Toggle Nav
Close
  • Menu
  • Setting

WAY 170523

Catalog No.
A4442
MMP-13 inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
1mg
$435.00
In stock
10mg
$734.00
Ship with 5-10 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Description:IC50: 17 nm (MMP-13)
Collagenase 3 is an enzyme that in humans is encoded by the MMP13 gene. Proteins of the matrix metalloproteinase (MMP) family are involved in the breakdown of extracellular matrix in normal physiological processes, such as embryonic development, reproduction, and tissue remodeling, as well as in disease processes, such as arthritis and metastasis .
In vitro: The combination of NMR spectroscopy with molecular modeling techniques and HTS data resulted in the design of a novel, potent, and selective MMP-13 inhibitor (WAY-170523) which has an IC50 of 17 nM for MMP-13 and showed >5800-, 56-, and >500-fold selectivity against MMP-1, MMP-9, and TACE, respectively. To the best of our knowledge, this represents the first example of a potent MMP-13 inhibitor that has been shown to be selective against MMP-9 [1].
In vivo: In order to investigate a putative role of MMP-13 in ISO-dependent cardiac dysfunction, the authors infused WT mice with ISO for 7 days and concurrently delivered the specific MMP-13 inhibitor WAY170523 daily by i.p injection. Remarkably, they found that WAY170523 completely abolished ISO-dependent increase of the left ventricular systolic diameter and preserved cardiac function in ISO-infused animals without modifying the hypertrophic response similar to the PAR1 KO animals. [2].
Clinical trial: WAY-170523 is currently in the preclinical development and no clinical trial is ongoing.
References:
[1] James M. Chen, Frances C. Nelson, Jeremy I. Levin, Dominick Mobilio, Franklin J. Moy, Ramaswamy Nilakantan, Arie Zask, and Robert Powers. Structure-Based Design of a Novel, Potent, and Selective Inhibitor for MMP-13 Utilizing NMR Spectroscopy and Computer-Aided Molecular Design. J. Am. Chem. Soc. 2000, 122, 9648-9654
[2] Jaffré F, Friedman AE, Hu Z, Mackman N, Blaxall BC. β-adrenergic receptor stimulation transactivates protease-activated receptor 1 via matrix metalloproteinase 13 in cardiac cells. Circulation. 2012;125(24):2993-3003.

Chemical Properties

Physical AppearanceWhite solid
StorageDesiccate at RT
M.Wt613.68
Cas No.307002-73-9
FormulaC33H31N3O7S
Solubility<61.37mg/ml in DMSO; <61.37mg/ml in ethanol
Chemical NameN-(2-(4-(N-benzyl-N-(2-(hydroxycarbamoyl)-4,6-dimethylphenyl)sulfamoyl)phenoxy)ethyl)benzofuran-2-carboxamide
SDFDownload SDF
Canonical SMILESO=C(C1=CC2=CC=CC=C2O1)NCCOC3=CC=C(S(=O)(N(C4=C(C)C=C(C)C=C4C(NO)=O)CC5=CC=CC=C5)=O)C=C3
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

WAY 170523