Simufilam (PTI-125) (hydrochloride) 是一种低毒的，具有口服活性的 filamin A (FLNA) 激活剂。Simufilam (hydrochloride) 可优先结合改变的 FLNA，并恢复其天然构象，恢复受体和突触活性，并减少其与 a7nAChR/TLR4 的关联和下游病理作用。Simufilam (hydrochloride) 可用于阿尔茨海默症的研究。
货号:ajcx35200
CAS:2480226-07-9
分子式:C15H22ClN3O
分子量：295.81
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Simufilam (PTI-125) (hydrochloride) is a low toxicity, orally active filamin A (FLNA) activator. Simufilam (hydrochloride) preferentially binds altered FLNA and restores its native conformation, restores receptor and synaptic activities, reduces its a7nAChR/TLR4 associations and downstream pathologies. Simufilam (hydrochloride) can be used for the research of Alzheimer’s disease[1].

Simufilam (1 pM~1 nM) (hydrochloride) dose-dependently improves NMDA/glycine-induced Arc expression[1].Simufilam (1 nM, 1 hour) (hydrochloride) largely restores filamin A to its native conformation and is effective in normalizing receptor activities in AD frontal cortices. Simufilam (hydrochloride) dose-dependently reduces Ab42-induced FLNA coupling to a7nAChR and TLR4 in both Ab42-treated control and AD hippocampus. Simufilam (hydrochloride) reduces Ab42’s binding affinity for a7nAChR, thereby prevents Ab42’s signaling and further accumulation on a7nAChRs[1].

Simufilam (P.o.; 2 months) (hydrochloride) restores FLNA to its native conformation. Simufilam (22 mg/kg; p.o.) (hydrochloride) robustly reduces FLNAea7nAChR/TLR4 associations. Simufilam (hydrochloride) significantly improves spatial memory. Simufilam (hydrochloride) significantly improves working memory[1].

[1]. Wang HY, et al. PTI-125 binds and reverses an altered conformation of filamin A to reduce Alzheimer’s disease pathogenesis. Neurobiol Aging. 2017;55:99-114.