5-(N,N-Hexamethylene) amiloride
An Antagonist of Na+/H+ Exchangers, P2X7 receptors and TRPA1, ASIC3 Channels
    Cat #: H-130
    Alternative Name 5-(N,N-Hexamethylene) amiloride
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 311.77
    Purity: >98%
    Effective concentration 1-300 µM.
      • HMA
    Chemical name 3-amino-5-(azepan-1-yl)-6-chloro-N-(diaminomethylidene)pyrazine-2-carboxamide.
    Molecular formula C12H18ClN7O.
    CAS No.: 1428-95-1.
    PubChem CID 1794
    Activity HMA is an amiloride derivative, shown to inhibit TRPA1-mediated calcium signal with IC50 of 35 µM1. It is an inhibitor of the Na+/H+ exchanger (NHE), with Ki of 0.013-2.4 µM for various NHE isoforms2. HMA also blocks ASIC3 channels by 51% at 20 µM3.
    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 +4°C.
    Solubility Up to 100mM in DMSO. Centrifuge all products before use (10000 x g 5 min).
    Storage of solutions Up to three months at -20°C.
      • HMA
        Alomone Labs HMA inhibits TRPA1 channels activation by AITC in HEK-293 cells.
        Dose response curve of HMA (#H-130) inhibition of the TRPA1-mediated, allyl isothiocyanate (AITC)-induced increase in intracellular Ca2+ (IC50 is estimated at 121.9 µM). Cells were loaded with Calcium 5 dye, incubated with HMA, and stimulated with 1 µM allyl isothiocyanate (EC80). Changes in intracellular Ca2+ following stimulation were detected as changes in relative fluorescence (RFU).
    References - Scientific background
      • HMA is a TRPA1 channel blocker with an IC50 value of 35 µM, an inhibitor of the Na+/H+ exchangers (NHE) and a blocker of ASIC3 channel (acid-sensing ion channels)1-3. HMA also antagonizes P2X7 receptors, although it is not potent4.

        HMA as an NHE inhibitor, is considered to be a promising adjuvant drug for overcoming acquired resistance to treatment in various malignant hemopathies1-3.

    Target NHE exchangers, TRPA1, ASIC3 channels, P2X7 receptors

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    Last update: 21/11/2019

    HMA (#H-130) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use