How does the assay work? |
The small enzyme fragment of β-galactosidase called ProLink™ (PK) is localized to intracellular endosomes and the larger, complementing enzyme fragment called Enzyme Acceptor (EA) is fused to β-Arrestin. Stimulation of the receptor results in Arrestin binding to the activated GPCR, internalization of the receptor and trafficking to cellular endosomes, resulting in complementation and an increase in activity that can easily be measured using PathHunter® Detection Reagents. |
Fast & Simple Protocol |
| PathHunter® Activated GPCR Internalization assays combine a simple, one-step addition protocol and standard chemiluminescent detection and are ideally suited for 96- or 384-well analysis. |
Robust & Reliable Results |
Benefits• Confirm compound pharmacology &selectivity • Combine with traditional second messenger assays to uncover compound-specific differences in receptor activation and internalization • Differentiate between slow and fast recycling receptors • Ideal for hit confirmation or tertiary screens following a primary screen |
Kit Contents• Frozen, assay-ready PathHunter® GPCRInternalization eXpress cells (1 or 2 vials each, 1 x 106 cells/vial) • PathHunter® Chemiluminescent Detection Reagents • Optimized Cell Plating Reagent • 96-well Tissue Culture Treated Plates |
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