| CAS NO: | 352017-71-1 |
| 包装: | 1mg |
| 市场价: | 1740元 |
| Physical Appearance | White lyophilised solid |
| Storage | Desiccate at -20°C |
| M.Wt | 680.8 |
| Cas No. | 352017-71-1 |
| Formula | C34H48N8O7 |
| Solubility | Soluble 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 |
| Canonical SMILES | C[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 | 蓝冰运输或根据您的需求运输。 |
| 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。溶液形式一般不宜长期储存，请尽快用完。 |
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.
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