mPGES1-IN-7

mPGES-1-IN-2 (compound III) is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PGDS) (5 μM, IR=60 %). mPGES-1-IN-2 reduces PGE2 production and tends to reduce levels of other prostaglandins. mPGES-1-IN-2 effectively inhibits acute inflammation in an air sac model stimulated by Carrageenan (HY-125474) in mice^[1]. IC50 & Target:IC50: 0.9 μM (recombinant human mPGES-1), 0.09 μM (recombinant rat mPGES-1)^[1]; lipocalin-type PGD synthase (I-PGDS)^[1] In Vitro:mPGES-1-IN-2 (compound III) (0.64-80 μM; 24 h) can reduce PGE2 production after LPS (10 ng/mL) stimulation in A549 cells, mouse macrophages, and blood [1] .br/mPGES-1-IN-2 () Inhibits PGE2 synthesis in a concentration-dependent manner, causing PGH2 to shunt to the prostacyclin pathway^[1].
In Vivo:mPGES-1-IN-2 (compound III) (10-100 mg/kg; ip; single dose) effectively inhibits global prostaglandin production in a mouse model of air sac inflammation induced by 1% λ-Carrageenan (HY-N9470). synthesis and reduce cell migration^[1].