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.

Product information

CAS Number: 1233855-46-3

Molecular Weight: 300.36

Formula: C16H20N4O2

Chemical Name: 3-{1-[cyclohexyl(methyl)carbamoyl]-1H-imidazol-4-yl}pyridin-1-ium-1-olate

Smiles: CN(C1CCCCC1)C(=O)N1C=C(N=C1)C1=C[N+]([O-])=CC=C1

InChiKey: DOWVMJFBDGWVML-UHFFFAOYSA-N

InChi: InChI=1S/C16H20N4O2/c1-18(14-7-3-2-4-8-14)16(21)19-11-15(17-12-19)13-6-5-9-20(22)10-13/h5-6,9-12,14H,2-4,7-8H2,1H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 2.2 mg/mL (7.32 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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).

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.

Products are for research use only. Not for human use.