1277168-95-2Relevant academic research and scientific papers
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
scheme or table, 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.
