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| Product Name: | KY-226 | | Synonyms: | KY-226;Benzamide, 4-[[([1,1'-biphenyl]-4-ylmethyl)thio]methyl]-N-(hexylsulfonyl)-;4-[[([1,1'-Biphenyl]-4-ylmethyl)thio]methyl]-N-(hexylsulfonyl)benzamide;inhibit,anti-diabetic,leptin,ZO-1,LPS,insulin,phosphorylated,KY-226,Akt,KY226,anti-obesity,PTP1B,Phosphatase,neurons,Inhibitor,KY 226;KY-226, 10 mM in DMSO | | CAS: | 1621673-53-7 | | MF: | C27H31NO3S2 | | MW: | 481.67 | | EINECS: | | | Product Categories: | | | Mol File: | 1621673-53-7.mol |  |
| | KY-226 Chemical Properties |
| density | 1.186±0.06 g/cm3(Predicted) | | storage temp. | -20° | | solubility | Soluble in DMSO (>25 mg/ml). | | pka | 3.91±0.40(Predicted) | | form | solid | | 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. | | InChI | 1S/C27H31NO3S2/c1-2-3-4-8-19-33(30,31)28-27(29)26-17-13-23(14-18-26)21-32-20-22-11-15-25(16-12-22)24-9-6-5-7-10-24/h5-7,9-18H,2-4,8,19-21H2,1H3,(H,28,29) | | InChIKey | MKXMABKUVSOEJF-UHFFFAOYSA-N | | SMILES | O=C(NS(=O)(CCCCCC)=O)C1=CC=C(CSCC2=CC=C(C3=CC=CC=C3)C=C2)C=C1 |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | KY-226 Usage And Synthesis |
| 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.1It significantly reduced plasma glucose, triglyceride, and A1c levels without weight gain in db/db mice.2It has been suggested that KY-226’s anti-diabetic effects occurviaenhancements in insulin signaling and anti-obesity effects via leptin signaling enhancements.2KY-226 has also been shown to protect neurons from cerebral ischemia.3This effect is mediated by restoration of tight junction proteinsviaactivation 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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| | References | [1] KO MORISHITA. Novel Non-carboxylate Benzoylsulfonamide-Based Protein Tyrosine Phosphatase 1B Inhibitors with Non-competitive Actions.[J]. Chemical & pharmaceutical bulletin, 2017, 65 12: 1144-1160. DOI:10.1248/cpb.c17-00635
[2] YUMA ITO . 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]. Journal of pharmacological sciences, 2018, 137 1: Pages 38-46. DOI:10.1016/j.jphs.2018.03.001
[3] MEILING SUN. Neuroprotective effects of protein tyrosine phosphatase 1B inhibitor on cerebral ischemia/reperfusion in mice[J]. Brain Research, 2018, 1694: Pages 1-12. DOI:10.1016/j.brainres.2018.04.029
[4] MEILING SUN Kohji F Yasuharu Shinoda. KY-226 Protects Blood–brain Barrier Function Through the Akt/FoxO1 Signaling Pathway in Brain Ischemia[J]. Neuroscience, 2019, 399: Pages 89-102. DOI:10.1016/j.neuroscience.2018.12.024 |
| | KY-226 Preparation Products And Raw materials |
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