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SML0353

Sigma-Aldrich

Azimilide dihydrochloride

≥97% (HPLC)

Sinonimo/i:

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

Formula empirica (notazione di Hill):
C23H28ClN5O3 · 2HCl
Numero CAS:
149888-94-8
Peso molecolare:
530.88
Codice UNSPSC:
12352200
ID PubChem:
329825356
NACRES:
NA.77

Saggio

≥97% (HPLC)

Forma fisica

powder

Condizioni di stoccaggio

desiccated

Colore

white to beige

Solubilità

DMSO: 1 mg/mL, clear (warmed)

Temperatura di conservazione

2-8°C

Stringa SMILE

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-;;
SUHOTCCGXXEWJN-DSHYBBOZSA-N

Applicazioni

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

Azioni biochim/fisiol

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.

Caratteristiche e vantaggi

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.

Pittogrammi

Skull and crossbones
GHS06

Avvertenze

Danger

Indicazioni di pericolo

H301

Classi di pericolo

Acute Tox. 3 Oral

Codice della classe di stoccaggio

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

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

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Yasuhide Watanabe et al.
Journal of pharmacological sciences, 114(1), 111-114 (2010-08-17)
We examined the effect of azimilide, a class III antiarrhythmic drug, on Na(+)/Ca(2+) exchange current (I(NCX)) in guinea-pig cardiac single ventricular cells. External application of azimilide suppressed bi-directional I(NCX) in a concentration-dependent manner. IC(50) values for outward and inward I(NCX)
Kazuharu Furutani et al.
Biochemical and biophysical research communications, 415(1), 141-146 (2011-10-25)
Nifekalant and azimilide, Class III antiarrhythmic agents, block the human ether-à-go-go-related gene K(+) (hERG) channel. However, when a depolarizing membrane potential is applied, they also increase the current at low potentials by shifting its activation curve towards hyperpolarizing voltages. This
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
Stefan H Hohnloser et al.
European heart journal, 27(24), 3027-3032 (2006-10-20)
The purpose of this study was to assess the incidence, features, and clinical sequelae of 'electrical storm' (ES). This study is a prospectively designed secondary analysis of SHIELD; a randomized trial of azimilide for suppression of ventricular tachycardia/fibrillation (VT/VF) leading
Emily Conway et al.
The American journal of cardiology, 102(6A), 12H-19H (2008-10-22)
Pharmacologic antiarrhythmic therapy is the most commonly used treatment in most patients with atrial fibrillation (AF), but currently available agents are limited by risks that may offset the benefits of sinus rhythm. The development of antiarrhythmic agents with the potential
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