498577-53-0

498577-53-0 structure

Name: AVE-0118
Chemical Name: 2-[2-[[[2-(4-methoxyphenyl)acetyl]amino]methyl]phenyl]-N-(2-pyridin-3-ylethyl)benzamide
CAS Number: 498577-53-0
Molecular Formula: C₃₀H₂₉N₃O₃
Molecular Weight: 479.57
Create Date: 2018-06-20 15:55:50
Modify Date: 2025-09-22 17:11:15
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].

Name	2-[2-[[[2-(4-methoxyphenyl)acetyl]amino]methyl]phenyl]-N-(2-pyridin-3-ylethyl)benzamide
Synonyms	unii-q1b712v03a ave-0118

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].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel
Target	IC50: 1.1 μM (Kv1.5), 3.4 uM (Ito), 4.5 uM (IKAch), 8.4 uM (IKr)[1]
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]。
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]。
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.