ASP2905 是由 Kcnh3/BEC1 基因编码的有效且选择性的钾通道 Kv12.2 抑制剂。ASP2905 可以穿越血脑屏障并具有抗精神病活性。
货号:ajcx32788
CAS:792184-90-8
分子式:C20H17FN8
分子量：388.4
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

ASP2905 is a potent and selective potassium channel Kv12.2 inhibitor encoded by the Kcnh3/BEC1 gene. ASP2905 can cross the blood-brain barrier and has antipsychotic activities[1][2].

ASP2905 potently inhibits potassium currents in CHO cells expressing KCNH3 (IC50 of 9.0 nM). ASP2905 (≤10 µM) minimally bound with low affinities to 55 transmembrane proteins. ASP2905 (0.1 µM, 1 µM) decreases the frequency of spontaneous inhibitory postsynaptic currents in cultured rat hippocampal neurons[1].

ASP2905 treatment inhibits hyperlocomotion induced by Phencyclidine. And significantly ameliorates Phencyclidine-induced prolongation of immobility time in mice subjected to the forced swimming test[2].

参考文献:
[1]. Shinji Takahashi, et al. Neurochemical and neuropharmacological characterization of ASP2905, a novel potent selective inhibitor of the potassium channel KCNH3. Eur J Pharmacol. 2017 Sep 5;810:26-35.
[2]. Shinji Takahashi, et al. ASP2905, a specific inhibitor of the potassium channel Kv12.2 encoded by the Kcnh3 gene, is psychoactive in mice. Behav Brain Res. 2020 Jan 27;378:112315.