MF498

MF498 is a novel and selective E prostanoid receptor 4 (EP4 receptor) antagonist, displayed strong binding affinity for the EP4 receptor with Ki of 0.7 nM.Ki value: 0.7 nMTarget: EP4 receptorin vitro: MF498 also displays a relatively good selectivity over other prostanoid receptors, does not compromise the mucosal integrity in the gastrointestinal tract.MF498 inhibits PGE2-stimulated cAMP accumulation in a dose-dependent manner with IC50 values of 1.7 and 17 nM in the absence and presence of 10% serum, respectively. in vivo: MF498 relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis. MF498 on inflammation in adjuvant-induced arthritis (AIA), a rat model for rheumatoid arthritis (RA), and joint pain in a guinea pig model of iodoacetate-induced osteoarthritis (OA).

Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor

Research Areas >> Metabolic Disease

[1]. Clark P, et al. MF498 [N-{[4-(5,9-Diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylbenzyl]sulfonyl}-2-(2-methoxyphenyl)acetamide], a selective E prostanoid receptor 4 antagonist, relieves joint inflammation and pain in rodent models of r

Dinoprostone | Prostaglandin E1 | E7046 | ONO-AE3-208 | PF 04418948 | Fevipiprant | grapiprant | TG6-10-1 | Taprenepag | GW 627368 | MRE-269 | Ramatroban | AH 6809 | Laropiprant | AZD1981