AVE-0118
Names
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]:
[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]
Chemical & Physical Properties
[ Molecular Formula ]:
C30H29N3O3
[ Molecular Weight ]:
479.57
[ Exact Mass ]:
479.22100
[ PSA ]:
87.30000
[ LogP ]:
6.00370