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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 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.
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
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Philippe Chevalier et al.
Journal of cardiovascular pharmacology, 50(6), 629-632 (2007-12-20)
The effects of chronic oral azimilide therapy on the ventricular defibrillation threshold (DFT) during ischemia are unknown. The effects of azimilide on defibrillation efficacy under ischemic condition were investigated in a closed-chest animal model. Azimilide (20 mg/kg/d) was administered orally
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)
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
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
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
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