Biological Activity
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.
In Vitro
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In Vivo
No in vivo data are provided in the current product source. Contact us for further information.
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.