Simufilam

Modify Date: 2024-01-08 22:53:04

Simufilam Structure
Simufilam structure
Common Name Simufilam
CAS Number 1224591-33-6 Molecular Weight 259.35
Density N/A Boiling Point N/A
Molecular Formula C15H21N3O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Simufilam


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

 Names

Name Simufilam

 Simufilam Biological Activity

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

FLNA[1]

In Vitro Simufilam (1 pM~1 nM) dose-dependently improves NMDA/glycine-induced Arc expression[1]. Simufilam (1 nM, 1 hour) largely restores filamin A to its native conformation and is effective in normalizing receptor activities in AD frontal cortices. Simufilam dose-dependently reduces Ab42-induced FLNA coupling to a7nAChR and TLR4 in both Ab42-treated control and AD hippocampus. Simufilam reduces Ab42's binding affinity for a7nAChR, thereby prevents Ab42's signaling and further accumulation on a7nAChRs[1].
In Vivo Simufilam (P.o.; 2 months) restores FLNA to its native conformation. Simufilam (22 mg/kg; p.o.) robustly reduces FLNAea7nAChR/TLR4 associations. Simufilam significantly improves spatial memory. Simufilam significantly improves working memory[1].
References

[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.

 Chemical & Physical Properties

Molecular Formula C15H21N3O
Molecular Weight 259.35
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