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AZIMILIDE

AZIMILIDE Structure
CAS No.
149908-53-2
Chemical Name:
AZIMILIDE
Synonyms
NE-10064;AZIMILIDE;Unii-74qu6p2934;AZIMILIDE USP/EP/BP;Azimilide (NE-10064);1-(((5-(4-Chlorophenyl)furan-2-yl)methylene)amino)-3-(4-(4-methylpiperazin-1-yl)butyl)imidazolidine-2,4-dione;1-[[[5-(4-Chlorophenyl)-2-furanyl]methylene]amino]-3-[4-(4-methyl-1-piperazinyl)butyl]-2,4-imidazolidinedione;2,4-Imidazolidinedione, 1-(((5-(4-chlorophenyl)-2-furanyl)methylene)amino)-3-(4-(4-methyl-1-piperazinyl)butyl)-
CBNumber:
CB0197878
Molecular Formula:
C23H28ClN5O3
Molecular Weight:
457.95
MOL File:
149908-53-2.mol
MSDS File:
SDS
Modify Date:
2023/5/18 11:31:13

AZIMILIDE Properties

Boiling point 594.9±60.0 °C(Predicted)
Density 1.32
storage temp. 2-8°C
solubility <4.58mg/mL in DMSO
form Powder
pka 7.72±0.10(Predicted)

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P280-P305+P351+P338

AZIMILIDE Chemical Properties,Uses,Production

Uses

Cardiac depressant (anti-arrhythmic).

General Description

Azimilide, E-1-[[[5-(4-chlorophenyl)-2-furanyl]methylene]amino]-3-[4-(4-methyl-1-piperazinyl)butyl]-2,4-imidazolidinedione, is a class III agent that significantlyblocks the delayed rectifier potassium current,Iks, including the Ikr component. Its ability to block multichannelsmay be caused by a lack of the methane sulfonamidegroup that is common to other class III agents, whichselectively block the Ikr potassium current. It is believedthat blocking both Ikr and Iks potassium currents yields consistentclass III antiarrhythmic effects at any heart rate.

Clinical Use

Azimilde is another Class III antiarrhythmic agent structurally unrelated to any of the above agents. Azimilide is not available in the United States; it is only available in Europe. Following oral administration, the drug is completely absorbed, with no effect of food. Protein binding is 94%. It is metabolized in the liver to an active carboxylate metabolite, but its concentration in plasma is less than 5% of the parent compound. Thus, it is considered to be therapeutically inactive. Renal excretion is approximately 10%. Its elimination half-life is 3 to 4 days.

Enzyme inhibitor

This class ΙΙΙ antiarrhythmic drug and ion channel blocker (FW = 457.95 g/mol; CAS 149908-53-2), also known by the code name NE-10064 and systematic name, 1-({(E)-[5-(4-chlorophenyl)furan-2-yl]methylidene} amino)-3-[4-(4-methylpiperazin-1-yl)butyl]-imidazolidine-2,4-dione, blocks both the slow-activating IKs and rapidly activating IKr components of the delayed rectifier potassium current, distinguishing its action from conventional potassium channel blockers such as sotalol and dofetilide,which block only IKr. Azimilide prolongs the cardiac refractory period in a dose-dependent manner, as manifested by increases in action potential duration, QTc interval, and effective refractory period.

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AZIMILIDE Spectrum

AZIMILIDE 1-[[[5-(4-Chlorophenyl)-2-furanyl]methylene]amino]-3-[4-(4-methyl-1-piperazinyl)butyl]-2,4-imidazolidinedione NE-10064 2,4-Imidazolidinedione, 1-(((5-(4-chlorophenyl)-2-furanyl)methylene)amino)-3-(4-(4-methyl-1-piperazinyl)butyl)- Unii-74qu6p2934 AZIMILIDE USP/EP/BP Azimilide (NE-10064) 1-(((5-(4-Chlorophenyl)furan-2-yl)methylene)amino)-3-(4-(4-methylpiperazin-1-yl)butyl)imidazolidine-2,4-dione 149908-53-2 140.9888-94-8 C23H28ClN5O3