Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH₂ into the biologically active PGE₂.¹ Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.² CAY10678 is a benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC₅₀ = 0.09 and 0.9 µM, respectively).³ It has minimal effects on COX-1, COX-2, PGIS, and hematopoietic PGDS at 50 μM but reduces lipocalin-type PGDS activity by 60% at this concentration.³ CAY10678 dose-dependently blocks PGE₂ synthesis in isolated cells and whole blood treated with LPS or IL-1β.³ It also dose-dependently reduces PGE₂ synthesis and cell recruitment during inflammation in mice.³

≥98%

Store at -20℃

mPGES-1 Inhibitor III;

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.Leclerc, P.,Idborg, H.,Spahiu, L., et al. Characterization of a human and murine mPGES-1 inhibitor and comparison to mPGES-1 genetic deletion in mouse models of inflammation. Prostaglandins & Other Lipid Mediators 107, 26-34 (2013).