KY-226 | CAS#1621673-53-7 | PTP1B Inhibitor

MedKoo Cat#: 555704 | Name: KY-226

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

KY-226

CAS#1621673-53-7

Theoretical Analysis

MedKoo Cat#: 555704

Name: KY-226

CAS#: 1621673-53-7

Chemical Formula: C27H31NO3S2

Exact Mass: 481.1745

Molecular Weight: 481.67

Elemental Analysis: C, 67.33; H, 6.49; N, 2.91; O, 9.96; S, 13.31

Price and Availability

Size	Price	Availability
5mg	USD 150.00	Ready to ship
10mg	USD 250.00	Ready to ship
25mg	USD 550.00	Ready to ship
50mg	USD 950.00	Ready to ship

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Related CAS #

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Synonym

KY-226; KY 226; KY226;

IUPAC/Chemical Name

4-(biphenyl-4-ylmethylsulfanylmethyl)-N-(hexane-1-sulfonyl)benzoylamide

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)

SMILES Code

O=C(NS(=O)(CCCCCC)=O)C1=CC=C(CSCC2=CC=C(C3=CC=CC=C3)C=C2)C=C1

Appearance

Fluffy white solid powder

Purity

>97% (or refer to the Certificate of Analysis)

Shipping Condition

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.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#A22T06K16

QC Data

View QC data: current batch, Lot#A22T06K16

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

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.

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/

	Solvent	mg/mL	mM
Solubility
	DMSO	173.0	359.17
	Ethanol	1.5	3.11

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 481.67 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Ito Y, Fukui M, Kanda M, Morishita K, Shoji Y, Kitao T, Hinoi E, Shirahase H. 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 Pharmacol Sci. 2018 May;137(1):38-46. doi: 10.1016/j.jphs.2018.03.001. Epub 2018 Mar 6. PMID: 29731242.

In vitro protocol:

In vivo protocol:

1: Sun M, Shinoda Y, Fukunaga K. KY-226 Protects Blood-brain Barrier Function Through the Akt/FoxO1 Signaling Pathway in Brain Ischemia. Neuroscience. 2019 Feb 10;399:89-102. doi: 10.1016/j.neuroscience.2018.12.024. Epub 2018 Dec 21. PubMed PMID: 30579831. 2: Ito Y, Fukui M, Kanda M, Morishita K, Shoji Y, Kitao T, Hinoi E, Shirahase H. 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 Pharmacol Sci. 2018 May;137(1):38-46. doi: 10.1016/j.jphs.2018.03.001. Epub 2018 Mar 6. PubMed PMID: 29731242. 3: Sun M, Izumi H, Shinoda Y, Fukunaga K. Neuroprotective effects of protein tyrosine phosphatase 1B inhibitor on cerebral ischemia/reperfusion in mice. Brain Res. 2018 Sep 1;1694:1-12. doi: 10.1016/j.brainres.2018.04.029. Epub 2018 Apr 26. PubMed PMID: 29705606.