ASP2905

ASP2905CAS号: 792184-90-8分子式: C20H17FN8分子量: 388.4描述纯度储存/保存方法可溶性/溶解性In vitro(体外研究)In vivo(体内研究)

产品描述
描述
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
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:27.5 mg/mL (70.8 mM)
生物活性
In vitro(体外研究)
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(体内研究)
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]