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DiscoveRx: GPCRs - PathHunter™ β-Arrestin Collaterals

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GPCR

- PathHunter™ β-Arrestin Assays

PathHunter™ β-Arrestin Assays



A wide variety of assays are available for analyzing GPCR signaling events, many
of them based on second messenger analysis. PathHunter™ β-Arrestin assays are unique in that they detect primary rather than secondary activation events. The assays provide a direct measure of GPCR activation by detecting the binding of
β-Arrestin to the GPCR of interest. Because Arrestin recruitment occurs independent of G-protein coupling, the PathHunter™ β-Arrestin assays offer a powerful and universal screening platform that can be used with virtually any Gi-, Gs-, or Gq-coupled receptors.

How the PathHunter β-Arrestin Works

In this system, β-Arrestin is fused to an N-terminal deletion mutant of β-gal (termed the enzyme acceptor of EA) 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, ligand stimulation results in the interaction of β-Arrestin and the ProLink-tagged GPCR, forcing the complementation of the two β-gal fragments and resulting in the formation of a functional enzyme that converts substrate to detectable signal.

Product Features

Over 220 validated Gi, Gs, and Gq-coupled GPCR assays
Direct measure of GPCR activation state via β-Arrestin recruitment, independent
of G-protein signaling
Human, Mouse and Rat GPCR assays available
Ideal for de-orphanization
Simple, non-radioactive single addition protocol optimized for a HTS-friendly format
HTS-friendly format, easily miniaturized

For instrument compatibility, please click here.

Available Collaterals

click here to view what we have available!

PathHunter™ Technology Available In Several Formats


Clonal Cell Lines
PathHunter™
Cell Lines
Expedite your functional GPCR screening efforts with the broadest portfolio of clonal cell lines available.
Choose from over 220 fully validated cell lines. Click here
PathHunter™
Orphan Cell Lines
Leverage the PathHunter technology to de-orphanize any orphan GPCR cell line. Choose from over 90 fully validated cell lines. Read More»
PathHunter™ Orthologs
Perform species selectivity, counter-screening and SAR evaluation of lead compounds with Mouse or Rat GPCR orthologs. Read More»
Assay-Ready Formats
PathHunter™ eXpress
β-Arrestin GPCR Assays
Off-the-shelf complete kit format that eliminates the need for lengthy and time consuming cell culture. Formatted for 96-well plates, 200 data points. Read More»
EasyScreen™
β-Arrestin GPCR Assays
Confirm hits or validate leads from a primary screen without lengthy and time consuming cell culture or assay development. Formatted for 384-well plates, 4000 data points. Read More»
Other
PathHunter™
Detection Reagents
Chemiluminescent detection reagents for use with all PathHunter
β-Arrestin Cell Lines. Kits available for either Glow or Flash luminescence. Read More»
PathHunter™
Toolbox Products
Create your own PathHunter β-Arrestin GPCR Assay using our validated β-Arrestin parental cell lines and expression vectors. Read More»

*Covered by Issued and Pending patents. Limited Label License Conditions apply. Click here to learn more.

Click here to view a complete list of GPCR targets.


Don't see your target?

Click here to request our Custom Assay Development Service

Don't want to do cell culture?

New! Bulk cell options are available with teh purchase of any PathHunter clone. Package sizes range from 100 million to 3 billion cells. Bulk cells are functionally tested for optimal assay performance and are confirmed to be Mycoplasma-free. Combine frozen, assay-ready bulk cells with PathHunter-Approved Cell Plating Reagent and Control Ligand to expedite your screening campaigns and ensure
optimal and reproducible results every time. Click here for a quote.

 

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