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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.1 It is without effect on EP4, DP1, IP, and β2-adrenergic receptors. TG6-129 reduces the expression of COX-2, IL-1β, IL-12, IL-23, IL-6, and TNF-α induced by the EP2-selective agonist butaprost (Item No. 13740) in P388D1 macrophages.1 It has low cell cytotoxicity (CC50 = 326 µM), prolonged plasma half-life, and does not cross the blood-brain barrier.1
WARNING This product is not for human or veterinary use.
1. Discovery and characterization of carbamothioylacrylamides as EP2 selective antagonists. ACS Med. Chem. Lett. 4(7), 616-621 (2013).