Potent dual CRTH2 and prostaglandin D2
) 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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Discovery of AMG 853, a CRTH2 and DP dual antagonist.
Liu et al.
ACS Med.Chem.Lett., 2011;2:326