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 selectivePAR4antagonist peptide. tcY-NH2 TFA 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 TFA (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 TFA potently activates aorta relaxation (RA) and gastric (LM) contraction, with IC50values of 64 μM (RA) and 1 μM (LM)[1]. tcY-NH2 TFA (Tc-YPGKF-NH2, 400 μM, 5 min) prevents endostatin release and platelet aggregation induced by thrombin or by AY-NH2[2]. 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[5].
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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[3]. 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[4]. tcY-NH2 TFA (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 | |
性状 | |
Formula | |
Sequence Shortening | {trans-Cinnamoyl}-YPGKF-NH2 |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Sealed storage, away from moisture Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : 100 mg/mL(117.11 mM;Need ultrasonic) 配制储备液 1 mM | 1.1711 mL | 5.8556 mL | 11.7112 mL | 5 mM | 0.2342 mL | 1.1711 mL | 2.3422 mL | 10 mM | 0.1171 mL | 0.5856 mL | 1.1711 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (2.44 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (2.44 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (2.44 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (2.44 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (2.44 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (2.44 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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