Diminazene aceturate
Chemical Name: 4,4'-(1-Triazene-1,3-diyl)bis[benzenecarboximidamide] bis(N-acetylglycinate)
Purity: ≥98%
Biological Activity
Diminazene aceturate is an ASIC blocker (IC50 values are 202, ~320, ~320 and 864 nM for ASIC1b, ASIC1a, ASIC3 and ASIC2a, respectively). Exhibits no activity in ENaC channels expressed in oocytes. Accelerates desensitization of ASIC currents in hippocampal neurons. Inhibits mesotrypsin (Ki = 3.6�0.3 μM). Displays in vitro and in vivo anti-inflammatory effects in mice. Antihyperalgesic.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Inhibition of acid-sensing ion channels by diminazene and APETx2 evoke partial and highly variable antihyperalgesia in a rat model of inflammatory pain.
Lee et al.
Br.J.Pharmacol., 2018;175:2204 -
Small molecule inhibitors of mesotrypsin from a structure-based docking screen.
Kayode et al.
PLoS One, 2017;12:e0176694 -
Diarylamidines: high potency inhibitors of acid-sensing ion channels.
Chen et al.
Neuropharmacology, 2010;58:1045 -
Molecular basis of inhibition of acid sensing ion channel 1A by diminazene.
Krauson et al.
PLoS One, 2018;13:e0196894 -
Diminazene aceturate prevents nephropathy by increasing glomerular ACE2 and AT2 receptor expression in a rat model of type1 diabetes.
Goru et al.
Br.J.Pharmacol., 2017;174:3118
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