BIA 10-2474

SKU: orb1226715

Description

BIA 10-2474 is a potent FAAH inhibitor with IC50s of 50-70 μg/kg (i.p.) in various brain regions; also inhibits several lipases that are not targeted by PF04457845, produces substantial alterations in lipid networks in human cortical neurons.Pain Phase 1 Discontinued(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.

Key Properties

• CAS Number: 1233855-46-3
• MW: 300.3556
• Purity: >98% (HPLC)
• Formula: C₁₆H₂₀N₄O₂
• SMILES: O=C(N1C=C(C2=C[N+]([O-])=CC=C2)N=C1)N(C3CCCCC3)C
• Target: FAAH
• Solubility: DMSO: 6.4 mg/mL (Need ultrasonic and warming)

Bioactivity

• 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.
• In Vitro:
  ExVivo: BIA 10-2474 proves to be a potent FAAH inhibitor with IC50s of 50-70 mg/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).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BIA10-2474 | BIA-10-2474

Quick Database Links

Gene Symbol

FAAH