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Simufilam (Synonyms: PTI-125)

Cat. No.: HY-139142
Handling Instructions

Simufilam (PTI-125) is a safe, orally active small molecule that preferentially binds altered filamin A (FLNA) and restores its native conformation, restoring receptor and synaptic activities and reducing its a7nAChR/TLR4 associations and downstream pathologies. Simufilam can be used for the research of Alzheimer's disease.

For research use only. We do not sell to patients.

Simufilam Chemical Structure

Simufilam Chemical Structure

CAS No. : 1224591-33-6

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Description

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

IC50 & 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 reduced 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 preventing Ab42’s signaling and further accumulation on a7nAChRs[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line:
Concentration: 1 pM~1 nM
Incubation Time:
Result: Dose-dependently improved NMDA/glycine-induced Arc expression.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

259.35

Formula

C₁₅H₂₁N₃O

CAS No.
SMILES

O=C1N(CC2=CC=CC=C2)C3(CCN(C)CC3)NC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

SimufilamPTI-125PTI125PTI 125Otherssafeorallysmall-moleculealtereda7nAChR/TLR4pathologiesInhibitorinhibitorinhibit

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Simufilam
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