产品描述:
Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 (Item No. 17020) into the biologically active PGE2 (Item No. 14010).{7229} Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.{11537} AF3485 is a selective 3-aminocarbazole inhibitor of mPGES-1, blocking the synthesis of PGE2 but not PGF2α (Item No. 16010) in A549 cells stimulated with IL-1β (IC50s = 2.9 and >100 µM, respectively).{27227} It reduces inflammatory pain (acetic acid-induced writhing) in mice by 74% when given intraperitoneally at 10 mg/kg.{27227} AF3485 is absorbed through enterocytes, is metabolically stable in human and rat microsome preparations, and is bioavailable in vivo.{27227}