Azimilide

Azimilide (NE-10064) is a class III antiarrhythmic agent, which works by blocking potassium channels in the heart. Azimilide is a dual blocker of IKs (IC50 = 2.6 μM (2mM [K⁺]ₑ) ) and IKr (IC50 = 1 μM (4 mM [K⁺]) ) . Azimilide blocked HERG channel at 0.1 and 1 Hz with IC50s of 1.4 μM and 5.2 μM respectively. Azimilide also inhibits L-type calcium current (ICa) (IC50 = 17.8 μM) and sodium current (INa) (IC50 = 19 μM) . Azimilide can be used for the study of atrial fibrillation and ventricular fibrillation[1][2][3][4].

Product Specifications

CAS Number

149908-53-2

Product Name Alternative

NE-10064

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Calcium Channel; Potassium Channel; Sodium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/Azimilide.html

Purity

99.01

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

O=C1N(CCCCN2CCN(C)CC2)C(CN1/N=C/C3=CC=C(C4=CC=C(Cl)C=C4)O3)=O

Molecular Formula

C23H28ClN5O3

Molecular Weight

457.95

Precautions

H302, H315, H319, H335

References & Citations

[1]Busch AE, et al. Blockade of HERG channels by the class III antiarrhythmic azimilide: mode of action. Br J Pharmacol. 1998 Jan;123 (1) :23-30.|[2]Yao JA, et al. Azimilide (NE-10064) can prolong or shorten the action potential duration in canine ventricular myocytes: dependence on blockade of K, Ca, and Na channels. J Cardiovasc Electrophysiol. 1997 Feb;8 (2) :184-98.|[3]Fermini B, et al. Use-dependent effects of the class III antiarrhythmic agent NE-10064 (azimilide) on cardiac repolarization: block of delayed rectifier potassium and L-type calcium currents. J Cardiovasc Pharmacol. 1995 Aug;26 (2) :259-71.|[4]Black SC, et al. Protection against programmed electrical stimulation-induced ventricular tachycardia and sudden cardiac death by NE-10064, a class III antiarrhythmic drug. J Cardiovasc Pharmacol. 1993 Dec;22 (6) :810-8.