CYP inhibition assay

RF Rafael Augusto Alves Ferreira
CJ Celso de Oliveira Rezende Junior
PM Pablo David Grigol Martinez
PK Paul John Koovits
BS Bruna Miranda Soares
LF Leonardo L. G. Ferreira
SM Simone Michelan-Duarte
RC Rafael Consolin Chelucci
AA Adriano D. Andricopulo
MG Mariana K. Galuppo
SU Silvia R. B. Uliana
AM An Matheeussen
GC Guy Caljon
LM Louis Maes
SC Simon Campbell
JK Jadel M. Kratz
CM Charles E. Mowbray
LD Luiz Carlos Dias
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These assays measure the ability of test compounds to inhibit cytochrome P450 activity for four isoforms CYP1A2, CYP2C9, CYP2D6 and CYP3A4, with a time dependent inhibition component for 3A4 only, in human liver microsomes, using luminescent and/or fluorescent assay kits. The test compound’s ability to inhibit the enzyme activity (IC50) was assessed by determining the extent of inhibition of metabolite formation relative to vehicle control (DMSO).

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