| Identification | Back Directory | [Name]
KY-226 | [CAS]
1621673-53-7 | [Synonyms]
KY-226
4-[[([1,1'-Biphenyl]-4-ylmethyl)thio]methyl]-N-(hexylsulfonyl)benzamide
Benzamide, 4-[[([1,1'-biphenyl]-4-ylmethyl)thio]methyl]-N-(hexylsulfonyl)- | [Molecular Formula]
C27H31NO3S2 | [MDL Number]
MFCD32263946 | [MOL File]
1621673-53-7.mol | [Molecular Weight]
481.67 |
| Chemical Properties | Back Directory | [density ]
1.186±0.06 g/cm3(Predicted) | [storage temp. ]
-20° | [solubility ]
Soluble in DMSO (>25 mg/ml). | [form ]
solid | [pka]
3.91±0.40(Predicted) | [color ]
Off-white | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| Hazard Information | Back Directory | [Description]
KY-226 (CAS 1621673-53-7)? is a selective allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor (IC50?= 250 nM) with no activity at PPARγ.1?It significantly reduced plasma glucose, triglyceride, and A1c levels without weight gain in db/db mice.2?It has been suggested that KY-226’s anti-diabetic effects occur?via?enhancements in insulin signaling and anti-obesity effects via leptin signaling enhancements.2?KY-226 has also been shown to protect neurons from cerebral ischemia.3?This effect is mediated by restoration of tight junction proteins?via?activation of the Akt/FoxO1 pathway.4 | [Uses]
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 vivo]
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] | | Dosage: | 10 mg/kg and 30 mg/kg | | Administration: | Oral administration; daily; for 4 weeks | | Result: | Significantly reduced plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain.
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| [storage]
Store at -20°C | [References]
1) Morashita (2017),?Novel Non-carboxylate Benzoylsulfonamide-Based Protein Tyrosine Phosphatase 1B Inhibitor with Non-competitive Actions;?Chem.Pharm.Bull.?65?1144
2) Ito?et al.?(2018),?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;?J.Pharmacol.Sci?137?38
3) Sun?et al.?(2018),?Neuroprotective effects of protein tyrosine phosphatase 1B on cerebral ischemia/reperfusion in mice;?Brain Res.?1694?1
4) Sun?et al.?(2019),?KY-226 Protects Blood-brain Barrier Function Through the Akt/FoxO1 Signaling Pathway on Brain Ischemia;?Neuroscience?399?89 |
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| Company Name: |
DC Chemicals
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021-58447131 13564518121 |
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http://m.approvedhomemanagement.com/ShowSupplierProductsList927327/0.htm |
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cjbscvictory
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| Tel: |
13348960310 13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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