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KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury[1][2].

In human hepatoma-derived cells (HepG2), KY-226 (0.3-10 μM) increases the phosphorylated insulin receptor (pIR) produced by insulin[1].KY-226 (1 μM; 24 hours; bEnd.3 cells) treatment rescues lipopolysaccharide-induced reduction of mRNA and protein levels of ZO-1. KY-226 treatment restores phosphorylation of pAkt (T308) and its downstream target forkhead box protein O1 (FoxO1) (S256) in bEnd.3 cells[2]. Western Blot Analysis[1] Cell Line: bEnd.3 cells stimulated with LPS

KY-226 (10-30 mg/kg/day; oral administration; daily; for 4 weeks; male db/db mice) treatment significantly reduces plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain[1]. KY-226 attenuates plasma glucose elevations in the oral glucose tolerance test. KY-226 also increases pIR and phosphorylated Akt in the liver and femoral muscle[1]. Animal Model: Male db/db mice (8-11 weeks old)[1]

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