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Merck

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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About This Item

经验公式(希尔记法):
C23H28ClN5O3 · 2HCl
分子量:
530.88
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

品質等級

化驗

≥97% (HPLC)

形狀

powder

儲存條件

desiccated

顏色

white to beige

溶解度

DMSO: 1 mg/mL, clear (warmed)

儲存溫度

2-8°C

SMILES 字串

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 密鑰

SUHOTCCGXXEWJN-DSHYBBOZSA-N

應用

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 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.

特點和優勢

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.

象形圖

Skull and crossbones

訊號詞

Danger

危險聲明

危險分類

Acute Tox. 3 Oral

儲存類別代碼

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

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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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)
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
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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