mPGES1-IN-3 is a potent, selective mPGES-1 inhibitor with enzyme IC50 of 8 nM, A549 cell IC50 of 16.24 nM, human whole blood IC50 of 249.9 nM.
mPGES1-IN-3 displays excellent in vitro selectivity over mPGES-2, cPGES, COX1/2, other prostanoid synthases, favorable hERG and CEREP panel profile.
mPGES1-IN-3 shows good efficacy in LPS-induced thermal hyperalgesia pain model.
mPGES1-IN-3 demonstrates good oral pharmacokinetic profiles and good CNS B/P ratio in rat and guinea pig.
