tcY-NH2 TFA (trans-Cinnamoyl-YPGKF-NH2 TFA)|cas:1262750-73-1|西域试剂

tcY-NH2 TFA (trans-Cinnamoyl-YPGKF-NH2 TFA),99.84%

产品编号：Bellancom-P1263A| CAS NO：1262750-73-1| 分子式：C₄₂H₅₀F₃N₇O₉| 分子量：853.88

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-P1263A		￥2000.00	杭州北京（现货）
Bellancom-P1263A		￥5800.00	杭州北京（现货）

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tcY-NH2 TFA (trans-Cinnamoyl-YPGKF-NH2 TFA)

产品介绍

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-NH₂-induced platelet aggregation and endostatin release, and can be used in the research of inflammation, immunology^[6].

体外研究

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^[5].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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 ^[4].
tcY-NH2 TFA (intrapleural injection, 40 ng/kg for a single dose) inhibits neutrophil recruitment in experimental inflammation in mice^[6].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Brain death (BD) rat model
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Brain death (BD) rat model
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (117.11 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。