Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product 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 CAY10686 is a selective 3-aminocarbazole inhibitor of mPGES-1, blocking the synthesis of PGE₂ but not PGF_2α (Item No. 16010) in A549 cells stimulated with IL-1β (IC₅₀s = 2.9 and >100 µM, respectively).³ It reduces inflammatory pain (acetic acid-induced writhing) in mice by 74% when given intraperitoneally at 10 mg/kg.³ CAY10686 is JPorbed through enterocytes, is metabolically stable in human and rat microsome preparations, and is bioavailable in vivo.³

≥95%

Store at -20℃

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.Alisi, M.A.,Cazzolla, N.,Coletta, I., et al. 3-Aminocarbazole compound, pharmaceutical composition containing it and preparation method therefor. PCT/EP2009/055652, 1-38 (2009).