High-Throughput Analysis of Cytochrome P450 Inhibition in Intact Human Hepatocytes
11 Jul 2014

Ultrafast methods of analysis were developed using the Agilent RapidFire High-Throughput Mass Spectrometry System in combination with an Agilent 6490 Triple Quadrupole Mass Spectrometer for cytochrome P450 (CYP) inhibition in human hepatocytes. The enzymatic activities of six major liver cytochrome P450 isoforms were evaluated using probe substrates under the application of 15 different model inhibitors. Dose-response curves and IC50 values were determined using seven inhibitor concentration points. Methods of analysis were all 13 seconds or less per sample, enabling ultrafast determination of CYP inhibition.

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