Amiloride hydrochloride

MK 870, Midamor®
Blocker of ENaC/ASIC/Degenerin Channels
Cat #: A-140
Alternative Name MK 870, Midamor®
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 266.09
    Purity: >99%
    Effective concentration 0.2 µM - 5 mM.
    Chemical name 3,5-Diamino-N-(aminoiminomethyl)-6-chloropyrazinecarboxamide hydrochloride.
    Molecular formula C6H8ClN7O•HCl.
    CAS No.: 2016-88-8.
    Activity Amiloride is a Na+ channel (ENaC/Degenerin/ASIC) blocker1. The IC50 values for Amiloride block of acid-sensing ion channels (ASIC) in PC12 cells are 0.2-0.7 μM2. Amiloride also inhibits TRPP3 channel activity in Xenopus oocytes with an IC50 value of 143 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 -20°C.
    Solubility 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.
      • Alomone Labs Amiloride hydrochloride blocks inward currents of ASIC3 channels expressed in Xenopus oocytes.
        A. ASIC3 currents were elicited by rapid exposure to pH 4.9 in physiological solution every 20 sec. Inhibition of the pH dependent inward transients was achieved upon perfusion of 200 μM or 2 mM Amiloride hydrochloride (#A-140) (indicated by the horizontal bars). Membrane potential was held at 5 mV. B. Superimposed traces of ASIC3 current in the absence or presence of 200 μM or 2 mM Amiloride hydrochloride, as indicated (taken from the experiment in A).
      • Amiloride is a well-known antagonist of ENaC, Na+/Ca2+, and Na+/H+ exchangers, nonselective cation channels, and voltage-gated K+ and Ca2+ channels1-8. It has been extensively used as a probe for a wide variety of transport systems1.

        Acid-sensing ion channels (ASICs) are expressed in various sensory and central neurons. Six different ASIC subunits have been cloned, which are encoded by four genes (ASIC1–ASIC4). Amiloride is a nonselective ASIC blocker and the channels cloned all belong to the Amiloride-sensitive Na+-channel. The IC50 values for Amiloride block of ASIC in PC12 cells are 0.2-0.7 µM9, values which are ~10–20 times lower than its block of ASICs in central10 and sensory neurons11.

        TRPP3, a member of the transient receptor potential (TRP) superfamily of cation channels, is a Ca2+-activated nonselective cation channel permeable to Ca2+, K+, Na+, Rb+, NH4, and Ba2+, inhibited by Mg2+, H+, La3+, and Gd3+12-13. TRPP3 is localized to a subset of taste receptor cells in the tongue, where it may play a crucial role in sour tasting, and to neurons surrounding the central canal of the spinal cord, where it may account for the long-sought proton-dependent regulation of the frequency of action potential. Amiloride inhibits TRPP3 channel activity in Xenopus oocytes with an IC50 value of 143 µM14.

    Target ENaC, ASIC, TRPP3 channels, NHE-1 transporter
    Last update: 20/05/2019

    Amiloride hydrochloride (#A-140) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use