10012553 CAY10595
(CAS 916047-16-0)
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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 PGD2.1 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.2 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.2
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1
Hirai, H., Tanaka, K., Yoshie, O., et al. Prostaglandin D2 selectivity induces chemotaxis in T helper type 2 cells, eosinophils, and basophils via seven-transmembrane receptor CRTH2. J Exp Med 193(2) 255-261 (2001).
2
Crosignani, S., Page, P., Missotten, M., et al. Discovery of a new class of potent, selective, and orally bioavailable CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases. J Med Chem 51 2227-2243 (2008).
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Pricing updated 2010-03-19.
Prices are subject to change without notice.
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Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.
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