Arhalofenate

Arhalofenate is a selective partial agonist of peroxisome proliferator-activated receptor PPARγ. It is used for the treatment of type 2 diabetes. (In Vitro) :Arhalofenate (MBX 102) 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. Arhalofenate (MBX 102) shows a dose-dependent activation of mouse GAL4-PPAR-γ with EC50s of appr 12 μM. (In Vivo) :Arhalofenate (MBX 102) (100 mg/kg, p.o.) significantly increases the glucose infusion rate and decreases hepatic glucose output in the clamped state in Zucker Diabetic Fatty (ZDF) rats. Arhalofenate (MBX 102) (60 mg/kg) leads to a dramatic decrease in plasma and also results in a dose-dependent, significant decrease in the insulin resistance indexinsulin levels. Arhalofenate (MBX 102) (100 mg/kg, p.o.) significantly decreases triglyceride, free fatty acid, and cholesterol levels in ZDF rats. MBX-102 significantly reduces fasting blood glucose, confirming that Arhalofenate (MBX 102) is an efficacious antidiabetic agent. Arhalofenate (MBX 102) (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.

24136-23-0

MBX 102 | JNJ 39659100

>98% (HPLC)

DMSO:10 mM

CC (=O) NCCOC (=O) [C@@H] (C1=CC=C (C=C1) Cl) OC2=CC=CC (=C2) C (F) (F) F

C19H17ClF3NO4

415.79

Storage temperature: -20°C. Stability: ≥ 2 years