Ibutilide Fumarate

Research use only, not for human use.

Ibutilide Fumarate is the fumarate salt form of ibutilide, a class III antiarrhythmic agent. Ibutilide exerts its effect by activating a slow, inward, predominately sodium current rather than by blocking outward potassium currents.

Ibutilide is a Class III antiarrhythmic agent that is indicated for acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm. It exerts its antiarrhythmic effect by induction of slow inward sodium current, which prolongs action potential and refractory period (physiology) of myocardial cells.(In Vitro):Ibutilide fumarate is a potent IKr blocker with an EC50 value of 20 nM at +20 mV in atrial tumor myocytes (AT-1) cells.Ibutilide fumarate blocks IKr in cells expressing HERG+MDR1*1 to the same extent as cells expressing HERG alone (IC50: 22.5 nM vs 27.4 nM). However, cells expressing MDR1*7 show a marked resistance to Ibutilide (IC50: 105.3 nM vs 27.4 nM).(In Vivo):Ibutilide fumarate prolongs cardiac repolarization in vitro and in vivo.Ibutilide (administered cumulatively in three doses, 0.01, 0.02 and 0.05 mg/kg i.v., each as a 10-min infusion) fumarate results in both polymorphic and monomorphic non-sustained ventricular tachycardia.

Ibutilide fumarate is a potent IKr blocker with an EC50 value of 20 nM at +20 mV in atrial tumor myocytes (AT-1) cells. Ibutilide fumarate blocks IKr in cells expressing HERG+MDR1*1 to the same extent as cells expressing HERG alone (IC50: 22.5 nM vs 27.4 nM). However, cells expressing MDR1*7 show a marked resistance to Ibutilide (IC50: 105.3 nM vs 27.4 nM).

Ibutilide fumarate prolongs cardiac repolarization in vitro and in vivo.Ibutilide (administered cumulatively in three doses, 0.01, 0.02 and 0.05 mg/kg i.v., each as a 10-min infusion) fumarate results in both polymorphic and monomorphic non-sustained ventricular tachycardia. Animal Model:Fifteen adult mongrel dogs of either sex Dosage:0.01, 0.02 and 0.05 mg/kg Administration:Intravenous injection; each as a 10-min infusion Result:The action potential duration at 90% (APD90) prolongation with Ibutilide (0.01 mg/kg) was significantly greater in congestive heart failure (CHF) vs. controls. An increased dispersion of left-right ventricular APD90 was observed in CHF at 0.01 mg/kg, but not in controls.

Ibutilide, Corvert, Ibutilida, Ibutilidum

Immunology/Inflammation

Antiviral

Sodium Channel

Cardiovascular Disease

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122647-32-9

885.23

(C20H36N2O3S)2·C4H4O4

>98% (HPLC)

DMSO : ≥ 50 mg/mL 112.97 mM; H2O : 50 mg/mL 112.97 mM

CCCCCCCN(CC)CCCC(C1=CC=C(C=C1)NS(=O)(=O)C)O.CCCCCCCN(CC)CCCC(C1=CC=C(C=C1)NS(=O)(=O)C)O.C(=C/C(=O)O)\C(=O)O

N-[4-[4-[ethyl(heptyl)amino]-1-hydroxybutyl]phenyl]methanesulfonamide

(-20℃)

With Ice Pack

≥ 2 years