NaV1.1-Compound 3a

N,N'-(1,3-phenylene)bis(2-methylbenzamide)
A Modulator of NaV1.1 Channel
    Cat #: CMN-002
    Alternative Name N,N'-(1,3-phenylene)bis(2-methylbenzamide)
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 344.41
    Purity: >97%
    Effective concentration 1-100 µM.
    Structure
    • NaV1.1-Compound 3a
    Chemical name N,N'-(1,3-phenylene)bis(2-methylbenzamide).
    Molecular formula C22H20N2O2.
    Activity A novel and selective modulator of NaV1.1 channels, shown to decrease the rate of inactivation of NaV1.1 channels, and to increase neuronal excitability in hippocampal fast-spiking interneurons under weak depolarization at 30-100 µM1.
    References-Activity
    1. Crestey, F. et al. (2015) ACS. Chem. Neurosci. 6, 1302.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Up to 30 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • NaV1.1-Compound 3a
      Alomone Labs NaV1.1-Compound 3a modulates the current of human NaV1.1 channels stably expressed in HEK/293 cells.
      A. Superimposed traces of NaV1.1 current upon application of control solution (black), and of 10 µM (grey) and 30 µM (green) NaV1.1-Compound 3a (#CMN-002). Current was elicited by a 50 ms voltage step from the holding potential of -120 mV to 0 mV, delivered every 3 sec. B. Normalized values of the decay time constant τ (diamonds) and peak amplitude (circles) of NaV1.1 current, plotted against rising concentrations of NaV1.1-Compound 3a, demonstrate concentration dependent modulation of the two parameters. At 30 µM NaV1.1-Compound 3a decreases current amplitude, yet significantly increases the decay time constant τ (reduces the rate of inactivation).
    References - Scientific background
    1. Crestey, F. et al. (2015) ACS. Chem. Neurosci. 6, 1302.
    2. Cardoso, F.C. et al. (2015) Mol. Pharmacol. 88, 291.
    Scientific background

    NaV1.1-Compound 3a is a modulator of the NaV1.1 channel. This compound increases the activity of NaV1.1 channels although its overall impact remains moderate. It has the ability to increase neuronal excitability in fast-spiking hippocampal interneurons1.

    Mutations of NaV channels are associated with a range of complex pathological conditions such as epilepsy, myotonic conditions and cardiac arrhythmias1,2. Loss-of-function mutations in mouse models has shown several phenotypes such as autistic-like behaviors, cognitive deficits, severe epilepsy, and unexpected death1.

    Target NaV1.1 channels
    Last update: 24/01/2020

    NaV1.1-Compound 3a (#CMN-002) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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