Description
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.
Product information
CAS Number: 1621673-53-7
Molecular Weight: 481.67
Formula: C27H31NO3S2
Chemical Name: 4-{[({[1,1'-biphenyl]-4-yl}methyl)sulfanyl]methyl}-N-(hexane-1-sulfonyl)benzamide
Smiles: CCCCCCS(=O)(=O)NC(=O)C1C=CC(CSCC2C=CC(=CC=2)C2C=CC=CC=2)=CC=1
InChiKey: MKXMABKUVSOEJF-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 250 mg/mL (519.03 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
In human hepatoma-derived cells (HepG2), KY-226 (0.3-10 μM) increases the phosphorylated insulin receptor (pIR) produced by insulin. KY-226 (1 μM; 24 hours; bEnd.3 cells) treatment rescues lipopolysaccharide-induced reduction of mRNA and protein levels of ZO-1. KY-226 treatment restores phosphorylation of pAkt (T308) and its downstream target forkhead box protein O1 (FoxO1) (S256) in bEnd.3 cells.
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. 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.
Products are for research use only. Not for human use.
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