| CAS NO: | 916170-19-9 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 518.36 |
| Cas No. | 916170-19-9 |
| Formula | C25H20BrN5O3 |
| Solubility | Soluble in DMSO |
| Chemical Name | (E)-N-(2-(2-(1-(3-bromophenyl)ethylidene)hydrazinyl)-2-oxo-1-(4-oxo-3,4-dihydrophthalazin-1-yl)ethyl)benzamide |
| Canonical SMILES | O=C1C2=CC=CC=C2C(C(NC(C3=CC=CC=C3)=O)C(N/N=C(C)/C4=CC=CC(Br)=C4)=O)=NN1 |
| 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。 |
AC 55541是高效的PAR2激动剂,pEC50值为6.7,功能范围从200-1000 nM [1-3].
蛋白酶活化受体2(PAR2)是7跨膜受体大家族的成员,在调节炎症反应中起重要作用,并在感染期间作为蛋白水解酶类产生的感受器[2].
AC 55541是选择性PAR2激动剂,对PAR1没有作用.细胞增殖实验(R-SAT)表明AC 55541通过活化PAR2从而刺激NIH-3T3细胞增殖.所有功能试验中,F240S突变组成型活化的受体对AC 55541的敏感度要高于SLIGRL和2-furorl LIGRLO近30倍[1, 2].在人角膜上皮(HCE)细胞中,给予AC 55541能显著诱导PAR2表达,并抑制棘阿米巴纤溶酶原激活物(APA)[3].
在SLIGRL-NH2或胰蛋白酶诱导的急性热伤害和足肿胀雄性SD大鼠模型中,足内给予低至30 ng的AC 55541能够诱导后趾水肿和热痛觉过敏,并表现出剂量依赖性促疼痛效应[1].
参考文献：
1. Gardell, L.R., et al., Identification and characterization of novel small-molecule proteaseactivated receptor 2 agonists. J Pharmacol Exp Ther, 2008. 327(3): p. 799-808.
2. Ma, J.N. and E.S. Burstein, The protease activated receptor 2 (PAR2) polymorphic variant F240S constitutively activates PAR2 receptors and potentiates responses to small-molecule PAR2 agonists. J Pharmacol Exp Ther, 2013. 347(3): p. 697-704.
3. Tripathi, T., M. Abdi, and H. Alizadeh, Protease-activated receptor 2 (PAR2) is upregulated by Acanthamoeba plasminogen activator (aPA) and induces proinflammatory cytokine in human corneal epithelial cells. Invest Ophthalmol Vis Sci, 2014. 55(6): p. 3912-21.
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