BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH; IC50 = 4.9 nM in HEK293T cells expressing the human recombinant enzyme).
CAS:1233855-46-3
分子式:C16H20N4O2
分子量:300.4
纯度:98%
存储:Store at -20°C
Background:
BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH; IC50 = 4.9 nM in HEK293T cells expressing the human recombinant enzyme). It also inhibits FAAH2, α/β-hydrolase domain-containing protein 6 (ABHD6), carboxylesterase 2 (CES2), and patatin-like phospholipase domain 6 (PNPLA6) with IC50 values of 0.4, 0.081, 2, and 11 μM, respectively. BIA 10-2474 alters expression of 161 lipid species, including FAAH substrates as well as other lipid classes, in human cortical neuron cultures indicating compound promiscuity. Formulations containing BIA 10-2474 were previously investigated clinically for the management of chronic pain but use was halted due to development of significant neurotoxicity.