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Arhalofenate

CAS No. : 24136-23-0

MCE 国际站：Arhalofenate

产品活性：Arhalofenate (MBX 102) 是选择性的(PPAR)-γ部分激动剂，常用于 2 型糖尿病的研究。

研究领域：Cell Cycle/DNA Damage  |  Vitamin D Related/Nuclear Receptor  |  Metabolic Enzyme/Protease

作用靶点：PPAR

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.

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