AGU654 (AGU-654) is a potent, selective microsomal prostaglandin E2 synthase 1 (mPGES-1) inhibitor with IC50 of 2.9 nM in cell-free assays.
AGU654 shows no activities of isolated COX-1/2 or 5-LOX in cell-free assays, nor FLAP in human neutrophils at 1 uM.
AGU654 blocks mPGES-1 in a reversible manner.
AGU654 selectively inhibits PGE2 formation in human macrophages and in human whole blood, without reducing the generation of other COX/LOX-derived LM.
AGU654 (10 and 30 mg/kg, oral) shows anti-inflammatory and analgesic effect in the carrageenan-induced paw edema model of guinea pig.
