Licofelone, Potassium Salt, Monohydrate

A cell-permeable, orally active arylpyrrolizine carboxylate that is both structurally and pharmacologically similar to, but less potent than, MK-886 (Cat. No. 475889). Both MK-886 and Licofelone effectively suppress cellular Cox pathway PGE2 (prostaglandin E2) production by inhibiting COX-1 and mPGES-1 (microsomal PGE2 synthase-1), but not COX-2 (IC50 = 0.8, 6, and >30 µM, respectively, by Licofelone), and both compounds suppress cellular 5-LO (5-Lypoxygenase; Cat. No. 437996) pathway activation (IC50 = 0.18 to 3.6 µM against ionophore-stimulated bovine and human PMNL LB4 production by Licofelone) by inhibiting FLAP (5-LO-activating protein), rather than 5-LO, activity (No inhibition up to 10 µM Licofelone). Unlike NSAIDs (nonsteroidal antiinflammatory drugs) that target only COX pathway, Licofelone does not cause gastrointestinal damages when applied in vivo.