KY-226 is a protein tyrosine phosphatase 1B (PTP1B) inhibitor with IC50 of 0.25 μM, which protects neurons from cerebral ischemic injury. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 (0.3-10 μM) increases the phosphorylated insulin receptor (pIR) produced by insulin in human hepatoma-derived cells.
In vivo, KY-226 (10-30 mg/kg/day; oral; for 4 weeks) treatment in male db/db mice significantly reduces plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥ 100 mg/mL|
KY-226 Protects Blood-brain Barrier Function Through the Akt/FoxO1 Signaling Pathway in Brain Ischemia
Meiling Sun, et al. Neuroscience. 2019 Feb 10;399:89-102. PMID: 30579831.
Therapeutic effects of the allosteric protein tyrosine phosphatase 1B inhibitor KY-226 on experimental diabetes and obesity via enhancements in insulin and leptin signaling in mice
Yuma Ito, et al. J Pharmacol Sci. 2018 May;137(1):38-46. PMID: 29731242.
Neuroprotective effects of protein tyrosine phosphatase 1B inhibitor on cerebral ischemia/reperfusion in mice
Meiling Sun, et al. Brain Res. 2018 Sep 1;1694:1-12. PMID: 29705606.
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