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Benzamil

Benzamil amiloride

An Inhibitor of Na+/Ca2+ Exchangers and a Blocker of ASIC, TRPP3 and TRPA1 Channels

Cat #: B-161
Alternative Name Benzamil amiloride
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 319.75
    Purity: >99%
    Effective concentration 1-300 µM.
    Structure
    Chemical name 3,5-diamino-N-(N'-benzylcarbamimidoyl)-6-chloropyrazine-2-carboxamide.
    Molecular formula C13H14ClN7O.
    CAS No.: 161804-20-2
    PubChem CID 108107
    Activity Benzamil is a potent amiloride analogue, an inhibitor of the Na+/Ca2+ exchanger (IC50 = 0.1 µM)1, a blocker of Deg/ENaC channels2, of TRPP3 channels (IC50 = 1.1 µM)3 and of TRPA1 channels (IC50 = 55 µM)4.
    References-Activity
    1. Fischer, K.G. et al. (2002) Nephrol. Dial. Transplant 17, 1742.
    2. Taruno, A. and Marunaka, Y. (2010) Cell Physiol. Biochem. 26, 925.
    3. Dai, X.Q. et al. (2007) Mol. Pharmacol. 72, 1576.
    4. Banke, T.G. (2011) Brain Res. 1381, 21.
    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 100 mM 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 Benzamil inhibits ASIC3 channels expressed in Xenopus oocytes.
      Alomone Labs Benzamil inhibits ASIC3 channels expressed in Xenopus oocytes.
      A. Time course of Benzamil (#B-161) inhibition of ASIC3 channels current. Membrane potential was held at -60 mV, current was elicited every 50 sec by transient applications of pH 5.5, and was inhibited significantly by a 4 min application of 50 µM Benzamil (horizontal bar). B. Superimposed traces of ASIC3 currents upon application of control and of 50 µM Benzamil, as indicated, taken from the experiment in A.
    • Alomone Labs Benzamil inhibits TRPA1 currents induced by AITC in HEK-293 cells.
      Alomone Labs Benzamil inhibits TRPA1 currents induced by AITC in HEK-293 cells.
      Dose-response curve of Benzamil (#B-161) inhibition of human TRPA1-mediated increase in intracellular Ca2+. Cells were loaded with Calcium 5 dye, incubated with Benzamil, 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. Fischer, K.G. et al. (2002) Nephrol. Dial. Transplant 17, 1742.
    2. Dai, X.Q. et al. (2007) Mol. Pharmacol. 72, 1576.
    3. Banke, T.G. (2011) Brain Res. 1381, 21.
    4. Jeong. S. et al. (2013) J. Korean Med. Sci. 28, 1238.
    Scientific background

    Benzamil is a potent amiloride analog that acts as an inhibitor of Na+/Ca2+ exchangers and a blocker of ASIC/Deg/ENaC, TRPP3, and TRPA1 channels displaying IC50 of 0.1, 1.1 and 55 µM respectively1-3.

    Benzamil is commercially available as an inhibitor for acid sensing ion channels (ASICs) belonging to the Deg/ENaC family. The compound is also well known as a diuretic compound that is used for the management of congestive heart disease or hypertension. Intrathecal administration of benzamil demonstrates antinociceptive effects in several pain models in animals and humans through the inhibition of acid sensing ion channels4.

    Target Na+/Ca2+ exchangers, ASIC/ENaC, TRPP3, TRPA1 channels
    Lyophilized Powder
    Last update: 06/11/2022

    Benzamil (#B-161) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
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