MK-7246 is a potent, selectie, orally availableprostaglandin D2 receptor (CRTH2, GPR44) antagonist with Ki of 2.5 nM (hCRTH2).
MK-7246 displayes149-fold selectivity over DP receptor, >1,500-fold over other prostanoid receptors, also binds to recombinant mouse, rat, dog and cynomolgus monkey CRTH2 receptors with Ki of <10 nM.
MK-7246 blocks DK-PGD2-induced inhibition of cAMP formation in HEK293E-CRTH2 cells with IC50 of 3 nM, inhibits DK-PGD2-induced eosinophil shape change (IC50=2.2 nM), also efficiently blocksDK-PGD2-induced CD11b up-regulation on eosinophils and basophils (IC50= 6.2 and 5.4 nM) in human whole blood.
MK-7246 significantly reduces antigen-induced late phase bronchoconstriction and airway hyper-responsiveness in vivo.
