Thiazolidinediones (TZDs) are a group of structurally related peroxisome proliferator-activated receptor γ (PPARγ) agonists with antidiabetic actions in vivo.1,2 The prototypical compound for this class is the TZD rosiglitazone (BRL 49653), which is currently marketed for the treatment of diabetes. CAY10599 is a PPARγ agonist that is 4-fold more potent than rosiglitazone at PPARγ demonstrating an EC50 value of 0.05 µM.3 This compound shows high selectivity for the PPARγ receptor over PPARα (EC50 = 3.99 µM) or PPARδ (EC50 > 10 µM).3
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 Chem39665-668(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 Chem373977-3985(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 Chem522618-2622(2009).
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 Chem373977-3985(1994).
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 Chem39665-668(1996).
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 Chem522618-2622(2009).
CAY10599 is available in the following screening
library: