"目录号: HY-14831
Cell Cycle/DNA DamageNF-κB-
MBX 102 是选择性的(PPAR)-γ部分激动剂，常用于治疗 2 型糖尿病。
PPAR
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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
CymaBay Therapeutics, Inc.
Gout-Hyperuricemia
August 2014
Phase 2
NCT01336686
CymaBay Therapeutics, Inc.
Hyperuricemia-Gout
May 2011
Phase 2
NCT01399008
CymaBay Therapeutics, Inc.
Gout
June 2011
Phase 2
NCT01416402
CymaBay Therapeutics, Inc.
Hyperuricemia-Gout
August 2011
Phase 2
NCT02063997
CymaBay Therapeutics, Inc.
Gout
March 2014
Phase 2
NCT02252835
CymaBay Therapeutics, Inc.
Gout-Hyperuricemia
August 2014
Phase 2
NCT01336686
CymaBay Therapeutics, Inc.
Hyperuricemia-Gout
May 2011
Phase 2
NCT01399008
CymaBay Therapeutics, Inc.
Gout
June 2011
Phase 2
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References
[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.