tcY-NH2 ((trans-Cinnamoyl)-YPGKF-NH2) TFA is a potent selective PAR4 antagonist peptide. tcY-NH2 TFA inhibits thrombin- and AY-NH 2 -induced platelet aggregation and endostatin release, and can be used in the research of inflammation, immunology.
性状
Solid
IC50 & Target[1][2]
PAR4
体外研究(In Vitro)
tcY-NH2 TFA (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 TFA potently activates aorta relaxation (RA) and gastric (LM) contraction, with IC50 values of 64 μM (RA) and 1 μM (LM).tcY-NH2 TFA (Tc-YPGKF-NH2, 400 μM, 5 min) prevents endostatin release and platelet aggregation induced by thrombin or by AY-NH2.tcY-NH2 TFA (5 μM, 15 min) decreases infarct size (IS) by 51%, and increases recovery of ventricular function by 26% in an isolated heart model. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
tcY-NH2 TFA (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 TFA (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 TFA (intrapleural injection, 40 ng/kg for a single dose) inhibits neutrophil recruitment in experimental inflammation in mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisturePowder -80°C 2 years;-20°C 1 year
SequenceShortening
{trans-Cinnamoyl}-YPGKF-NH2
参考文献
[1]. Morley D Hollenberg, et al. Proteinase-activated receptor-4: evaluation of tethered ligand-derived peptides as probes for receptor function and as inflammatory agonists in vivo. Br J Pharmacol. 2004 Oct;143(4):443-54.[2]. L Ma, et al. Thrombin-induced platelet endostatin release is blocked by a proteinase activated receptor-4 (PAR4) antagonist. Br J Pharmacol. 2001 Oct;134(4):701-4.
溶解度数据
In Vitro: DMSO : 100 mg/mL (117.11 mM; Need ultrasonic)配制储备液