2. Academic Validation
  3. 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

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

  • Bioorg Med Chem Lett. 2011 Feb 1;21(3):1036-40. doi: 10.1016/j.bmcl.2010.12.016.
Nicholas Stock 1,  Deborah Volkots,  Karin Stebbins,  Alex Broadhead,  Brian Stearns,  Jeffrey Roppe,  Timothy Parr,  Christopher Baccei,  Gretchen Bain,  Charles Chapman,  Lucia Correa,  Janice Darlington,  Christopher King,  Catherine Lee,  Daniel S Lorrain,  Pat Prodanovich,  Angelina Santini,  Jilly F Evans,  John H Hutchinson,  Peppi Prasit
Affiliations

Affiliation

  • 1 Amira Pharmaceuticals, 9535 Waples St., San Diego, CA 92121, USA. nickstock@gmail.com
PMID: 21211969 DOI: 10.1016/j.bmcl.2010.12.016
Abstract

Compound 21 (AM432) was identified as a potent and selective antagonist of the DP(2) 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 DP(2) receptor, excellent pharmacokinetics in dog and in vivo activity in two mouse models of inflammatory disease after oral dosing.

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