KY-226 是选择性的，口服活性的和变构蛋白酪氨酸磷酸酶 1B 抑制剂，IC50=0.25 μM，且不激活 PPARγ 。它可以保护神经元免受脑缺血损伤。它通过增强胰岛素和瘦素信号传导发挥抗糖尿病和抗肥胖作用。

KY-226 is a potent inhibitor of protein tyrosine phosphatase 1B (PTP1B)(IC50: 0.25 μM,)

In db/db mice, the oral administration of KY-226 (10 and 30 mg/kg/day, 4 weeks) significantly reduced plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain, while pioglitazone exerted similar effects with increases in body weight gain.?KY-226 attenuated plasma glucose elevations in the oral glucose tolerance test.?KY-226 also increased pIR and phosphorylated Akt in the liver and femoral muscle.?In high-fat diet-induced obese mice, the oral administration of KY-226 (30 and 60 mg/kg/day, 4 weeks) decreased body weight gain, food consumption, and fat volume gain with increases in phosphorylated STAT3 in the hypothalamus.

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C27H31NO3S2

481.67

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years