Memoquin

Memoquin is an anti-amyloid and anti-oxidant multi-target-directed ligand. Memoquin is an orally active inhibitor of BACE-1 and AChE with IC50 values of 108 and 1.55 nM, respectively. Memoquin is a cognitive enhancer that prevents the Aβ-induced neurotoxicity mediated by oxidative stress. Memoquin can be used for the research of Alzheimer’s disease (AD)[1][2].

Signaling Pathways >> Neuronal Signaling >> Beta-secretase

Research Areas >> Neurological Disease

Signaling Pathways >> Neuronal Signaling >> AChE

hAChE:1.55 nM (IC50)

BACE1:108 nM (IC50)

Memoquin 抑制 hAChE，hAChE 诱导的 Aβ(1-40) 聚集，Aβ(1-42) 自聚集和 BACE-1 的 IC50 值分别为 0.00155，28.3，5.93 和 0.108 μM[2]。 Memoquin 具有与 hAChE 结合的特性，Ki 值为 2.6 nM[2]。

Memoquin (7-15 mg/kg；口服，一次) 可挽救 scopolamine 诱导的遗忘模型的记忆缺陷[1]。 Memoquin (15 mg/kg；口服，每天 1 次，连续 2-6 天) 6 天治疗可完全挽救 Aβ1-42 诱导的遗忘模型的记忆缺陷[1]。 Animal Model: Mice with scopolamine-induced amnesia[1] Dosage: 7, 10 and 15 mg/kg Administration: Oral administration; 7, 10 and 15 mg/kg, once Result: Reversed the scopolamine-induced memory deficits and verified by a T-maze test. Rescueed episodic memory impairment at a dose of 15 mg/kg. Animal Model: Mice with Aβ- induced amnesia[1] Dosage: 15 mg/kg Administration: Oral administration; 15 mg/kg, daily for 2, 4, and 6 days before behavioral testing Result: Weekly alleviated the insult induced by Aβ1-42 for 2-4 days treatment and fully rescued with a 6-day treatment.

[1]. Capurro V, et al. Pharmacological characterization of memoquin, a multi-target compound for the treatment of Alzheimer's disease. PLoS One. 2013;8(2):e56870.  

[2]. Cavalli A, et al. A small molecule targeting the multifactorial nature of Alzheimer's disease. Angew Chem Int Ed Engl. 2007;46(20):3689-92.