AVE-0118 |
Catalog No.GC70456 |
AVE-0118 es un bloquekv1.5 no selectivo con un IC50 de 1.1 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 498577-53-0
Sample solution is provided at 25 µL, 10mM.
AVE-0118 is shown to be a Kv1.5 blocker (IC50 = 1.1 uM) with moderate selectivity versus Ito (3.4 uM), IKr (8.4 uM), and IKAch (4.5 uM) and good selectivity versus IKs, IK1, IKATP[1].
AVE-0118 (10 μM) significantly potentiates the electrical field stimulation (EFS)-induced neurogenic type of contractions[2].
AVE-0118 reduces the inducibility of AF in goats with remodeled atria at a dose of 3 mg/kg and did not prolong QTc up to 5 mg/kg[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.
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