| Name | ASP2905 |
| Description | ASP-2905 is a potent and selective inhibitor of potassium channel Kv12.2 encoded by the Kcnh3/BEC1 gene. It can cross the blood-brain barrier and has antipsychotic activities |
| In vitro | ASP2905 (0.1 M, 1 M) decreased the frequency of spontaneous inhibitory postsynaptic currents in cultured rat hippocampal neurons.?In mice, ASP2905 reversed the disruption of spontaneous alternation behavior induced by MK-801 and scopolamine (minimum effective dose of ASP2905: 0.0625mg/kg, po).?ASP2905 ameliorated the cognitive deficits of aged rats in step-through passive avoidance (0.0313 and 0.0625mg/kg, po) and Morris water-maze tasks (0.01mg/kg, po) and effectively penetrated the brain.?The mean plasma and brain concentrations of ASP2905 reached their maxima (Cmax = 0.399ng/ml and 1.77ng/g, respectively) 1h after a single oral administration and then decreased (t1/2 = 1.5-1.6h) (brain plasma ratio = 2.7-4.9).?ASP2905 is a selective, orally administered inhibitor of KCNH3, which can enhance cognitive performance[1]. |
| In vivo | ASP2905 on channel activity in vitro and its neuropharmacological properties in young and aged rats as well as in mice.?ASP2905 potently inhibited potassium currents in CHO cells expressing KCNH3 (IC50 = 9.0nM).?In contrast, ASP2905 ( 10μM) minimally bound with low affinities to 55 transmembrane proteins.[1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.15 mM), Sonication is recommended.
DMSO : 27.5 mg/mL (70.8 mM), Sonication is recommended.
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| Keywords | PotassiumChannel | Potassium Channel | Kv12.2 | KcsA | Kcnh3 | Inhibitor | inhibit | cognitive | CNS | ASP2905 | ASP 2905 | antipsychotic |
| Inhibitors Related | Minoxidil sulfate | Tannic acid | Hydrochlorothiazide | (±)-Naringenin | Tetraethylammonium bromide | Halothane | Butamben | Ursodeoxycholic acid | Cloperastine hydrochloride | Minoxidil | Nifedipine | Indapamide |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | CNS-Penetrant Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Potassium Channel Targeted Library | Ion Channel Targeted Library | Anti-Cancer Compound Library |
United States
