Chemical Name: 5-Chloro-4-[2-[[(2-chloro-4-cyclopropylphenyl)sulfonyl]amino]-4-[[(1,1-dimethylethyl)amino]carbonyl]phenoxy]-2-fluorobenzeneacetic acid
Biological ActivityPotent dual CRTH2 and prostaglandin D2 (PGD2) receptor antagonist (IC50 values are 8 and 35 nM, respectively in plasma). Inhibits PGD2-induced down modulation of CRTH2 on CD16- granulocytes in human whole blood as well as PGD2-induced cAMP response in platelets. Inhibits PGD2-induced airway constriction in vivo. Also inhibits BRD4 (Kd = 170 nM). Orally bioavailable.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of AMG 853, a CRTH2 and DP dual antagonist.
Liu et al.
ACS Med.Chem.Lett., 2011;2:326
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HL-1 cardiomyocytes were pre-incubated with AMG 853 (1 µM, 30 min) followed by treatment with 15d-PGJ2 (15 µM, 30 min) to follow p38 activation using Western blot analysis. AMG 853 inhibited 15d-induced p38 phosphorylation.