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1233855-46-3

1233855-46-3 structure
1233855-46-3 structure
  • Name: BIA 10-2474
  • Chemical Name: BIA 10-2474
  • CAS Number: 1233855-46-3
  • Molecular Formula: C16H20N4O2
  • Molecular Weight: 300.356
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease FAAH
  • Create Date: 2018-04-05 03:46:18
  • Modify Date: 2024-01-02 19:52:05
  • 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.

Name BIA 10-2474
Synonyms BIA-10-2474
N-Cyclohexyl-N-methyl-4-(1-oxido-3-pyridinyl)-1H-imidazole-1-carboxamide
5AP1ZW859M
1H-Imidazole-1-carboxamide, N-cyclohexyl-N-methyl-4-(1-oxido-3-pyridinyl)-
BIA 10-2474
Description 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.
Related Catalog
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].
Animal Admin Rats: Groups of rats (n=4) are pre-treated with BIA 10-2474 (2 mL/kg in 5% Tween 80 in saline i.p.) or with vehicle 40 min prior to radiotracer injection. Rats, in a restraining box, receives 3–4 MBq of high-specific activity [18F]-DOPP in 0.3mL of 10% ethanol in citrate buffer (pH 6) via the tail vein which has been vasodilated in a warm water bath. They are sacrificed by decapitation at 40 min after radiotracer administration, the brain is surgically removed from the skull and stored on ice. Brain regions are excised, blotted, and weighed while blood is collected. Radioactivity in tissues is assayed[1].
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

Density 1.3±0.1 g/cm3
Boiling Point 568.3±52.0 °C at 760 mmHg
Molecular Formula C16H20N4O2
Molecular Weight 300.356
Flash Point 297.5±30.7 °C
Exact Mass 300.158630
LogP -0.41
Vapour Pressure 0.0±1.6 mmHg at 25°C
Index of Refraction 1.642
Storage condition 2-8℃