名称 | TG4-155 |
描述 | 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 |
细胞实验 | Cytotoxicity of TG4-155 was examined with the CellTiter-Glo Luminescent Cell Viability Assay by measuring cellular ATP level, which correlates with cell viability.?Briefly, C6G cells were plated in 384-well plates at 2,000 cells/well in 25 μl DMEM plus test compound and incubated for 2 days.?CellTiter-Glo reagent (25 μl) was then added to each well.?The contents were mixed for 2 minutes on an orbital shaker to induce cell lysis and incubated at room temperature for 10 minutes.?Relative viability is proportional to luminescence intensity as measured by a microplate reader with an integration time of 1 second[2]. |
动物实验 | C57BL/6 mice (8 12 wk old) were injected with pilocarpine (280 mg/kg, i.p.) to induce status epilepticus (SE). SE was allowed for 1 h and terminated by pentobarbital (30 mg/kg, i.p.). Mice were then randomized by assignment to a random number stream and received two doses of vehicle or TG4-155 (5 mg/kg, i.p.) at 1 and 12 h after SE termination. Mice were euthanized under deep isoflurane anesthesia 24 h after SE and brains were collected for histology[1]. |
体外活性 | 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[1]. |
体内活性 | TG4-155 significantly reduces neurodegeneration in a mouse model of status epilepticus, induced by pilocarpine. It inhibits proliferation, invasion, and inflammatory cytokine expression in cancer cells treated with butaprost[2]. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 125 mg/mL (316.89 mM)
|
关键字 | inhibit | TG4-155 | TG-4-155 | TG4155 | TG4 155 | Prostaglandin Receptor | Inhibitor |
相关产品 | Angoroside C | Pranoprofen | Tranilast | Benorilate | Rutin | Ozagrel | Ethamsylate | Rebamipide | Evodiamine | Tebufelone | Timapiprant | p-Hydroxycinnamic acid |
相关库 | 疼痛相关化合物库 | 经典已知活性库 | 膜蛋白靶向化合物库 | 血脑屏障通透化合物库 | 抑制剂库 | NO PAINS 化合物库 | 抗衰老化合物库 | 已知活性化合物库 | 共价抑制剂库 | GPCR靶点分子库 |