货号 | 19085-500ug |
描述 | Prostaglandin E2(PGE2; Item No. 14010) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor that has diverse roles, including those in cancer, inflammation, and neuroprotection.1,2,3 TG6-129 is an antagonist of the EP2 receptor, suppressing PGE2-induced elevation of cAMP in cells expressing EP2 with an IC50 value of 1.6 µM.4 It is without effect on EP4, DP1, IP, and β2-adrenergic receptors. TG6-129 reduces the expression of COX-2, IL-1β, IL-12, IL-23, IL-6, and TNF-α induced by the EP2-selective agonist butaprost (Item No. 13740) in P388D1 macrophages.4 It has low cell cytotoxicity (CC50 = 326 µM), prolonged plasma half-life, and does not cross the blood-brain barrier.4 |
别名 | SID 17503974; |
供应商 | Cayman |
应用文献 | |
1.Majima, M.,Amano, H., and Hayashi, I. Prostanoid receptor signaling relevant to tumor growth and angiogenesis. Trends in Pharamacological Sciences 34(10), 524-529 (2003). 2.Jiang, J., and Dingledine, R. Prostaglandin receptor EP2 in the crosshairs of anti-inflammation, anti-cancer, and neuroprotection. Trends in Pharamacological Sciences 34(7), 413-423 (2013). 3.Kawahara, K.,Hohjoh, H.,Inazumi, T., et al. Prostaglandin E2-induced inflammation: Relevance of prostaglandin E receptors. Biochimica et Biophysica Acta 1851(4), 414-421 (2015). 4.Ganesh, T.,Jiang, J.,Shashidharamurthy, R., et al. Discovery and characterization of carbamothioylacrylamides as EP2 selective antagonists. ACS Med.Chem.Lett. 4(7), 616-621 (2013). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 491.6 |
分子式 | C20H18FN5O3S3 |
CAS号 | 1164464-14-5 |
稳定性 | ≥ 2 years |
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