916046-55-4

The biological effects of prostaglandin D₂ (PGD₂) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP₁ and CRTH2/DP₂. In humans, CRTH2/DP₂ is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD₂. CAY10597, as a racemic mixture, is a potent CRTH2/DP₂ receptor antagonist that binds to the human receptor with a K_i value of 37 nM. The R enantiomer is slightly more potent exhibiting K_i values of 23 and 22 nM at the human and murine CRTH2/DP₂ receptor, respectively. The R enantiomer of CAY10597 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-prostaglandin D₂ with an IC₅₀ value of 40 nM.

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