| Description | 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 |
| In vitro | TG4-155是一种能穿透大脑的EP2拮抗剂（KB=2.4 nM），其对EP4的效果降低超过1000倍（KB=11.4 μM），并且对一系列其他受体和通道[1]的作用也较低。 |
| In vivo | TG4-155在由山梨醇引发的癫痫持续状态小鼠模型中显著减少神经退行性变化。该化合物抑制了经布他前列素[2]处理的癌细胞中的增殖、侵袭及炎症细胞因子表达。 |
| Cell experiments | 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]. |
| Animal experiments | 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]. |
| Target activity | EP2 receptor:9.9 nM (Ki) |
| molecular weight | 394.46 |
| Molecular formula | C23H26N2O4 |
| CAS | 1164462-05-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 125 mg/mL (316.89 mM) |
| References | 1. Jiang J , Ganesh T , Du Y , et al. Small molecule antagonist reveals seizure-induced mediation of neuronal injury by prostaglandin E2 receptor subtype EP2[J]. Proceedings of the National Academy of Sciences, 2012, 109(8):3149-3154. 2. Jiang J , Dingledine R . Role of Prostaglandin Receptor EP2 in the Regulations of Cancer Cell Proliferation, Invasion, and Inflammation[J]. Journal of Pharmacology and Experimental Therapeutics, 2012, 344(2):360-367. |