TG8-260 is a second-generation, potent, selective EP2 antagonist with Schild KB of 13.2 nM.
TG8-260 displays 500-fold selectivity to EP2 against other prostanoid receptors.
TG8-260 has a plasma half-life of 2.14 h (PO) and excellent oral bioavailability (77.3%), TG8-260 is a potent inhibitor of CYP450 enzymes.
TG8-260 displays antagonistic activity on the induction of EP2 receptor-mediated inflammatory gene expression in microglia BV2-hEP2 cells.
TG8-260 reduces hippocampal neuroinflammation and gliosis after pilocarpine-induced status epilepticus in rats.
TG8-260 is a tool for investigating anti-inflammatory pathways in peripheral inflammatory disease animal models.
