A class III antiarrhythmic agent; blocks IKr and IKs currents in isolated guinea pig ventricular myocytes (IC50s = 0.3 and 3 μM

Azimilide (hydrochloride) – 100 mg

Brand:
Cayman
CAS:
149888-94-8
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Azimilide is a class III antiarrhythmic agent.{46367} It blocks rapidly activating delayed rectifier (IKr) and slowly activating delayed rectifier (IKs) potassium currents in isolated guinea pig ventricular myocytes (IC50s = 0.3 and 3 μM, respectively). Azimilide (0.1-10 μM) prolongs action potential duration (APD) in isolated calf Purkinje fibers and ventricular trabeculae in a concentration-dependent manner. It increases the effective refractory period (ERP) in isolated perfused guinea pig hearts and ferret papillary muscles. Azimilide (0.3-30 mg/kg) increases ERP and the absolute refractory period and decreases heart rate in dogs. It reduces mean arrhythmia score in a rat model of coronary artery ligation and reperfusion-induced severe ventricular arrhythmia. Azimilide (10-30 mg/kg) also prevents sustained and non-sustained ventricular tachyarrhythmias in dogs.  

 

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Description

A class III antiarrhythmic agent; blocks IKr and IKs currents in isolated guinea pig ventricular myocytes (IC50s = 0.3 and 3 μM, respectively); prolongs APD in isolated calf Purkinje fibers and ventricular trabeculae from 0.1-10 μM; increases the ERP in isolated perfused guinea pig hearts and ferret papillary muscles; increases ERP and the absolute refractory period and decreases heart rate in dogs from 0.3-30 mg/kg; reduces mean arrhythmia score in a rat model of coronary artery ligation and reperfusion-induced severe ventricular arrhythmia; prevents sustained and non-sustained ventricular tachyarrhythmias in dogs from 10-30 mg/kg

Formal name: 1-[[[5-(4-chlorophenyl)-2-furanyl]methylene]amino]-3-[4-(4-methyl-1-piperazinyl)butyl]-2,4-imidazolidinedione, dihydrochloride

Synonyms:  NE 10064

Molecular weight: 530.9

CAS: 149888-94-8

Purity: ≥95%

Formulation: A crystalline solid

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