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| | Cytochrome P450 Inhibition |
| Description: | The effect of compound on cytochrome P450 (CYP) enzyme catalytic activity was determined in human liver microsomes, using a cocktail of probe substrates at concentrations equal to their approximate Km values for each of the CYP enzymes. Metabolites were detected using LC-MS. Peak area ratios for the metabolites against the internal standard were used to express the metabolite formation. The percent of inhibition by the test compound was determined by dividing the peak area ratio obtained in the presence of the compound by the corresponding ratio in the absence of the compound. IC50 values were determined using percent activity remaining (compared to a control sample with no drug added) versus the concentration (log scale) in WinNonlin version 3.2 Model 103. |
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