Overview
Alternative Name 5-(N,N-Hexamethylene) amiloride
Lyophilized Powder yes
Source Synthetic
MW: 311.77
Purity: >98%
Effective concentration 1-300 µM.
Structure
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.
References-Activity
- Banke, T.G. (2011) Brain Res. 1381, 21.
- Masereel, B. et al. (2003) Eur. J. Med. Chem. 38, 547.
- 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.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
- Banke, T.G. (2011) Brain Res. 1381, 21.
- Kuduk, S.D. et al. (2009) Bioorg. Med. Chem. Lett. 19, 2514.
- 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
Lyophilized Powder
HMA (#H-130) is a highly pure, synthetic, and biologically active compound.
For research purposes only, not for human use
Last Update: 07/05/2024
Applications
Citations
Citations
Powered by Bioz
