ASP 2905

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种新型有效、选择性、口服生物可利用的电压门控钾通道 KCNH3 抑制剂，IC50 为 9.0 nM。

A novel potent, selective, orally bioavailable inhibitor of voltage-gated potassium channel KCNH3 with IC50 of 9.0 nM; displays minimally bound with low affinities to 55 transmembrane proteins; decreases the frequency of spontaneous inhibitory postsynaptic currents in cultured rat hippocampal neurons at 0.1-1 uM; reverses the disruption of spontaneous alternation behavior induced by MK-801 and scopolamine in mice, and ameliorates the cognitive deficits of aged rats.Alzheimer Disease Phase 1 Discontinued.

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.

ASP2905 treatment inhibits hyperlocomotion induced by Phencyclidine. And significantly ameliorates Phencyclidine-induced prolongation of immobility time in mice subjected to the forced swimming test. Animal Model:Male ddY mice (aged 4-5 weeks) injected with Phencyclidine hydrochloride (PCP) Dosage:0.01 mg/kg, 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg Administration:Oral administration; once Result:Inhibited hyperlocomotion induced by Phencyclidine.

ASP2905 | ASP-2905

Cell Cycle/DNA Damage

Potassium Channel

Potassium Channel

Neurological Disease

Alzheimer Disease

792184-90-8

388.41

C20H17FN8

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (257.47 mM)

FC(C=C1)=CC=C1NC2=NC(NC3=CC=CC=C3)=NC(NCC4=NC=CC=N4)=N2.Cl

N-(4-fluorophenyl)-N'-phenyl-N''-(pyrimidin-2-ylmethyl)-1,3,5-triazine-2,4,6-triamine

(-20℃)

With Ice Pack

≥ 2 years