IbutilideIbutilide
MedChemExpress (MCE)
HY-B0387A
122647-31-8
U70226E free base
98.98%
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Room temperature in continental US
may vary elsewhere.
Ibutilide (U70226E free base), an action potential-prolonging antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K+ current (IKr) in AT-1 cells.
Ibutilide is a potent IKr blocker with an EC50 value of 20 nM at +20 mV in atrial tumor myocytes (AT-1) cells[1]. Ibutilide 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)[2].
Ibutilide prolongs cardiac repolarization in vitro and in vivo[1]. Ibutilide infusions (administered cumulatively in three doses, 0.01, 0.02 and 0.05 mg/kg i.v., each as a 10-min infusion) results in both polymorphic and monomorphic non-sustained ventricular tachycardia[3].
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[1]. Ibutilide, a methanesulfonanilide antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K+ current (IKr) in AT-1 cells. Concentration-, time-, voltage-, and use-dependent effects. Circulation. 1995 Mar 15
91(6):1799-806. [Content Brief]
[2]. B F McBride, et al. Influence of the G2677T/C3435T haplotype of MDR1 on P-glycoprotein trafficking and Ibutilide-induced block of HERG. Pharmacogenomics J. 2009 Jun
9(3):194-201. [Content Brief]
[3]. S S Chugh, et al. Altered response to Ibutilide in a heart failure model. Cardiovasc Res. 2001 Jan
49(1):94-102. [Content Brief]