IS) by 51%, and increases recovery of ventricular function by 26% in an isolated heart model.
In Vivo: tcY-NH2 (tail vein injection, 0.6 mg/kg for a single dose) alleviates liver injury in Brain death (BD) rat model, indicated by lower serum ALT/AST levels and better histomorphology.
tcY-NH2 (intraperitoneal injection, 0.6 mg/kg for a single dose) increases posttraumatic activation of CD4+ Tregs within the draining lymph nodes in burn injury mice model .
tcY-NH2 (intrapleural injection, 40 ng/kg for a single dose) inhibits neutrophil recruitment in experimental inflammation in mice.
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