Arhalofenate (JNJ 39659100) is a selective partial agonist of peroxisome proliferator-activated receptor PPARγ. It is used for the treatment of type 2 diabetes.

Arhalofenate displays a dose-dependent activation of mouse GAL4-PPAR-γ (EC50s: appr 12 μM). Arhalofenate is a prodrug ester, that is rapidly and completely modified in vivo by non-specific serum esterases to the mature free acid form Arhalofenate (MBX 102) acid. [2].

MBX-102 significantly reduces fasting blood glucose, confirming that Arhalofenate (MBX 102) is an efficacious antidiabetic agent. Arhalofenate (60 mg/kg) causes a dramatic decrease in plasma and also results in a dose-dependent, significant decrease in the insulin resistance indexinsulin levels[1]. Arhalofenate (100 mg/kg, p.o.) obviously increases the glucose infusion rate and decreases hepatic glucose output in the clamped state in Zucker Diabetic Fatty (ZDF) rats. Arhalofenate (100 mg/kg, p.o.) significantly reduces triglyceride, free fatty acid, and cholesterol levels in ZDF rats. Arhalofenate (100 mg/kg, p.o.) also significantly lowers fasting plasma insulin, and robustly decreases fasting plasma triglycerides after 32 days of treatment in Zucker Fatty (ZF) rats[2].