Name: ML161
Price: 282.00 USD

- Overview
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    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].
    
    [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).
- Properties
  - Alternative Name
    
    2-bromo-N-[3-(butanoylamino)phenyl]benzamide
    
    CAS Number
    
    423735-93-7
    
    Molecular Formula
    
    C17H17BrN2O2
    
    Molecular Weight
    
    361.23
    
    Appearance
    
    A solid
    
    Purity
    
    97.00%
    
    Solubility
    
    insoluble in H2O; ≥16.4 mg/mL in DMSO; ≥46.9 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only