切换导航

AY-NH2

Catalog No.
A8667
PAR4激动剂
组合的产品项目
规格价格库存 数量
1mg
¥ 1,320.00
Ship with 10-15 days
5mg
¥ 3,960.00
Ship with 10-15 days
10mg
¥ 6,360.00
Ship with 10-15 days

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

AY-NH2 is a selective agonist of PAR4 with EC50 value of 11 μM [1].

Protease-activated receptor-4 (PAR4) is a member of PARs and plays an important role in mediating cellular effects of thrombin through acting G-proteins i, 12/13 (Rho and Ras activation) and q (calcium signaling) [2].

AY-NH2 is a potent PAR4 agonist and has a higher (~10 fold) activity than GYPGKF-NH2. Using rat platelet aggregation assay, it was shown that AY-NH2 had highly platelet aggregation ability than GY-NH2 and GF-NH2 [1]. When tested with platelet-rich plasma harvested from wild-type C57BL6 mice, AY-NH2 treatment exhibited highly agonist activity on PAR4 while had no effect on other PARs [3].

In male Wistar rats model of paw oedema, i.pl. injection of AY-NH2 markedly reduced the nociceptive score in response to both noxious and non-noxious mechanical stimuli, thus inhibiting carrageenan-induced mechanical hyperalgesia and allodynia [4].

References:
[1].  Hollenberg, M.D., 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. 143(4): p. 443-54.
[2].  Yu, G., et al., Increased expression of protease-activated receptor 4 and Trefoil factor 2 in human colorectal cancer. PLoS One, 2015. 10(4): p. e0122678.
[3].  Faruqi, T.R., et al., Structure-function analysis of protease-activated receptor 4 tethered ligand peptides. Determinants of specificity and utility in assays of receptor function. J Biol Chem, 2000. 275(26): p. 19728-34.
[4].   Asfaha, S., et al., Protease-activated receptor-4: a novel mechanism of inflammatory pain modulation. Br J Pharmacol, 2007. 150(2): p. 176-85.

Chemical Properties

Physical AppearanceWhite lyophilised solid
StorageDesiccate at -20°C
M.Wt680.8
Cas No.352017-71-1
FormulaC34H48N8O7
SolubilitySoluble in H2O
Chemical Name(S,Z)-N-((Z)-2-(((S,Z)-6-amino-1-hydroxy-1-(((S)-1-hydroxy-1-imino-3-phenylpropan-2-yl)imino)hexan-2-yl)imino)-2-hydroxyethyl)-1-((S)-2-((Z)-((S)-2-amino-1-hydroxypropylidene)amino)-3-(4-hydroxyphenyl)propanoyl)pyrrolidine-2-carbimidic acid
SDFDownload SDF
Canonical SMILESC[C@@](N)([H])/C(O)=N/[C@@](C(N1CCC[C@@]1([H])/C(O)=N/C/C(O)=N/[C@@](/C(O)=N/[C@@](C(O)=N)([H])CC2=CC=CC=C2)([H])CCCCN)=O)([H])CC3=CC=C(O)C=C3
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议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。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

质量控制和MSDS

批次:

化学结构

AY-NH2