TG6-10-1

TG6-10-1 is a potent antagonist of E prostanoid receptor 2 (EP2, Kb = 17.8 nM in C6 glioma cells overexpressing human EP2). It is 300-, 25-, and 10-fold selective for EP2 over other prostanoid receptors, including human EP3-4, FP and TP, and DP1 receptors, respectively. TG6-10-1 is also selective for EP2 over a panel of 40 enzymes, ion channels, receptors, and neurotransmitter transporters (IC50s >10 µM). In vivo, TG6-10-1 increases survival, decreases weight loss, prevents induction of IL-1beta, IL-6, TNF-alpha, and MCP-1/CCL2 mRNA, and inhibits neuronal cell death in the hippocampus in mouse and rat models of status epilepticus induced by pilocarpine (Cay-14487) and diisopropyl fluorophosphate, respectively.Formal Name: (2E)-N-[2-[2-(trifluoromethyl)-1H-indol-1-yl]ethyl]-3-(3,4,5-trimethoxyphenyl)-2-propenamide. CAS Number: 1415716-58-3. Molecular Formula: C23H23F3N2O4. Formula Weight: 448.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 50 mg/ml, DMSO: 30 mg/ml, Ethanol: 5 mg/ml. lambdamax: 216, 272, 300 nm. SMILES: COC1=CC(/C=C/C(NCCN2C(C(F)(F)F)=CC3=C2C=CC=C3)=O)=CC(OC)=C1OC. InChi Code: InChI=1S/C23H23F3N2O4/c1-30-18-12-15(13-19(31-2)22(18)32-3)8-9-21(29)27-10-11-28-17-7-5-4-6-16(17)14-20(28)23(24,25)26/h4-9,12-14H,10-11H2,1-3H3,(H,27,29)/b9-8+. InChi Key: WUYOECAJFJFUFC-CMDGGOBGSA-N.