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Azimilide-d8 (dihydrochloride)

Azimilide-d8 (NE-10064-d8) dihydrochloride is the deuterium labeled Azimilide dihydrochloride. Azimilide dihydrochloride is a class III antiarrhythmic agent, which works by blocking potassium channels in the heart. Azimilide dihydrochloride is a dual blocker of IKs (IC50 = 2.6 μM (2mM [K⁺]ₑ) ) and IKr (IC50 = 1 μM (4 mM [K⁺]) ). Azimilide dihydrochloride blocked HERG channel at 0.1 and 1 Hz with IC50s of 1.4 μM and 5.2 μM respectively. Azimilide dihydrochloride also inhibits L-type calcium current (ICa) (IC50 = 17.8 μM) and sodium current (INa) (IC50 = 19 μM). Azimilide dihydrochloride can be used for the study of atrial fibrillation and ventricular fibrillation[1][2][3][4].

Product Specifications

Product Name Alternative

NE-10064-d8 (dihydrochloride)

UNSPSC

12352005

Target

Calcium Channel; Isotope-Labeled Compounds; Potassium Channel; Sodium Channel

Type

Isotope-Labeled Compounds

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling; Others

Field of Research

Cardiovascular Disease

Solubility

10 mM in DMSO

Smiles

O=C1N(/N=C/C2=CC=C(O2)C3=CC=C(C=C3)Cl)CC(N1CCCCN4C([2H])(C([2H])(N(C)C([2H])(C4([2H])[2H])[2H])[2H])[2H])=O.[2HCl]

Molecular Formula

C23H22D8Cl3N5O3

Molecular Weight

538.92

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]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.|[3]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.|[4]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.|[5]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.

Shipping Conditions

Room temperature

Scientific Category

Isotope-Labeled Compounds

Clinical Information

No Development Reported

Available Sizes

Frequently Asked Questions

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