| Name | Arhalofenate |
| Description | Arhalofenate (JNJ 39659100) is a selective partial agonist of peroxisome proliferator-activated receptor PPARγ. It is used for the treatment of type 2 diabetes. |
| In vitro | 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]. |
| In vivo | 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 32.5 mg/mL (78.16 mM)
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| Keywords | PPAR | Peroxisome proliferator-activated receptors | MBX-102 | MBX102 | JNJ-39659100 | JNJ39659100 | Inhibitor | inhibit | Arhalofenate |
| Inhibitors Related | PHYTOL | (S)-(+)-Ibuprofen | BADGE | Cinnamyl alcohol | Daidzein | Fenofibrate | Pioglitazone hydrochloride | 5-Aminosalicylic Acid | Naringenin | Fisetin | 2,3-Butanediol | Icariin |
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United States
