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Merck
CN

A3227

Sigma-Aldrich

Ala-Tyr-Pro-Gly-Lys-Phe-NH2 三氟乙酸盐

≥98% (HPLC), lyophilized powder, PAR4 agonist

别名:

AYPGKF-NH2, PAR4-AP

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About This Item

经验公式(希尔记法):
C34H48N8O7 · xC2HF3O2
分子量:
680.79 (free base basis)
MDL编号:
UNSPSC代码:
12352202
PubChem化学物质编号:
NACRES:
NA.77

product name

Ala-Tyr-Pro-Gly-Lys-Phe-NH2 三氟乙酸盐, ≥98% (HPLC), lyophilized powder

质量水平

检测方案

≥98% (HPLC)

形式

lyophilized powder

颜色

white

溶解性

H2O: >10 mg/mL

储存温度

−20°C

SMILES字符串

OC(=O)C(F)(F)F.C[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2CCCC2C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc3ccccc3)C(N)=O

InChI

1S/C34H48N8O7.C2HF3O2/c1-21(36)31(46)41-27(19-23-12-14-24(43)15-13-23)34(49)42-17-7-11-28(42)33(48)38-20-29(44)39-25(10-5-6-16-35)32(47)40-26(30(37)45)18-22-8-3-2-4-9-22;3-2(4,5)1(6)7/h2-4,8-9,12-15,21,25-28,43H,5-7,10-11,16-20,35-36H2,1H3,(H2,37,45)(H,38,48)(H,39,44)(H,40,47)(H,41,46);(H,6,7)/t21-,25-,26-,27-,28-;/m0./s1

InChI key

BGPJLFVICWHITH-HKJXYENISA-N

Amino Acid Sequence

Ala-Tyr-Pro-Gly-Lys-Phe-NH2

一般描述

Ala-Tyr-Pro-Gly-Lys-Phe-NH2(AYPGKF- NH2)是一种选择性,特异性蛋白酶激活受体4(PAR4)激动剂肽。 PAR4是一种G蛋白偶联受体,表达于人血小板表面,参与凝血酶信号通路。 蛋白酶凝血酶对PAR4的切割会刺激受体,并导致血小板聚集的信号传导。

应用

4-雄甾烯-11-β醇-3,17-二酮已用于血小板聚集。
AYPGKF-NH2可用于探测培养系统和血小板中的PAR4信号传导。

生化/生理作用

AYPGK是PAR4受体的配体;结合导致PAR4的激活。 AYPGK通过PAR4刺激体外血小板聚集(EC50=15 μM)。 在用PAR4激动剂处理的人血小板中,AYPGKF刺激血栓烷的产生,血栓烷是一种有效的血小板聚集剂。 此外,AYPGKF介导凝血酶诱导的内皮抑素从大鼠血小板释放。

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

Eyeshields, Gloves, type N95 (US)


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Essentials Spatiotemporal regulation of protein kinases during thrombus formation remains elusive in vivo. Activities of protein kinases were live imaged in mouse platelets at laser-ablated arterioles. Protein kinase A was activated in the dislodging platelets at the downstream side of
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Human platelets display a unique dual receptor system for responding to its primary endogenous activator, α-thrombin. Because of the lack of efficacious antagonists, the field has relied on synthetic peptides and pepducins to describe protease-activated receptor PAR1 and PAR4 signaling.

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