MF63

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Description

MF63 potently inhibited the human mPGES-1 enzyme (IC50=1.3 nM), with a high degree (>1000-fold) of selectivity over other prostanoid synthases. Microsomal prostaglandin E synthase-1 (mPGES-1) is a terminal prostaglandin E (2) (PGE (2)) synthase in the cyclooxygenase pathway. Inhibitors of mPGES-1 may block PGE (2) production and relieve inflammatory symptoms. In rodent species, MF63 strongly inhibited guinea pig mPGES-1 (IC50=0.9 nM) but not the mouse or rat enzyme. In addition, MF63 did not cause NSAID-like gastrointestinal toxic effects, such as mucosal erosions or leakage in the KI mice or nonhuman primates, although it markedly inhibited PGE2 synthesis in the KI mouse stomach.

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