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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $133 | In Stock | |
5 mg | $302 | In Stock | |
10 mg | $453 | In Stock | |
25 mg | $747 | In Stock | |
50 mg | $1,050 | In Stock | |
100 mg | $1,420 | In Stock | |
500 mg | $2,830 | In Stock | |
1 mL x 10 mM (in DMSO) | $348 | In Stock |
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]. |
Alias | JNJ 39659100, MBX 102 |
Molecular Weight | 415.79 |
Formula | C19H17ClF3NO4 |
Cas No. | 24136-23-0 |
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) ![]() | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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