| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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KY-226 is a novel, selective, orally bioactive and allosteric inhibitor of protein tyrosine phosphatase 1B (PTP1B) 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. KY-226 protects neurons from cerebral ischemic injury. KY-226 restores Akt (protein kinase B) phosphorylation and extracellular signal-regulated kinase (ERK) reduction in transient middle cerebral artery occlusion (tMCAO) damage. KY-226 protects BBB integrity by restoration of TJ proteins, an effect partly mediated by Akt/FoxO1 pathway activation.
| ln Vitro |
In human Manhattan-derived cells (HepG2), KY-226 (0.3-10 μM) enhances insulin synthesis at the phosphorylated insulin receptor (pIR) [1]. The reductions in ZO-1 mRNA and protein levels caused by LPS were reversed by treatment with KY-226 (1 μM; 24 hours; bEnd.3 cells). pAkt (T308) and its downstream target Forkhead protein framework O1 (FoxO1) (S256) are phosphorylated again in bEnd.3 cells by KY-226 [2].
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| ln Vivo |
KY-226 (10-30 mg/kg/day; epidermal documentation; daily; for 4 weeks; cosmetic db/db mice) treatment dramatically lowered antibiotic and lipid levels and hemoglobin A1c values, resulting in enhanced body weight [1 ]. KY-226 attenuates the increase in bone hyperplasia in the bone marrow tolerance test. KY-226 will enhance pIR and phosphorylated Akt in myocardial and femoral resection [1].
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| Cell Assay |
Western Blot analysis [1]
Cell Types: bEnd.3 stimulated with LPS Cell Tested Concentrations: 1 μM Incubation Duration: 24 hrs (hours) Experimental Results: Rescued lipopolysaccharide-induced decrease in ZO-1 mRNA and protein levels. |
| Animal Protocol |
Animal/Disease Models: Male db/db mice (8-11 weeks old) [1]
Doses: 10 mg/kg and 30 mg/kg Route of Administration: Oral; daily; for 4 weeks Experimental Results: Significant reduction in plasma glucose and Triglyceride levels and hemoglobin A1c values without increasing weight gain. |
| References |
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| Molecular Formula |
C27H31NO3S2
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|---|---|
| Molecular Weight |
481.669945001602
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| Exact Mass |
481.174
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| Elemental Analysis |
C, 67.33; H, 6.49; N, 2.91; O, 9.96; S, 13.31
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| CAS # |
1621673-53-7
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| PubChem CID |
76955652
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| Appearance |
Fluffy white solid powder
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| LogP |
6.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
33
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| Complexity |
653
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| Defined Atom Stereocenter Count |
0
|
| InChi Key |
MKXMABKUVSOEJF-UHFFFAOYSA-N
|
| InChi Code |
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)
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| Chemical Name |
4-(biphenyl-4-ylmethylsulfanylmethyl)-N-(hexane-1-sulfonyl)benzoylamide
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| Synonyms |
KY-226 KY 226 KY226
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~519.03 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.32 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0761 mL | 10.3806 mL | 20.7611 mL | |
| 5 mM | 0.4152 mL | 2.0761 mL | 4.1522 mL | |
| 10 mM | 0.2076 mL | 1.0381 mL | 2.0761 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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