Toggle Nav
Close
  • Menu
  • Setting

ML161

Catalog No.
A8229
PAR1 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$133.00
In stock
Evaluation Sample
$28.00
In stock
10mg
$105.00
In stock
50mg
$330.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

ML161 is a selective inhibitor of PAR1 with IC50 value of 0.26 μM [1].

Protease-activated receptor-1(PAR-1) is a unique G-protein-coupled receptor belonging to the protease-activated receptor family and its activation leads to downstream signaling events that launch a variety of cellular responses related to tumor progression [1].

ML161 is a potent PAR1 inhibitor and has a different selectivity with the reported ALK inhibitor crizotinib. When tested with human platelets, ML161 treatment inhibited the activation of thrombin-induced platelet in a dose-dependent manner by detecting P-selectin expression [1]. When tested with granule secretion, ML161 exhibited a potent inhibition on P-selectin expression in a dose-dependent manner with EC50 value of 0.3μM and also inhibited SFLLRN-induced thrombus formation [2].

References:
[1].  Dockendorff, C., et al., Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor. ACS Med Chem Lett, 2012. 3(3): p. 232-237.
[2].  VerPlank, L., et al., Chemical Genetic Analysis of Platelet Granule Secretion-Probe 3, in Probe Reports from the NIH Molecular Libraries Program. 2010, National Center for Biotechnology Information (US): Bethesda (MD).

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt361.23
Cas No.423735-93-7
FormulaC17H17BrN2O2
Solubility≥16.4mg/mL in DMSO, ≥46.9 mg/mL in EtOH with ultrasonic,insoluble in H2O
Chemical Name2-bromo-N-[3-(butanoylamino)phenyl]benzamide
SDFDownload SDF
Canonical SMILESCCCC(=O)NC1=CC=CC(=C1)NC(=O)C2=CC=CC=C2Br
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description ML-161 is an allosteric inhibitor of PAR1 with IC50 of 0.26 μM.
Targets PAR1          
IC50 0.26 μM          

Quality Control

Chemical structure

ML161