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Submit ReviewDiminazene 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.
分子量 | 515.52 |
公式 | C14H15N7.2C4H7NO3 |
储存 | Store at RT |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
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
关键词: 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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