Miniaturization of Cytochrome P450 Time-dependent Inhibition Screening Using the Echo® Liquid Handler

1 May 2013

As a large number of compounds are screened for ADMET properties against various cytochrome P450 (CYP) enzymes on a regular basis, miniaturization and automation of ADMET assays have become one of the top priorities to manage the cost and labor. This application note presents results from miniaturized time-dependent inhibition assays. The time-dependent inhibition for two of the most abundant CYP enzymes, CYP3A4 and 1A2, were evaluated. The results from the Echo liquid handler method demonstrate fast, reliable and accurate IC50 values.

Echo® 500 Series Liquid Handlers

The Echo® liquid handler revolutionizes liquid handling with acoustic energy. Sound waves eject precisely sized droplets from a source onto a microplate, slide or other surface suspended above the source. This product does not use tips, pin tools or nozzles—completely eliminating contact between the instrument and the liquid. The Echo liquid handler provides powerful benefits: Tipless transfer, resulting in dramatic cost savings Improved information about sample integrity and improved transfer quality through measurement of DMSO hydration level Elimination of the need for calibration through Dynamic Fluid Analysis™ technology, a patented Labcyte process Elimination of cross-contamination, carryover or leachates through non-contact transfer Accurate, precise movement of nanoliter-scale quantities, enabling assay miniaturization and further reducing costs Better results through direct dilution of compounds, an improvement over serial dilution methods Greatly simplified assay development and dilution processes through the flexibility to transfer any volume of liquid from any well to any other well

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Miniaturization of Cytochrome P450 Time-dependent Inhibition Screening Using the Echo® Liquid Handler