The PathHunter
® eXpress GPCR Profiler Kit allows you to mix-and-match up to 10 different GPCR targets. Select from over 350 targets available in β-Arrestin recruitment, cAMP accumulation, or GPCR internalization readouts. Build a unique panel of assays to compare human and ortholog pharmacology or jump start your deoprhanization campaign by testing your compounds with a unique combination of Orphan GPCR receptors. Profiler kits contain everything needed to perform functional assays on 10 unique targets including frozen pre-validated cells, detection reagents, cell plating reagents and assay plates. Perform compound selectivity profiling on your bench top with our simple and easy to use Profiler kit.
Features & Advantages
- Flexible - mix and match over 350 GPCR assays
- Multiple readouts - Arrestin recruitment, cAMP accumulation and receptor internalization
- Convenient - benchtop profiling of lead compounds
- Customizable - create unique selectivity panels or study off-target effects
- Compound dosing - compare pharmacology between human and ortholog targets
- Novel tool for receptor de-oprhanization
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How it Works |
Assay Performance
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Chemokine Receptor Family Profiling
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A series of known chemokine agonists were tested against select multiple chemokine targets. CCR6, CXCR1, CCR2, and CCR5 maintain agonist selectivity demonstrating that these assays are
uniquely suited for in house profiling and/or target prioritization [click to enlarge].
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The PathHunter
® GPCR Explorer Kit is a simple and easy-to-use method for building on-demand functional GPCR assays in just 3 simple steps – Clone. Transfect. Read. Whether you have a panel of mutant GPCR cDNAs or a favorite GPCR heterodimer you’d like to functionally test, the simple, optimized transfection protocol combined with PathHunter
® EFC-based chemiluminescent detection makes it the ideal platform for exploring novel GPCR receptor biology.
Features & Advantages
- Based on G-protein independent β-Arrestin read-out
- Contains highly transfectable, ready-to-assay CHO-K1 cells
- Choice of vectors optimized for maximal expression in mammalian cells
- Ideal for GPCR heterodimerization, siRNA knockdown, or mutant receptor studies
- Chemiluminescent detection used with any standard luminometer
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How it Works |
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Assay Performance
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Create Customized GPCR Biosensor Lines
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CHO-K1 GPCR eXplorer cells were plated at 10,000 cells per well and incubated overnight at 37°C. The following day, cells were transfected with 2 µg of pEGFP vector and 48 hr post-transfection, greater than 60% of the GPCR Explorer cells were transfected ([Left panel) [click to enlarge]. In a separate experiment, eXplorer cells were transiently transfected with 2 µg of the pCMV-SSTR2-PK vector (+ SSTR2 DNA) or an empty vector (- SSTR2 DNA). Twenty-four hours later, cells were treated with increasing concentrations of Somatostatin 28, a control agonist. Activation of the SSTR2 receptor stimulates binding of Arrestin resulting in an increase in β-gal enzyme activity that can be measured using chemiluminescent PathHunter Detection Reagents (Right panel) [click to enlarge].
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