| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | 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]. Animal Model: | ||||||||||||
| Name | ASP2905 | ||||||||||||
| CAS | 792184-90-8 | ||||||||||||
| Formula | C20H17FN8 | ||||||||||||
| Molar Mass | 388.40 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |