BIA 10-2474

1233855-46-3

C16H20N4O2

DMSO : 6.4 mg/mL (21.31 mM; Need ultrasonic and warming)

Neuronal Signaling; Metabolic Enzyme/Protease

BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC₅₀ values of 50 to 70mg/kg in various rat brain regions. IC50 & Target: IC50: 50-70mg/kg (FAAH, rat brain regions)^[1] In Vitro: ExVivo: BIA 10-2474 proves to be a potent FAAH inhibitor with IC₅₀s of 50-70mg/kg (i.p.) in various brain regions. IC₅₀ values for brain regions are 52 (cerebellum), 67 (rest of brain), 68 (cortex), and 71 mg/kg (hypothalamus)^[1]. In Vivo: In January 2016, severe adverse events (SAE) occurs in the Phase I clinical trial using the drug BIA 10-2474 including one death. The possibilities for failure of trials such as off-target effect, dose calculation, unexpected immune response, species variation, and cumulative dose toxicity would be sought^[2].