Tarafenacin D-tartrate

"目录号: HY-14831

MBX 102 是选择性的(PPAR)-γ部分激动剂，常用于治疗 2 型糖尿病。

生物活性

Description

MBX 102 is a selective partial agonist of peroxisome proliferator-activated receptor(PPAR)-γ, used for the treatment of type 2 diabetes.

In Vitro

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 MBX-102 acid. MBX-102 shows a dose-dependent activation of mouse GAL4-PPAR-γ with EC50s of appr 12 μM[2].

In Vivo

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. 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]. 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 MBX-102 is an efficacious antidiabetic agent. 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].

Clinical Trial

NCT01416402

CymaBay Therapeutics, Inc.

Hyperuricemia-Gout

August 2011

Phase 2

NCT02063997

CymaBay Therapeutics, Inc.

Gout

March 2014

Phase 2

NCT02252835