TG8-260 is a second-generation EP2 antagonist developed to alleviate the pathology of central nervous system and peripheral diseases driven by inflammation. TG8-260 can reduce neuroinflammation and gliosis in the hippocampus of rats after pilocarpine-induced persistent epileptic status. Pharmacokinetic data of TG8-260 showed that its plasma half-life was 2.14 hours and its oral bioavailability was 77.3%. TG8-260 is also a potent inhibitor of CYP450 and shows antagonistic activity in inhibiting EP2 receptor-mediated inflammatory gene expression in BV2-hEP2 microglia, which is suitable for studying anti-inflammatory pathways in animal models of peripheral inflammatory diseases.
References:
[1]. Amaradhi R, Mohammed S, Banik A, et al. Second-generation prostaglandin receptor EP2 antagonist, TG8-260, with high potency, selectivity, oral bioavailability, and anti-inflammatory properties[J]. ACS Pharmacology & Translational Science, 2022, 5(2): 118-133.