AVE-0118

Names

[ Name ]:
AVE-0118

[Synonym ]:
unii-q1b712v03a
ave-0118

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₀H₂₉N₃O₃

[ Molecular Weight ]:
479.57

[ Exact Mass ]:
479.22100

[ PSA ]:
87.30000

[ LogP ]:
6.00370

Related Compounds

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