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。
| 生物活性 | tcY-NH2 ((trans-Cinnamoyl)-YPGKF-NH2) is a potent selectivePAR4antagonist peptide. tcY-NH2 inhibits thrombin- and AY-NH2-induced platelet aggregation and endostatin release, and can be used in the research of inflammation, immunology[1][2][6]. |
体外研究
(In Vitro) | tcY-NH2 (0-500 μM) inhibits AYPGKF-NH2(10 μM)-induced platelet (obtained from male albino Sprague–Dawley rats) aggregation, with an IC50value of 95 μM[1].
tcY-NH2 potently activates aorta relaxation (RA) and gastric (LM) contraction, with IC50values of 64 μM (RA) and 1 μM (LM)[1].
tcY-NH2 (Tc-YPGKF-NH2, 400 μM, 5 min) prevents endostatin release and platelet aggregation induced by thrombin or by AY-NH2[2].
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[5].
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体内研究
(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[3].
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[4].
tcY-NH2 (intrapleural injection, 40 ng/kg for a single dose) inhibits neutrophil recruitment in experimental inflammation in mice[6].
| Animal Model: | Brain death (BD) rat model[3] | | Dosage: | 0.6 mg/kg for a single dose | | Administration: | Tail vein injection for a single dose | | Result: | Reduced blood platelet activation and hepatic platelet accumulation.
Attenuated the inflammatory response and apoptosis in the livers.
Inhibited the activation of NF-κB and MAPK pathways induced by Brain death (BD). |
| Animal Model: | Burn injury model of C57BL/6 N mice[4] | | Dosage: | 0.6 mg/kg for a single dose | | Administration: | Intraperitoneal injection | | Result: | Increased expression and phosphorylation of PKC-θ in the presence of platelets, without affecting early posttraumatic hemostasis. |
| Animal Model: | BALB/c mice[6] | | Dosage: | 40 ng/kg for a single dose | | Administration: | Intrapleural injection | | Result: | Abolished the number of rolling and adhering neutrophils on the vessel wall.
Inhibited CXCL8- and Cg-induced neutrophil migration into the pleural cavity of mice. |
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| 分子量 | |
| Formula | |
| CAS 号 | |
| Sequence Shortening | {trans-Cinnamoyl}-YPGKF-NH2 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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