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