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Key Documents

A3227

Sigma-Aldrich

Ala-Tyr-Pro-Gly-Lys-Phe-NH2 三氟乙酸盐

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

同義詞:

AYPGKF-NH2, PAR4-AP

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About This Item

經驗公式(希爾表示法):
C34H48N8O7 · xC2HF3O2
CAS號碼:
分子量::
680.79 (free base basis)
MDL號碼:
分類程式碼代碼:
12352202
PubChem物質ID:
NACRES:
NA.77

product name

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

化驗

≥98% (HPLC)

形狀

lyophilized powder

顏色

white

溶解度

H2O: >10 mg/mL

儲存溫度

−20°C

SMILES 字串

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 密鑰

BGPJLFVICWHITH-HKJXYENISA-N

Amino Acid Sequence

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

一般說明

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。

應用

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。

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

Eyeshields, Gloves, type N95 (US)


分析證明 (COA)

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Frederic Lagarrigue et al.
Blood, 136(10), 1180-1190 (2020-06-11)
Ras-related protein 1 (Rap1) is a major convergence point of the platelet-signaling pathways that result in talin-1 binding to the integrin β cytoplasmic domain and consequent integrin activation, platelet aggregation, and effective hemostasis. The nature of the connection between Rap1
Hongyao Xu et al.
The American journal of sports medicine, 48(1), 197-209 (2019-11-26)
Meniscal injury is very common, and injured meniscal tissue has a limited healing ability because of poor vascularity. Platelets contain both pro- and anti-angiogenic factors, which can be released by platelet selective activation. Platelets release a high level of vascular
Seema Bhatlekar et al.
Haematologica, 104(10), 2075-2083 (2019-02-09)
Apoptosis is a recognized limitation to generating large numbers of megakaryocytes in culture. The genes responsible have been rigorously studied in vivo in mice, but are poorly characterized in human culture systems. As CD34-positive (+) cells isolated from human umbilical
Ruth Ann Henriksen et al.
Arteriosclerosis, thrombosis, and vascular biology, 22(5), 861-866 (2002-05-15)
Previous reports have indicated that thrombin-induced thromboxane production by human platelets occurs through two types of interaction between thrombin and the platelet surface. One of these interactions is with protease activated receptor(PAR)-1, the first identified thrombin receptor. These studies were
Matthew T Duvernay et al.
Molecular pharmacology, 91(1), 39-47 (2016-10-28)
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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