Diminazene aceturate

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Cat.No. 6705 - Diminazene aceturate | C14H15N7.2C4H7NO3 | CAS No. 908-54-3
Description: ASIC blocker; antihyperalgesic
Chemical Name: 4,4'-(1-Triazene-1,3-diyl)bis[benzenecarboximidamide] bis(N-acetylglycinate)
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (3)

Biological Activity

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

M. Wt 515.52
Formula C14H15N7.2C4H7NO3
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 908-54-3
PubChem ID 5284544
InChI Key OKQSSSVVBOUMNZ-UHFFFAOYSA-N
Smiles CC(NCC(O)=O)=O.CC(NCC(O)=O)=O.NC(C1=CC=C(C=C1)N/N=N/C2=CC=C(C(N)=N)C=C2)=N

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 51.55 100

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

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References

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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Keywords: Diminazene aceturate, Diminazene aceturate supplier, acid-sensing, acid, ion, channels, ASIC, blockers, analgesic, pain, thermal, mechanical, chemical, inflammatory, in, vivo, mesotrypsin, blocks, DIZE, 6705, Tocris Bioscience

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Literature in this Area

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