BIA 10-2474

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BIA 10-2474 是一种有效的 FAAH 抑制剂，在不同脑区的 IC50 为 50-70 μg/kg (ip)。

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.

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 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.

BIA10-2474 | BIA-10-2474

Metabolic Enzyme/Protease

FAAH

FAAH

Neurological Disease

Pain

1233855-46-3

300.3556

C16H20N4O2

>98% (HPLC)

DMSO: 6.4 mg/mL (Need ultrasonic and warming)

O=C(N1C=C(C2=C[N+]([O-])=CC=C2)N=C1)N(C3CCCCC3)C

1H-Imidazole-1-carboxamide, N-cyclohexyl-N-methyl-4-(1-oxido-3-pyridinyl)-

(-20℃)

With Ice Pack

≥ 2 years