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The assay is based on fresh human liver microsome
incubation of well-known substrates and inhibitors. The enzyme
activities are measured by the concentrations of the
metabolite for each substrate when inhibitor is either absent
or present at various concentrations. Testosterone,
dextromethorphan and diclofenac are the substrates for CYP3A4,
CYP2D6 and CYP2C9, respectively. The corresponding metabolites
are 6b-hydroxytestosterone, dextrorphan and
4-hydroxydiclofenac. The incubation for each CYP is done
separately. The samples are pooled and analyzed by LC-MS/MS.
IC50 of each testing compound will be provided.
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Discovery
