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PathHunter® eXpress β-Arrestin GPCR Kits
Universal GPCR Technology for Direct Pharmacology in Live Cells
The PathHunter® eXpress β-Arrestin GPCR assays are based on the proven PathHunter® β-Arrestin technology which is a universal method for detection of GPCR activity regardless of coupling status. Unlike second messenger or other imaging assays, the PathHunter β-Arrestin assay is unique in that it provides a direct measure of β-Arrestin binding to the GPCR of interest and can be used with any Gi-, Gq-, Gs-coupled receptor.
Product Features
Over 150
human
and mouse
Gi-, Gq-, and Gs-coupled GPCRs available
Off-the-shelf complete kit format
Pre-validated cells and reagents
Complete step-by-step protocol
Assay-Ready frozen cells
Read on any standard benchtop luminometer
How the PathHunter® eXpress β-Arrestin GPCR Assay Works
In this system, β-Arrestin is fused to an N-terminal deletion mutant of β-gal (termed the enzyme acceptor, EA) and the GPCR of interest is fused to a smaller (42 amino acids), weakly complementing fragment termed ProLink™. In cells that stably express these fusion proteins, the interaction of β-Arrestin and the GPCR following ligand stimulation forces the complementation of the two β-gal fragments resulting in the formation of a functional enzyme that converts substrate to detectable signal. In the absence of an interaction between the GPCR and β-Arrestin, the enzyme activity is low due to the low affinity of the two enzyme fragments.
click on figure to enlarge
Figure 1. Confirm pharmacology of your compound regardless of whether it is an agonist, antagonist, inverse agonist or allosteric modulator using a simple, homogeneous protocol combined with chemiluminescent detection.
click on figure to enlarge
Figure 2. Performance comparison between live cell and frozen eXpress cells
(A) Correlation between EC50 values of control agonists obtained using live cells and PathHunter
eXpress cells. Data is presented for 100 receptors. EC50 values above the line indicate higher
sensitivity in the eXpress format compared to live cells. (B) CHO-K1 PathHunter eXpress cells
and live cells expressing the Somatostatin 2 (SSTR2) receptor were stimulated with increasing concentrations of SST-28,
a known agonist, for 90 minutes prior to the addition of detection reagents. PathHunter eXpress cells
show equivalent pharmacology to live cells.
New! LumiLITE™ Microplate Reader
Introducing the LumiLITE™ Microplate Reader, a cost effective, 96-well bench top luminometer ideal for use with all PathHunter and cAMP Hunter eXpress GPCR Assays. Learn More»
Kit Contents
Assay-ready, frozen PathHunter® eXpress cells (2 vials each, 1 x 106 cells/vial)
Optimized Assay Buffer
PathHunter™ Detection Reagents
96-well Tissue Culture Treated Plates
Available Literature
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Download the user manual 
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