AC 55541
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
| 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 |
| SDF | Download SDF |
| 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 | 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。 |
化学结构
