Ibutilide Fumarate

SKU: orb1222801

Description

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.

Key Properties

• CAS Number: 122647-32-9
• MW: 885.23
• Purity: >98% (HPLC)
• Formula: (C₂₀H₃₆N₂O₃S)2·C₄H₄O₄
• SMILES: 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
• Target: Antiviral
• Solubility: DMSO : ≥ 50 mg/mL 112.97 mM; H2O : 50 mg/mL 112.97 mM

Bioactivity

• 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. 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.
• 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).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ibutilide, Corvert, Ibutilida, Ibutilidum

Quick Database Links

Gene Symbol

Antiviral