| Bioactivity | Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes. |
| Invitro | 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[2]. |
| 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[1]. 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[2]. |
| Name | Arhalofenate |
| CAS | 24136-23-0 |
| Formula | C19H17ClF3NO4 |
| Molar Mass | 415.79 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Gregoire FM, et al. MBX-102/JNJ39659100, a novel peroxisome proliferator-activated receptor-ligand with weak transactivation activity retains antidiabetic properties in the absence of weight gain and edema. Mol Endocrinol. 2009 Jul;23(7):975-88. [2]. Chandalia A, et al. MBX-102/JNJ39659100, a novel non-TZD selective partial PPAR-γ agonist lowers triglyceride independently of PPAR-α activation. PPAR Res. 2009;2009:706852. |
Arhalofenate
CAS: 24136-23-0 F: C19H17ClF3NO4 W: 415.79
Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for
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