货号 | 17639-1mg |
描述 | Prostaglandin E2(PGE2) 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 TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4(KB = 11.4 µM) and a panel of other receptors and channels.4,5 It blocks the induced expression of inflammatory markers in microglial cells treated with the selective EP2 agonist butaprost (Item No. 13740) alone or with LPS and IFNγ.4,6 TG4-155 significantly reduces neurodegeneration in a mouse model of status epilepticus, induced by pilocarpine (Item No. 14487).4 It inhibits proliferation, invasion, and inflammatory cytokine expression in cancer cells treated with butaprost.5 |
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.Jiang, J.,Ganesh, T.,Du, Y., et al. Small molecule antagonist reveals seizure-induced mediation of neuronal injury by prostaglandin E2 receptor subtype EP2. Proceedings of the National Academy of Sciences of the United States of America 109(8), 3149-3154 (2012). 5.Jiang, J. and Dingledine, R. Role of prostaglandin receptor EP2 in the regulations of cancer cell proliferation, invasion, and inflammation. Journal of Pharmacology and Experimental Therapeutics 344, 360-367 (2013). 6.Quan, Y.,Jiang, J. and Dingledine, R. EP2 receptor signaling pathways regulate classical activation of microglia. The Journal of Biological Chemisty 288(13), 9293-9302 (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 | 394.5 |
分子式 | C23H26N2O4 |
CAS号 | 1164462-05-8 |
稳定性 | ≥ 2 years |
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