TG6-129

Prostaglandin E2 (PGE2, Cay-14010) 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. TG6-129 is an antagonist of the EP2 receptor, suppressing PGE2-induced elevation of cAMP in cells expressing EP2 with an IC50 value of 1.6 µM. It is without effect on EP4, DP1, IP, and beta2-adrenergic receptors. TG6-129 reduces the expression of COX-2, IL-1beta, IL-12, IL-23, IL-6, and TNF-alpha induced by the EP2-selective agonist butaprost (Cay-13740) in P388D1 macrophages. It has low cell cytotoxicity (CC50 = 326 µM), prolonged plasma half-life, and does not cross the blood-brain barrier.Formal Name: (2E)-N-[[[4-[[(5-ethyl-1,3,4-thiadiazol-2-yl)amino]sulfonyl]phenyl]amino]thioxomethyl]-3-(4-fluorophenyl)-2-propenamide. CAS Number: 1164464-14-5. Synonyms: SID 17503974. Molecular Formula: C20H18FN5O3S3. Formula Weight: 491.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 8 mg/ml, DMSO: 10 mg/ml. lambdamax: 224, 310 nm. SMILES: FC1=CC=C(/C=C/C(NC(NC2=CC=C(S(NC3=NN=C(CC)S3)(=O)=O)C=C2)=S)=O)C=C1. InChi Code: InChI=1S/C20H18FN5O3S3/c1-2-18-24-25-20(31-18)26-32(28,29)16-10-8-15(9-11-16)22-19(30)23-17(27)12-5-13-3-6-14(21)7-4-13/h3-12H,2H2,1H3,(H,25,26)(H2,22,23,27,30)/b12-5+. InChi Key: SYSMVOANBVDZNG-LFYBBSHMSA-N.