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KY-226

Cat. No. M9699
KY-226 Structure
Synonym:

KY226

Size Price Availability
5mg USD 160  USD160 4-7 Days
10mg USD 270  USD270 4-7 Days
25mg USD 480  USD480 4-7 Days
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 481.67
Formula C27H31NO3S2
CAS Number 1621673-53-7
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Meiling Sun, et al. Neuroscience. KY-226 Protects Blood-brain Barrier Function Through the Akt/FoxO1 Signaling Pathway in Brain Ischemia

[2] Yuma Ito, et al. J Pharmacol Sci. 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

[3] Meiling Sun, et al. Brain Res. Neuroprotective effects of protein tyrosine phosphatase 1B inhibitor on cerebral ischemia/reperfusion in mice

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Keywords: KY-226, KY226 supplier, Phosphatase, inhibitors, activators


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