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Key Documents

SML0353

Sigma-Aldrich

Azimilide dihydrochloride

≥97% (HPLC)

Synonyma:

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

Přihlásitk zobrazení cen stanovených pro organizaci a smluvních cen


About This Item

Empirický vzorec (Hillův zápis):
C23H28ClN5O3 · 2HCl
Číslo CAS:
Molekulová hmotnost:
530.88
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77

assay

≥97% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 1 mg/mL, clear (warmed)

storage temp.

2-8°C

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

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 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.

pictograms

Skull and crossbones

signalword

Danger

hcodes

Hazard Classifications

Acute Tox. 3 Oral

Storage Class

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

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Navštívit knihovnu dokumentů

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
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
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
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
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

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