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Merck
CN

SML0353

Sigma-Aldrich

Azimilide dihydrochloride

≥97% (HPLC)

别名:

1-[[[5-(4-Chlorophenyl)-2-furanyl]methylene]amino]-3-[4-(4-methyl-1-piperazinyl)butyl]-2,4-imidazolidinedione dihydrochloride

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About This Item

经验公式(希尔记法):
C23H28ClN5O3 · 2HCl
分子量:
530.88
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

方案

≥97% (HPLC)

表单

powder

储存条件

desiccated

颜色

white to beige

溶解性

DMSO: 1 mg/mL, clear (warmed)

储存温度

2-8°C

SMILES字符串

Cl.Cl.CN1CCN(CCCCN2C(=O)CN(\N=C/c3ccc(o3)-c4cccc(Cl)c4)C2=O)CC1

InChI

1S/C23H28ClN5O3.2ClH/c1-26-11-13-27(14-12-26)9-2-3-10-28-22(30)17-29(23(28)31)25-16-20-7-8-21(32-20)18-5-4-6-19(24)15-18;;/h4-8,15-16H,2-3,9-14,17H2,1H3;2*1H/b25-16-;;

InChI key

SUHOTCCGXXEWJN-DSHYBBOZSA-N

应用

Azimilide dihydrochloride may be used in the electrophysiology experiments with human ether-a-go-go-related gene 1a (HERG1a) subunit.

生化/生理作用

Azimilide is an inhibitor of human ether-a-go-go-related gene (HERG) channel. It displays a decrease in inhibitory effect in acidic pH conditions.
Azimilide is an investigational class III anti-arrhythmic drug that blocks fast and slow components of the delayed rectifier cardiac potassium channels. It inhibits KV7.1 and KV11.1 potassium channels. Azimilide′s block of K+ currents is relatively selective for IKr over IKs: It potently blocks the rapidly activating component of the delayed rectifier, IKr (IC50 0.4 mM), and inhibits IKs (IC50 3 mM) with nearly 10-fold less potency. At 10 mM, it does not block the inward rectifier K+ current. It blocks (10 mM) the L-type Ca2+ current (ICa) in a use-dependent manner.

特点和优势

This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

象形图

Skull and crossbones

警示用语:

Danger

危险声明

危险分类

Acute Tox. 3 Oral

储存分类代码

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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访问文档库

Action potential and QT prolongation not sufficient to cause Torsade de Pointes: role of action potential triangulation.
Augustus O Grant et al.
Journal of cardiovascular electrophysiology, 18(2), 204-205 (2007-03-07)
Donglin Guo et al.
Journal of cardiovascular electrophysiology, 18(2), 196-203 (2007-01-11)
The morphology of the mammalian cardiac action potential (AP) is an important factor in the susceptibility to drug-induced early afterdepolarizations (EADs) that may initiate torsade de pointes (TdP). AP triangulation has been shown to be an important predictor of drug-induced
S Sharma
The Journal of the Association of Physicians of India, 55 Suppl, 43-46 (2008-03-29)
The treatment of cardiac arrhythmias has undergone a sea change with the advent of catheter ablative procedures (radiofrequency ablation) and use of implantable cardioverter defibrillator (ICD). The antiarrhythmic drugs at times are used to prevent device related arrhythmia rather than
Qian Yang et al.
Yao xue xue bao = Acta pharmaceutica Sinica, 46(1), 12-18 (2011-04-07)
Due to the complicated pathogenesis of cardiac arrhythmia, the safe and effective therapeutic strategies for cardiac arrhythmia remain an urgent medical problems in the recent years. In this paper, we introduced the research practice of anti-arrhythmic agents targeting on potassium
Jarosław Kaźmierczak et al.
Pacing and clinical electrophysiology : PACE, 30(8), 1043-1046 (2007-08-03)
The presented case report describes a male patient with an implanted cardioverter-defibrillator (ICD) in whom a coadministration of ciprofloxacin and azimilide caused QT interval prolongation and multiple episodes of torsades de pointes (TdP) followed by ICD shocks (arrhythmic storm). The

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