CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist, with a Ki of 0.6 nM for hCRTH2, selective over human thromboxane A2 receptor TP (Ki, >10000 nM) or PGD2 receptor DP (Ki, 1200 nM). CAY10471 Racemate also has effect on mouse and rat orthologs of CRTH2[1]. Ki: 0.6 nM (CRTH2), 1200 nM (DP)[1]
CAY10471 Racemate (Compound 13) inhibits PGD2-induced inositol phosphate or cAMP formation, suppresses β-arrestin translocation with IC50s of 12 and 3 nM, respectively[1].
[1]. Ulven T, et al. Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J Med Chem. 2005 Feb 24;48(4):897-900.