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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
¥ 2,925.00
Ship with 10-15 days

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A

背景

AY-NH2是PAR4的选择性激动剂,EC50值为11 μM [1].

蛋白酶活化受体-4(PAR4)是PARs的成员,通过作用于G蛋白i\12/13(Rho和Ras活化)和q(钙信号),从而在介导凝血酶的细胞效应中起重要作用[2].

AY-NH2是高效的PAR4激动剂,比GYPGKF-NH2具有更高(约10倍)的活性.大鼠血小板凝集实验表明,AY-NH2比GY-NH2和GF-NH2具有更高的血小板凝集能力[1].野生型C57BL6小鼠分离出的富含血小板的血浆实验中,AY-NH2处理对PAR4表现出较高的激动活性,而对其它PARs没有作用[3].

在雄性Wistar大鼠足肿胀模型中,腹腔注射AY-NH2在响应毒性与非毒性机械刺激时能显著降低感受伤害评分,从而抑制角叉菜胶诱导的机械痛觉过敏和异常性疼痛[4].

参考文献:
[1].  Hollenberg, M.D., et al., Proteinase-activated receptor-4: evaluation of tethered ligandderived 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.

化学属性

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
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化学结构

AY-NH2