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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 yes
  • Bioassay Tested
  • Source Synthetic
    MW: 311.77
    Purity: >98%
    Effective concentration 1-300 µM.
    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.
    1. Banke, T.G. (2011) Brain Res. 1381, 21.
    2. Masereel, B. et al. (2003) Eur. J. Med. Chem38, 547.
    3. Kuduk, S.D. et al. (2009) Bioorg. Med. Chem. Lett. 19, 2514.
    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.
    Our bioassay
    • Alomone Labs HMA inhibits TRPA1 channels activation by AITC in HEK-293 cells.
      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
    1. Banke, T.G. (2011) Brain Res. 1381, 21.
    2. Kuduk, S.D. et al. (2009) Bioorg. Med. Chem. Lett. 19, 2514.
    3. Chessell, I.P. et al. (1998) Br. J. Pharmacol. 124, 1314.
    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
    Last update: 06/11/2022

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

    For research purposes only, not for human use
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