| Bioactivity | 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[1]. |
| Invitro | 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]. |
| In Vivo | 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]. Animal Model: |
| Name | Ibutilide |
| CAS | 122647-31-8 |
| Formula | C20H36N2O3S |
| Molar Mass | 384.58 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. [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. [3]. S S Chugh, et al. Altered response to Ibutilide in a heart failure model. Cardiovasc Res. 2001 Jan;49(1):94-102. |
Ibutilide
CAS: 122647-31-8 F: C20H36N2O3S W: 384.58
Ibutilide (U70226E free base), an action potential-prolonging antiarrhythmic, is a potent blocker of the rapidly activat
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