SML0353
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:
分子量:
530.88
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
SMILES string
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
assay
≥97% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 1 mg/mL, clear (warmed)
storage temp.
2-8°C
Quality Level
Application
Azimilide dihydrochloride may be used in the electrophysiology experiments with human ether-a-go-go-related gene 1a (HERG1a) subunit.
Biochem/physiol Actions
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.
Features and Benefits
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.
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Atsushi Nishida et al.
Journal of pharmacological sciences, 105(3), 229-239 (2007-10-30)
Effects of azimilide, a class III antiarrhythmic drug, on the acetylcholine (ACh) receptor-operated K+ current (I K.ACh) and the delayed rectifier K+ current (IK) were examined in guinea-pig atrial cells using patch-clamp techniques. Effects of azimilide on experimental atrial fibrillation
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
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
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
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