Anti-diabetic drugs of the thiazolidinedione (TZD) structural class as well as alpha-lipoic acid activate peroxisome proliferator-activated receptor gamma (PPARgamma), a nuclear transcription factor that controls glucose metabolism and lipid homeostasis. CAY10506 is a hybrid lipoic acid-TZD derivative that transactivates human PPARgamma with an EC50 value of 10 uM.