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Diminazene aceturate New
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.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 515.52. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.94 mL||9.7 mL||19.4 mL|
|5 mM||0.39 mL||1.94 mL||3.88 mL|
|10 mM||0.19 mL||0.97 mL||1.94 mL|
|50 mM||0.04 mL||0.19 mL||0.39 mL|
References are publications that support the biological activity of the product.
Lee et al (2018) Inhibition of acid-sensing ion channels by diminazene and APETx2 evoke partial and highly variable antihyperalgesia in a rat model of inflammatory pain. Br.J.Pharmacol. 175 2204 PMID: 29134638
Kayode et al (2017) Small molecule inhibitors of mesotrypsin from a structure-based docking screen. PLoS One 12 e0176694 PMID: 28463992
Chen et al (2010) Diarylamidines: high potency inhibitors of acid-sensing ion channels. Neuropharmacology 58 1045 PMID: 20114056
Krauson et al (2018) Molecular basis of inhibition of acid sensing ion channel 1A by diminazene. PLoS One 13 e0196894 PMID: 29782492
Goru et al (2017) Diminazene aceturate prevents nephropathy by increasing glomerular ACE2 and AT2 receptor expression in a rat model of type1 diabetes. Br.J.Pharmacol. 174 3118 PMID: 28688122
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Literature in this Area
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.