Overview
Alternative Name Benzamil amiloride
Lyophilized Powder yes
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
- Fischer, K.G. et al. (2002) Nephrol. Dial. Transplant 17, 1742.
- Taruno, A. and Marunaka, Y. (2010) Cell Physiol. Biochem. 26, 925.
- Dai, X.Q. et al. (2007) Mol. Pharmacol. 72, 1576.
- 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 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).
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
For research purposes only, not for human use
Last Update: 07/05/2024
Specifications
Citations
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