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Ibutilide fumarate

CAS No. : 122647-32-9

MCE 国际站：Ibutilide fumarate

产品活性：Ibutilide (U70226E) fumarate 是一种延长动作电位的抗心律失常剂，作用于 AT-1 细胞，可有效阻断快激活延迟整流钾电流 (I_Kr)。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Potassium Channel

In Vitro: Ibutilide fumarate is a potent I_Kr blocker with an EC₅₀ value of 20 nM at +20 mV in atrial tumor myocytes (AT-1) cells.
Ibutilide fumarate blocks I_Kr 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.

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