产品
编 号:F082135
分子式:C20H36N2O3S
分子量:384.58
产品类型
结构图
CAS No: 122647-31-8
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生物活性:
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.
体内研究:
Ibutilide prolongs cardiac repolarization in vitro and in vivo.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. 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 is a potent?IKr?blocker?with an EC50?value of 20 nM at +20 mV in atrial tumor myocytes (AT-1) cells. 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).