| 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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 65 mg/ml (195.61 mM)
|
| Keywords | PTI-125 Dihydrochloride | Simufilam | Inhibitor | PTI 125 Dihydrochloride | PTI-125 | inhibit | PTI 125 | PTI125 Dihydrochloride | Simufilam dihydrochloride | Simufilam Dihydrochloride | PTI125 |
| Inhibitors Related | Adiphenine hydrochloride | Nanofin | Forskolin | Pilocarpine Hydrochloride | (+)-Sparteine | Pilocarpine nitrate | CLOZAPINE N-OXIDE | Ribavirin | Adenine | Amitriptyline hydrochloride | Choline chloride | Propoxur |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Anti-Alzheimer's Disease Compound Library | Drug Repurposing Compound Library | NO PAINS Compound Library | Orally Active Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library |
United States
