KY-226
- Product Name
- KY-226
- CAS No.
- 1621673-53-7
- Chemical Name
- KY-226
- Synonyms
- KY-226;KY-226, 10 mM in DMSO;4-[[([1,1'-Biphenyl]-4-ylmethyl)thio]methyl]-N-(hexylsulfonyl)benzamide;Benzamide, 4-[[([1,1'-biphenyl]-4-ylmethyl)thio]methyl]-N-(hexylsulfonyl)-;inhibit,anti-diabetic,leptin,ZO-1,LPS,insulin,phosphorylated,KY-226,Akt,KY226,anti-obesity,PTP1B,Phosphatase,neurons,Inhibitor,KY 226
- CBNumber
- CB14668126
- Molecular Formula
- C27H31NO3S2
- Formula Weight
- 481.67
- MOL File
- 1621673-53-7.mol
KY-226 Property
- 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.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0077591
- Product name
- KY-226
- Purity
- 98.02%
- Packaging
- 5mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- CS-0077591
- Product name
- KY-226
- Purity
- 98.02%
- Packaging
- 10mg
- Price
- $250
- Updated
- 2021/12/16
- Product number
- CS-0077591
- Product name
- KY-226
- Purity
- 98.02%
- Packaging
- 25mg
- Price
- $450
- Updated
- 2021/12/16
- Product number
- CS-0077591
- Product name
- KY-226
- Purity
- 98.02%
- Packaging
- 50mg
- Price
- $750
- Updated
- 2021/12/16
- Product number
- CS-0077591
- Product name
- KY-226
- Purity
- 98.02%
- Packaging
- 100mg
- Price
- $1100
- Updated
- 2021/12/16
KY-226 Chemical Properties,Usage,Production
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. |
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
Raw materials
Preparation Products
KY-226 Suppliers
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- 400-164-7117 13681763483
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