| Bioactivity | 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. | ||||||||||||
| Target | IC50: 50-70mg/kg (FAAH, rat brain regions) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | BIA 10-2474 | ||||||||||||
| CAS | 1233855-46-3 | ||||||||||||
| Formula | C16H20N4O2 | ||||||||||||
| Molar Mass | 300.36 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Tong J, et al. Inhibition of fatty acid amide hydrolase by BIA 10-2474 in rat brain. J Cereb Blood Flow Metab. 2016 Sep 20. [2]. Kaur R, et al. What failed BIA 10-2474 Phase I clinical trial? Global speculations and recommendations for future Phase I trials. J Pharmacol Pharmacother. 2016 Jul-Sep;7(3):120-6 |
BIA 10-2474
CAS: 1233855-46-3 F: C16H20N4O2 W: 300.36
BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC50 values of 50 to 70mg/kg in various rat brain
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