LT175 是一种双重PPARα/γ配体，具有强大的胰岛素增敏作用和降低的脂肪生成特性。LT175是口服有效 PPARγ 的部分激动剂 (hPPARα:EC50=0.22 μM; mPPARα:EC50=0.26 μM; hPPARγ:EC50=0.48 μM)。LT175 与 PPARγ 相互作用并影响辅助调节因子环 AMP 反应元件结合蛋白结合蛋白和核辅助抑制因子 1 (NCoR1) 的募集。LT175 在“二苯口袋”的疏水区域中与 PPARγ 相互作用。

LT175 is a dual PPARα/γ ligand with potent insulin-sensitizing effects and reduced adipogenic properties. LT175 is an orally active partial agonist against PPARγ(hPPARα: EC 50 =0.22 μm; mPPARα: EC 50 =0.26 μm; hPPARγ: EC 50 =0.48 μm). LT175 interacts with PPARγ and affects the recruitment of the coregulators cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1). LT175 interacts with PPARγ in a hydrophobic region called “diphenyl pocket” [1].

LT175 (100 mg/kg/day; orally; for 3 days) significantly reduce the body weight (11%) and reduces fasting blood glucose, triglycerides, and free fatty acids. LT175 decreases total plasma cholesterol significantly in diet-induced Insulin-resistant mice (six-week-old C57Bl/6J male mice) [1].

862901-87-9

C21H18O3

318.37

LT175

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years