1175525-90-2Relevant articles and documents
Sodium [2′-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4′-(6- ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): A potent, selective prostaglandin D2 receptor antagonist
Stock, Nicholas,Volkots, Deborah,Stebbins, Karin,Broadhead, Alex,Stearns, Brian,Roppe, Jeffrey,Parr, Timothy,Baccei, Christopher,Bain, Gretchen,Chapman, Charles,Correa, Lucia,Darlington, Janice,King, Christopher,Lee, Catherine,Lorrain, Daniel S.,Prodanovich, Pat,Santini, Angelina,Evans, Jilly F.,Hutchinson, John H.,Prasit, Peppi
, p. 1036 - 1040 (2011/03/21)
Compound 21 (AM432) was identified as a potent and selective antagonist of the DP2 receptor (CRTH2). Modification of a bi-aryl core identified a series of tri-aryl antagonists of which compound 21 proved a viable clinical candidate. AM432 shows excellent potency in a human whole blood eosinophil shape change assay with prolonged incubation, a comparatively long off-rate from the DP2 receptor, excellent pharmacokinetics in dog and in vivo activity in two mouse models of inflammatory disease after oral dosing.
