Specification
Description
KY-226 is a protein tyrosine phosphatase 1B (PTP1B) inhibitor that 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.
Synonyms
KY-226; KY 226; KY226
IUPAC Name
4-(biphenyl-4-ylmethylsulfanylmethyl)-N-(hexane-1-sulfonyl)benzoylamide
Canonical SMILES
O=C(NS(=O)(CCCCCC)=O)C1=CC=C(CSCC2=CC=C(C3=CC=CC=C3)C=C2)C=C1
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)
InChI Key
MKXMABKUVSOEJF-UHFFFAOYSA-N
Solubility
Soluble in DMSO
Appearance
Fluffy white solid powder
Shelf Life
>3 years if stored properly
Storage
Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Biological Target
KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM.
Drug Formulation
This drug may be formulated in DMSO
Elemental Analysis
C, 67.33; H, 6.49; N, 2.91; O, 9.96; S, 13.31
HS Tariff Code
2934.99.9001
In Vitro Activity
KY-226 inhibited PTP1B activity at 0.1-10 μM, and the IC50 value was 0.28 ± 0.01 μM (mean ± S.E.M, n = 6).
Reference: J Pharmacol Sci. 2018 May;137(1):38-46. https://pubmed.ncbi.nlm.nih.gov/29731242/
In Vivo Activity
KY-226 at 10 and 30 mg/kg/day did not exhibit toxicity, and significantly reduced non-fasting plasma glucose and TG levels without increasing body weight gain in db/db mice (Fig. 4A). HFD-feeding markedly increased body weight gain, fat volume gain, and reduced food consumption, possibly due to the high calorie diet. KY-226 did not exhibit toxicity, significantly reduced body weight gain at 30 and 60 mg/kg/day, and reduced total food consumption and visceral fat volume gain at 60 mg/kg/day (Fig. 7A-D).
Reference: J Pharmacol Sci. 2018 May;137(1):38-46. https://pubmed.ncbi.nlm.nih.gov/29731242/
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Stock Solution Storage
0-4 °C for short term (days to weeks), or -20 °C for long term (months).