| Name | Simufilam dihydrochloride |
| Description | Simufilam dihydrochloride (PTI-125 dihydrochloride) is a low toxicity, orally active filamin A (FLNA) activator, which can be used for the research of Alzheimer's disease. Simufilam dihydrochloride preferentially binds altered FLNA and restores its native conformation, restoring receptor and synaptic activities and reducing its α7nAChR/TLR4 associations and downstream pathologies. |
| In vitro | Simufilam dihydrochloride (1 pM~1 nM) increases NMDA/glycine-induced Arc expression in a dose-dependent manner. Simufilam dihydrochloride (1 nM, 1 hour) largely restores filamin A to its native conformation and effectively normalizes 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. |
| In vivo | Simufilam dihydrochloride (22 mg/kg; p.o.) robustly reduces FLNAea7nAChR/TLR4 associations. Simufilam dihydrochloride significantly improves spatial memory. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 65 mg/mL (195.61 mM), Sonication is recommended.
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| Keywords | Simufilam dihydrochloride | Simufilam | PTI-125 Dihydrochloride | PTI125 Dihydrochloride | PTI-125 | PTI125 | PTI 125 Dihydrochloride | PTI 125 | Inhibitor | inhibit | a7nAChR |
| Inhibitors Related | Flubendazole | Urethane | Decanoic Acid | L-Glutamic acid | HEPPS | Adenine | Indole-2-carboxylic acid | Mitotane | Methylene Blue trihydrate | Methyl eugenol | N,N-Dicyclohexylcarbodiimide | Arecoline |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Neurotransmitter Receptor Compound Library | Drug Repurposing Compound Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library |
United States
