tcY-NH2 TFA (Synonyms: (trans-Cinnamoyl)-YPGKF-NH2 TFA)
目录号: PL10693 纯度: ≥99%
CAS No. :1262750-73-1
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中文名称
tcY-NH2 TFA
英文名称
tcY-NH2 TFA
英文别名
MS-31577;tcY-NH2 (TFA);CS-0131874;TP1925L;WQJKBSZTPQERHW-USBDLMLUSA-N;tcY-NH2 TFA;G13305;1262750-73-1;DTXSID80746616;(2S)-N-[2-[[(2S)-6-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]-1-[(2S)-3-(4-hydroxyphenyl)-2-[[(E)-3-phenylprop-2-enoyl]amino]propanoyl]pyrrolidine-2-carboxamide;2,2,2-trifluoroacetic acid;tcY-NH2 TFA(327177-34-4 free base);AKOS040764144;HY-P1263A;Trifluoroacetic acid--N-[(2E)-3-phenylprop-2-enoyl]-L-tyrosyl-L-prolylglycyl-L-lysyl-L-phenylalaninamide (1/1)
Cas No.
1262750-73-1
分子式
C42H50F3N7O9
分子量
853.88
包装储存
Sealed storage, away from moisturePowder -80°C 2 years;-20°C 1 year
产品详情
tcY-NH2 ((trans-Cinnamoyl)-YPGKF-NH2) TFA 是一种有效的 PAR4 选择性肽类拮抗剂。tcY-NH2 TFA 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) 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
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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