CAY10599 is a PPARγ agonist that is 4-fold more potent than rosiglitazone at PPARγ demonstrating an EC50 value of 0.05 μM. This compound shows high selectivity for the PPARγ receptor over PPARβ (EC50 > 10 μM) or PPARα (EC50 = 3.99 μM).
1 Willson, T.M., Cobb, J.E., Cowan, D.J., et al. The structure-activity relationship between peroxisome proliferator-activated receptor γ agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem 39 665-668 (1996). 2 Cantello, B.C.C., Cawthorne, M.A., Cottam, G.P., et al. [[ω-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents. J Med Chem 37 3977-3985 (1994). 3 Lin, C., Peng, Y., Coumar, M.S., et al. Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor g agonists. J Med Chem 52 2618-2622 (2009).
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