Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 into the biologically active PGE2 .
CAS：1195786-61-8
分子式：C22H17F3N2O2
分子量：398.4
纯度：98%
存储：Store at -20°C

Background:

Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 into the biologically active PGE2 . Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α. CAY10686 is a selective 3-aminocarbazole inhibitor of mPGES-1, blocking the synthesis of PGE2 but not PGF2α in A549 cells stimulated with IL-1β (IC50s = 2.9 and >100 uM, respectively). It reduces inflammatory pain (acetic acid-induced writhing) in mice by 74% when given intraperitoneally at 10 mg/kg. CAY10686 is absorbed through enterocytes, is metabolically stable in human and rat microsome preparations, and is bioavailable in vivo.