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PQM130 Sale

目录号 : GC36954

PQM130是一种能透过大脑的、魏罗酮-多奈哌齐杂化化合物,是多靶点的候选药物,可用于Aβ1-42 低聚物引起的神经毒性,还具有抗炎活性。PQM130 是具有神经保护作用的、有潜力的抗 AD 药物。

PQM130 Chemical Structure

Cas No.:2089415-51-8

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产品描述

PQM130, a Feruloyl-Donepezil Hybrid compound with brain penatration, is a multitarget drug candidate against the neurotoxicity induced by Aβ1-42 oligomer (AβO) and shows anti-inflammatory activity. PQM130 acts as a neuroprotective compound for anti-AD drug development[1].

PQM130 (0.5-1 mg/kg, i.p., daily for 10 days) treatment after the i.c.v. AβO injection reduces oxidative damage and neuroinflammation and induces cell survival and protein synthesis through the modulation of GSK3β and extracellular signal-regulated kinases (ERK1/2) [1]. Animal Model: Adult male C57Bl/6 mice (9 weeks old, 25-30 g body weight) [1].

[1]. Morroni F, et al. PQM130, a Novel Feruloyl-Donepezil Hybrid Compound, Effectively Ameliorates the Cognitive Impairments and Pathology in a Mouse Model of Alzheimer's Disease. Front Pharmacol. 2019 Jun 12;10:658.

Chemical Properties

Cas No. 2089415-51-8 SDF
Canonical SMILES O=C(OCC1CCN(CC2=CC=CC=C2)CC1)/C=C/C3=CC=C(O)C(OC)=C3
分子式 C23H27NO4 分子量 381.46
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mM 2.6215 mL 13.1075 mL 26.2151 mL
5 mM 0.5243 mL 2.6215 mL 5.243 mL
10 mM 0.2622 mL 1.3108 mL 2.6215 mL
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Research Update

PQM130, a Novel Feruloyl-Donepezil Hybrid Compound, Effectively Ameliorates the Cognitive Impairments and Pathology in a Mouse Model of Alzheimer's Disease

Front Pharmacol 2019 Jun 12;10:658.PMID:31244664DOI:PMC6581760

Alzheimer's disease (AD) is the most frequent type of dementia in older people. The complex nature of AD calls for the development of multitarget agents addressing key pathogenic processes. Donepezil, an acetylcholinesterase inhibitor, is a first-line acetylcholinesterase inhibitor used for the treatment of AD. Although several studies have demonstrated the symptomatic efficacy of donepezil treatment in AD patients, the possible effects of donepezil on the AD process are not yet known. In this study, a novel feruloyl-donepezil hybrid compound (PQM130) was synthesized and evaluated as a multitarget drug candidate against the neurotoxicity induced by Aβ1-42 oligomer (AβO) injection in mice. Interestingly, PQM130 had already shown anti-inflammatory activity in different in vivo models and neuroprotective activity in human neuronal cells. The intracerebroventricular (i.c.v.) injection of AβO in mice caused the increase of memory impairment, oxidative stress, neurodegeneration, and neuroinflammation. Instead, PQM130 (0.5-1 mg/kg) treatment after the i.c.v. AβO injection reduced oxidative damage and neuroinflammation and induced cell survival and protein synthesis through the modulation of glycogen synthase kinase 3β (GSK3β) and extracellular signal-regulated kinases (ERK1/2). Moreover, PQM130 increased brain plasticity and protected mice against the decline in spatial cognition. Even more interesting is that PQM130 modulated different pathways compared to donepezil, and it is much more effective in counteracting AβO damage. Therefore, our findings highlighted that PQM130 is a potent multi-functional agent against AD and could act as a promising neuroprotective compound for anti-AD drug development.