Description
An orally bioavailable antagonist of CRTH2/DP2 (IC50 = 6 nM for the human receptor); selective for CRTH2/DP2 over DP1 in a radioligand binding assay (IC50 = 1,290 nM) and EP2 and EP4 in a β-arrestin assay (IC50s = 2,600 and >10,000 nM, respectively); inhibits PGD2-induced calcium flux in HEK293 cells expressing human CRTH2/DP2 (IC50 = 30 nM); inhibits PGD2-induced shape change in human eosinophils (IC50 = 235 nM)