[CAS NO. 1233855-46-3] BIA10-2474
PRODUCTS SPECIFICATIONS [1233855-46-3]
DESCRIPTION [1233855-46-3]
Overview
| MDL | MFCD30532661 |
|---|---|
| Molecular Weight | 300.36 |
| Molecular Formula | C16H20N4O2 |
| SMILES | O=C(N1C=C(C2=C[N+]([O-])=CC=C2)N=C1)N(C3CCCCC3)C |
1 Publications Citing Use of MCE
Summary
BIA 10-2474 is an inhibitor of fatty acid amide hydrolase ( FAAH ) with IC 50 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 IC 50 s of 50-70mg/kg (i.p.) in various brain regions. IC 50 values for brain regions are 52 (cerebellum), 67 (rest of brain), 68 (cortex), and 71 mg/kg (hypothalamus) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 2.2 mg/mL ( 7.32 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.3293 mL | 16.6467 mL | 33.2934 mL |
| 5 mM | 0.6659 mL | 3.3293 mL | 6.6587 mL |
| 10 mM | --- | --- | --- |
References
- [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
Synonyms
