| Description |
AVE-0118 is a nonselective Kv1.5 blocker with an IC50 of 1.1 μM. AVE-0118 is a multichannel inhibitor with weak, micromolar activity against Kv1.5 and other ion channels. It is inactive against IKs, IKATP, and L-type Ca+ channels[1].
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| Related Catalog |
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| Target |
IC50: 1.1 μM (Kv1.5), 3.4 uM (Ito), 4.5 uM (IKAch), 8.4 uM (IKr)[1]
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| In Vitro |
AVE-0118 是一种 Kv1.5 阻滞剂 (IC50 = 1.1 uM)，对 Ito (3.4 uM)、IKr (8.4 uM) 和 IKAch (4.5 uM) 具有中等选择性，对IKs、IK1、IKATP 具有良好的选择性[1]。 AVE-0118 (10 μM) 显著增强电场刺激 (EFS) 诱导的神经源性收缩[2]。
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| In Vivo |
在 3 mg/kg 剂量下，AVE-0118 降低了心房重构山羊 AF 的诱导性，在 5mg/kg 也并没有延长 QTc[1]。
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| References |
[1]. Bilodeau MT, et al. Kv1.5 blockers for the treatment of atrial fibrillation: approaches to optimization of potency and selectivity and translation to in vivo pharmacology. Curr Top Med Chem. 2009;9(5):436-51. [2]. Kun A, et al. Neurogenic contraction induced by the antiarrhythmic compound, AVE 0118, in rat small mesenteric arteries. Basic Clin Pharmacol Toxicol. 2014 Oct;115(4):315-20.
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