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 absorbed through enterocytes, is metabolically stable in human and rat microsome preparations, and is bioavailable in vivo.³

≥95%