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

KY-226
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 555704

CAS#: 1621673-53-7

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.

Chemical Structure

KY-226

CAS# 1621673-53-7

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 555704
Name: KY-226
CAS#: 1621673-53-7
Chemical Formula: C27H31NO3S2
Exact Mass: 481.17
Molecular Weight: 481.669
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	Ready to ship
10mg	USD 250	Ready to ship
25mg	USD 550	Ready to ship
50mg	USD 950	Ready to ship
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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/

Solubility Data

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

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:	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 vivo 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.

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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.

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