产品
编 号:F082136
分子式:C24H40N2O7S
分子量:442.61
产品类型
结构图
CAS No: 122647-32-9
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生物活性:
Ibutilide (U70226E) fumarate, an action potential-prolonging antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K+ current (IKr) in AT-1 cells.
体内研究:
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.
体外研究:
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).