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.
Product information
CAS Number: 1224591-33-6
Molecular Weight: 259.35
Formula: C15H21N3O
Chemical Name: 1-benzyl-8-methyl-1,4,8-triazaspiro[4.5]decan-2-one
Smiles: CN1CCC2(CC1)NCC(=O)N2CC1C=CC=CC=1
InChiKey: BSQPTZYKCAULBH-UHFFFAOYSA-N
InChi: InChI=1S/C15H21N3O/c1-17-9-7-15(8-10-17)16-11-14(19)18(15)12-13-5-3-2-4-6-13/h2-6,16H,7-12H2,1H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Simufilam (1 pM~1 nM) dose-dependently improves NMDA/glycine-induced Arc expression. 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.
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.
Products are for research use only. Not for human use.
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