Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product prostaglandin H₂ (PGH₂; Item No. 17020) into the biologically active PGE₂ (Item No. 14010).¹ Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.² PF-9184 is a potent inhibitor of mPGES-1 (IC₅₀ = 16.5 nM for recombinant human enzyme).³ It displays at least 6,500-fold selectivity for mPGES-1 over COX-1 and COX-2. PF-9184 blocks the synthesis of PGE₂ in LPS-treated human whole blood and in IL-1β-stimulated fibroblasts (IC₅₀s = 0.4-5 µM).^4,5

≥98%

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1.Jakobsson, P.J.,Thorén, S.,Morgenstern, R., et al. Identification of human prostaglandin E synthase: A microsomal, glutathione-dependent, inducible enzyme, constituting a potential novel drug target. Proceedings of the National Academy of Sciences of the United States of America 96, 7220-7225 (1999).

2.Stichtenoth, D.O.,Thorén, S.,Bian, H., et al. Microsomal prostaglandin E synthase is regulated by proinflammatory cytokines and glucocorticoids in primary rheumatoid synovial cells. Journal of Immunology 167, 469-474 (2001).

3.Mbalaviele, G.,Pauley, A.M.,Shaffer, A.F., et al. Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor. Biochemical Pharmacology 79(10), 1445-1454 (2010).

4.Chang, H.H. and Meuillet, E.J. Identification and development of mPGES-1 inhibitors: Where we are at? Future Med.Chem. 3(15), 1909-1934 (2011).

5.Korotkova, M. and Jakobsson, P.J. Microsomal prostaglandin E synthase-1 in rheumatic diseases. Frontiers in Pharmacology 1(146), 1-8 (2011).