Prostaglandin E2 is the major PG synthesized at sites of inflammation and plays an important role in different inflammatory diseases. It acts as a mediator of pain and inflammation and promotes bone destruction. The increased synthesis of PGE2 during inflammation can be accounted for by increased expression of both COX-2 and microsomal PGE synthase-1 (mPGES-1). CAY10700 is an orally bioavailable inhibitor of mPGES-1 (IC50 = 0.24 uM in an in vitro human whole blood assay). It is inactive against COX-1 and COX-2 (9% inhibition at 100 uM and 16% at 30 uM, respectively).
References:
[1].Schiffler, M.A., Antonysamy, S., Bhattachar, S.N., et al. Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors Journal of Medicinal Chemistry 59(1), 194-205 (2016).