TG4-155

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. 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. It blocks the induced expression of inflammatory markers in microglial cells treated with the selective EP2 agonist butaprost (Cay-13740) alone or with LPS and IFNgamma. TG4-155 significantly reduces neurodegeneration in a mouse model of status epilepticus, induced by pilocarpine (Cay-14487). It inhibits proliferation, invasion, and inflammatory cytokine expression in cancer cells treated with butaprost.Formal Name: (2E)-N-[2-(2-methyl-1H-indol-1-yl)ethyl]-3-(3,4,5-trimethoxyphenyl)-2-propenamide. CAS Number: 1164462-05-8. Molecular Formula: C23H26N2O4. Formula Weight: 394.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 50 mg/ml, DMSO: 30 mg/ml, Ethanol: 5 mg/ml. lambdamax: 225, 292 nm. SMILES: COC1=CC(/C=C/C(NCCN2C(C)=CC3=C2C=CC=C3)=O)=CC(OC)=C1OC. InChi Code: InChI=1S/C23H26N2O4/c1-16-13-18-7-5-6-8-19(18)25(16)12-11-24-22(26)10-9-17-14-20(27-2)23(29-4)21(15-17)28-3/h5-10,13-15H,11-12H2,1-4H3,(H,24,26)/b10-9+. InChi Key: YBHUXHFZLMFETJ-MDZDMXLPSA-N.