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The biological effects of prostaglandin D2 are transduced by at least two 7-transmembrane G-protein coupled receptors, designated DP1 and CRTH2/DP2. BAY-u3405 (Ramatroban) is an approved human medication for the treatment of allergic rhinitis that has documented activity as an antagonist of both the TP and CRTH2/DP2 receptors.1,2 CAY10471 is an analog of BAY-u3405 which contains modifications that increase both its potency and selectivity for the human CRTH2/DP2 receptor.3 CAY10471 binds to the human CRTH2/DP2, DP1, and TP receptors with Ki values of 0.6, 1200, and >10,000 nM, respectively.3
1
Sugimoto, H., Shichijo, M., Iino, T., et al. An orally bioavailable small molecule antagonist of CRTH2, Ramatroban (BAY u3405), inhibits prostaglandin D2-induced eosinophil migration in vitro. J Pharmacol Exp Ther305347-352(2003).
2
McKenniff, M.G., Norman, P., Cuthbert, N.J., et al. BAY u3405, a potent and selective thromboxane A2 receptor antagonist on airway smooth muscle in vitro.. Br J Pharmacol104(3)585-590(1991).
3
Ulven, T., and Kostenis, E. Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J Med Chem48(4)897-900(2005).
Sugimoto, H., Shichijo, M., Iino, T., et al. An orally bioavailable small molecule antagonist of CRTH2, Ramatroban (BAY u3405), inhibits prostaglandin D2-induced eosinophil migration in vitro. J Pharmacol Exp Ther305347-352(2003).
McKenniff, M.G., Norman, P., Cuthbert, N.J., et al. BAY u3405, a potent and selective thromboxane A2 receptor antagonist on airway smooth muscle in vitro.. Br J Pharmacol104(3)585-590(1991).
Ulven, T., and Kostenis, E. Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J Med Chem48(4)897-900(2005).
CAY10471 is available in the following screening
library: