YS121 is a dual inhibitor of mPGES-1 (IC50 = 3.9 μM) and 5-LO (IC50 = 4.1 μM). It effectively inhibits PGE2 and LT synthesis in both cell free and intact cell assays. Moreover, YS121 (1.5 mg/kg, intraperitoneal) reduced pleural levels of PGE2 and LTB4 while blocking exudate formation and leukocyte infiltration in carrageenan-induced rat pleurisy. YS121 has minor effects on Cox-1 and Cox-2, inhibiting these enzymes 24.8% and 38%, respectively, at 10 μM.
1 Koeberle, A., Zettl, H., Greiner, C., et al. Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase. J Med Chem 51 8068-8076 (2008). 2 Werz, O., Greiner, C., Koeberle, A., et al. Novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structures of pirinixic acid. J Med Chem 51 5449-5453 (2008). 3 Koeberle, A., Rossi, A., Zettl, H., et al. The molecular pharmacology and in vivo activity of 2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid (YS121), a dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase. J Pharmacol Exp Ther 332 840-848 (2010).
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