Simufilam dihydrochloride
Names
[ CAS No. ]:
2480226-06-8
[ Name ]:
Simufilam dihydrochloride
Biological Activity
[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].
[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]
Chemical & Physical Properties
[ Molecular Formula ]:
C15H23Cl2N3O
[ Molecular Weight ]:
332.27
[ Storage condition ]:
-20°C