A Bright New Approach to Measuring
P-glycoprotein (Pgp)

Pgp is an ATP-dependent drug efflux pump that plays an important role in multi-drug resistance, drug absorption and drug-drug interactions. Compounds that interact with Pgp can be identified as stimulators or inhibitors of its ATPase activity. The Pgp-Glo™ Assay uses unmetabolized ATP from a Pgp-ATPase reaction in a light generating luciferase/luciferin reaction. The luminescent signal produced reflects Pgp activity. Compared to traditional methods, this assay is simple, fast and amenable to automation.

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EC₅₀ and IC₅₀  Measurements using the Pgp-Glo™ Assay

Panel A Verapamil was tested at a range of concentrations for its capacity to stimulate Pgp ATPase activity.

Panel B IC₅₀ Measurements where cyclosporin-A was tested at a range of concentrations for its capacity to inhibit 200um Verpamil stimulated Pgp ATPase activity

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