CAY10595 |
Catalog No.GC18678 |
CAY10595 es un potente antagonista del receptor CRTH2/DP2 que se une al receptor humano con una Ki de 10 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 916047-16-0
Sample solution is provided at 25 µL, 10mM.
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. CAY10595, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 10 nM. The R enantiomer of CAY10595 is significantly more potent exhibiting Ki values of 5.3 and 5 nM at the human and murine CRTH2/DP2 receptor, respectively. The R enantiomer of CAY10595 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-PGD2 with an IC50 value of 7.3 nM.
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