| Name | BIA 10-2474 |
| Description | BIA 10-2474 is a long-acting reversible inhibitor of fatty acid amide hydrolase (FAAH) that increases levels of the neurotransmitter anandamide in the central nervous system and in peripheral tissues (that is, the rest of the body other than the brain and spinal cord). BIA 10-2474(BIA10-2474) interacts with the human endocannabinoid system. BIA 10-2474(BIA10-2474) was in development for the treatment of a range of different medical conditions from anxiety to Parkinson's disease, also for the treatment of chronic pain of multiple sclerosis, Y, hypertension or the treatment of obesity. |
| In vitro | ExVivo: BIA 10-2474 is a potent FAAH inhibitor with IC50 values of 52 mg/kg (cerebellum), 67 mg/kg (rest of brain), 68 mg/kg (cortex), and 71 mg/kg (hypothalamus), and 50-70 mg/kg (i.p.) in various brain regions [1]. |
| In vivo | In January 2016, a Phase I clinical trial involving the drug BIA 10-2474 experienced severe adverse events (SAE), including a fatality. Investigations into the trial's failure will explore various potential causes, such as off-target effects, miscalculated dosage, unforeseen immune responses, interspecies variability, and cumulative dose toxicity[2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 4 mg/mL (13.3 mM)
|
| Keywords | Inhibitor | inhibit | Fatty acid amide hydrolase | FAAH | BIA 10-2474 | BIA 102474 | BIA 10 2474 | Autophagy |
| Inhibitors Related | Stavudine | Aceglutamide | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Valproic Acid | Curcumin | Paeonol | Naringin | Salicylic acid | Gefitinib |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Anti-Neurodegenerative Disease Compound Library | ReFRAME Related Library | Autophagy Compound Library | Anti-Parkinson's Disease Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | NO PAINS Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max |
United States
