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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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关于此项目

经验公式（希尔记法）:
C23H28ClN5O3 · 2HCl
化学文摘社编号:
149888-94-8
分子量:
530.88
UNSPSC代码:
12352200
PubChem化学物质编号:
329825356
NACRES:
NA.77

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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 a Class III antiarrhythmic; blocker of the delayed rectifier cardiac potassium channels; inhibits KV7.1 and KV11.1 potassium channels.
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
GHS06

警示用语：

Danger

危险声明

H301

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

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000409436
0000409436
0000248322
0000248322
0000129751

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Richard L Page et al.
Journal of cardiovascular electrophysiology, 19(2), 172-177 (2007-10-06)
Azimilide hydrochloride is an investigational antiarrhythmic medication that had shown evidence of efficacy in prolonging the time to recurrence of atrial fibrillation (AF) or atrial flutter (AFL) and paroxysmal supraventricular tachycardia (PSVT). This study was designed to confirm efficacy of
L Brent Mitchell
Cardiology clinics, 26(3), 405-418 (2008-06-10)
Antiarrhythmic drug therapy, broadly defined, is the mainstay of treatment and prevention of ventricular tachycardia (VT)/ventricular fibrillation (VF), which can lead to sudden death. This article evaluates the evidence for and appropriate use of class I antiarrhythmic drugs, class III
Azimilide: another effort to prevent implantable cardioverter-defibrillator shocks and their sequelae why it is important and how it works.
David S Cannom et al.
Journal of the American College of Cardiology, 52(13), 1084-1085 (2008-10-14)
James A Reiffel
Current cardiology reports, 9(5), 381-386 (2007-09-20)
Implantable cardioverter defibrillators (ICDs) are now the mainstay of therapy in patients with sustained ventricular tachycardia (VT), ventricular fibrillation, resuscitated sudden cardiac death, or certain high-risk markers for these arrhythmic events. Although ICDs in such patients can be life-saving, they
Paul Dorian et al.
Journal of the American College of Cardiology, 52(13), 1076-1083 (2008-10-14)
The goal of this study was to determine whether azimilide, as compared with placebo, will reduce the number of emergency department (ED) visits and hospitalizations caused by arrhythmias or cardiac events in patients with an implantable cardioverter-defibrillator (ICD). Patients with
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