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5-(N,N-Dimethyl)amiloride hydrochloride

DMA, Dimethyl amiloride

A Blocker of TRPA1 Channels and Selective Blocker of Na+/H+ and Na+/Ca2+ Exchangers

Cat #: D-165
Alternative Name DMA, Dimethyl amiloride
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 294.1
    Purity: >99% (HPLC)
    Form Lyophilized powder.
    Effective concentration 1-100 µM.
    Chemical name 3-amino-6-chloro-N-(diaminomethylidene)-5-(dimethylamino)pyrazine-2-carboxamide;hydrochloride.
    Molecular formula C8H13Cl2N7O.
    CAS No.: 1214-79-5
    PubChem CID 11957442
    Activity 5-(N,N-Dimethyl)amiloride hydrochloride blocks TRPA1 channels with an IC50 of 80 µM1.
    1. 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 -20°C.
    Solubility Up to 50 mM in methanol. Centrifuge all product preparations before use (5,000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs 5-(N,N-Dimethyl)amiloride hydrochloride inhibits allyl isothiocyanate induced calcium signal in TRPA1 expressing cells. 
      Alomone Labs 5-(N,N-Dimethyl)amiloride hydrochloride inhibits allyl isothiocyanate induced calcium signal in TRPA1 expressing cells
      Dose-response curve for the inhibition of human TRPA1 expressing HEK-293 cells loaded with Calcium 5 dye for changes in intracellular Ca2+ measurements. Allyl isothiocyanate (100 µM) induced calcium signal was inhibited by 50, 100 and 200µM of 5-(N,N-Dimethyl)amiloride hydrochloride (#D-165), with estimated IC50 of about 60 µM.
    References - Scientific background
    1. Gunawardana, S.C. et al. (2008) Am. J. Physiol. 294, 1097.
    2. Gunawardana, S.C. et al. (2005) BMC Endocr. Disord. 5, 9.
    3. Soliman, M. (2009) J. Saudi Heart Assoc. 21, 159.
    4. Cui, X.L. et al. (2002) Sheng Li Xue Bao. 54, 219.
    5. Banke, T.G. (2011) Brain Res. 1381, 21.
    Scientific background

    5-(N,N-Dimethyl)amiloride hydrochloride (DMA) is an amiloride derivative that selectively inhibits Na+/H+ exchangers in cellular membranes, resulting in the retention of H+ ions and in the decrease of intracellular pH. Amiloride derivatives are commonly used for their diuretic and antihypertensive properties.

    Several studies have reported that DMA has positive effects in pancreatic β-cells on insulin release as a result of mis-regulation of intracellular pH and enhanced insulin secretion. Thus, amiloride derivatives are promising potential therapeutic agents for Type 2 Diabetes. In addition, positive effects on other cell functions have been demonstrated such as, cell membrane electrical activity, increase in intracellular Ca2+ and retention of K+1. DMA also enables glucose to induce time-dependent potentiation and enables it to occur in situations where it is normally absent1,2. Another study has suggested the possibility of DMA protection of the heart against post-resuscitation myocardial injury3.

    DMA also has the ability to inhibit the Na+/Ca2+ exchanger and to increase its currents in rat cardiomyocytes. Experimental trials have showed that DMA increases calcium sensitivity in normal and hypertrophied cardiomyocytes4.

    DMA also blocks TRPA1 channels5.

    Target TRPA1 channel, Na+/H+ and Na+/Ca2+ exchangers
    Last update: 06/11/2022

    5-(N,N-Dimethyl)amiloride hydrochloride (#D-165) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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