Name | Simufilam dihydrochloride |
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Description | Simufilam (PTI-125) dihydrochloride is a low toxicity, orally active filamin A (FLNA) activator. Simufilam dihydrochloride preferentially binds altered FLNA and restores its native conformation, restores receptor and synaptic activities, reduces its a7nAChR/TLR4 associations and downstream pathologies. Simufilam dihydrochloride can be used for the research of Alzheimer's disease[1]. |
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Related Catalog | |
Target |
FLNA[1] |
In Vitro | Simufilam dihydrochloride (1 pM~1 nM) dose-dependently improves NMDA/glycine-induced Arc expression[1]. Simufilam dihydrochloride (1 nM, 1 hour) largely restores filamin A to its native conformation and is effective in normalizing receptor activities in AD frontal cortices. Simufilam dihydrochloride dose-dependently reduces Ab42-induced FLNA coupling to a7nAChR and TLR4 in both Ab42-treated control and AD hippocampus. Simufilam dihydrochloride reduces Ab42's binding affinity for a7nAChR, thereby prevents Ab42's signaling and further accumulation on a7nAChRs[1]. |
In Vivo | Simufilam dihydrochloride (P.o.; 2 months) restores FLNA to its native conformation. Simufilam dihydrochloride (22 mg/kg; p.o.) robustly reduces FLNAea7nAChR/TLR4 associations. Simufilam dihydrochloride significantly improves spatial memory. Simufilam significantly improves working memory[1]. |
References |
Molecular Formula | C15H23Cl2N3O |
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Molecular Weight | 332.27 |
Storage condition | -20°C |