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Simufilam hydrochloride

CAS No. : 2480226-07-9

MCE 国际站：Simufilam hydrochloride

产品活性：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。

研究领域：Others

作用靶点：Others

In Vitro: Simufilam (1 pM~1 nM) (hydrochloride) dose-dependently improves NMDA/glycine-induced Arc expression.
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.

In Vivo: 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.

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