MF63

MF63 is a selective and orally active inhibitor of mPGES-1. MF63 reduces the accumulation of PGE₂, relieves pyresis, hyperalgesia, and inflammatory pain by inhibiting mPGES-1^[1]. IC50 & Target:mPGES-1^[1] In Vitro:MF63 (0.01-100 µM; 24 h) selectively inhibits PGE₂ induced by 10 ng/mL IL-1β in A549 cells, and increases the formation of PGF_2α in a dose-dependent manner^[1].
MF63 (10 µM; 24 h) enhances the expression of various metallothionein 1 (MT1) subtypes and endogenous antagonists of IL-1 and IL-36 with the anti-inflammatory effects^[2]. In Vivo:MF63 (100 mg/kg; p.o.; single dose) attenuates PEG₂ accumulation in air pouches and brains of the KI (knock-in mPGES-1 gene) mice and inhibits PEG₂ formation in a dose-dependent manner^[1].
MF63 (10 mg/kg and 100 mg/kg; p.o.; single dose) inhibits the hyperalgesic response induced by LPS in the KI mice, with dose-dependently manner^[1].
MF63 (0-150 mg/kg; p.o.; single dose) inhibits PEG₂ synthesis, hyperalgesia, pyresis and relieves Chronic Osteoarthritic-Like Pain in the guinea pig^[1].
MF63 (0-100 mg/kg; p.o.; twice daily for 4 days) has gastrointestinal tolerability in KI mice and nonhuman primates^[1].