Gi/o GPCR-GIRK Thallium Flux Assay

$695.00$11,690.00

A complete Gi/o GPCR assay for discovering modulators through direct coupling to GIRK channels. Cell lines and thallium flux reagents are included.

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Variation SKU Price Quantity Action
Size: Flex kit - 10 plate without cells
11100-b
$695.00
Size: Flex kit - 10 plate with cells
11100-a
$11,690.00

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Specifications

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Product Description

ION’s Gi/o GPCR-GIRK Thallium Flux Assay is a total assay solution for multi-well plate-based, high-throughput measurements of Gi/o GPCR agonism measured via native GIRK coupling. This kit provides most reagents needed, including a stable HEK293 cell line that expresses human Kir3.1 and Kir3.2, to conduct Gi/o GPCR HTS. A simple transduction step allows the flexibility to study a plethora of GPCRs that couple to GIRK using thallium flux.

Key Benefits:

  • Native coupling
  • Does not require artificial stimulation
  • Flexibility to insert any G/o GPCR
  • Discover additional hits
  • Uncover biased agonists
  • Explore complex pharmacology

GPCR-GIRK Thallium Flux Assay Principle.

Data

Dose-response curves for four Gi GPCR, g-protein coupled receptors, (Dopamine D2, 5HT1A, M2, and Delta opioid) with EC50 values labeled, showing activation vs. ligand concentration.

Study any Gi/o GPCR

Insert any Gi/o GPCR of interests using transient or stable expression systems for rapid hit finding. Generate HTS results for your target within 24 hours. 

  • Rapid results
  • Ultimate flexibility
Two dose-response plots showing dopamine effects on dopamine D2 receptors. The left graph shows cAMP response with an EC50 of 5.5 µM. The right graph displays GPCR-GIRK assay results with an EC50 of 6.7 nM. Both graphs plot response intensity against log dopamine concentration.

cAMP versus Gi/o GPCR-GIRK Assay

As demonstrated in this dopamine (D2) receptor example, cAMP assays can be complicated by the combination of Gs and Gi GPCR receptor expression. HEK cells endogenously express multiple dopamine receptors, Our Gi/o GPCR-GIRK Thallium Flux Assay readout is specific to Gi GPCR signaling, enabling you to ignore the noise and hone in on your target of interest.

  • No artificial stimulation needed
  • Measure Gi receptor signalling only

cAMP versus Gi/o GPCR-GIRK Assay

Unlock better assay quality with Z’ out-matching cAMP assays. When studying Gi-coupled receptors which inhibit cAMP production, the high basal cAMP levels induced by forskolin can make it difficult to detect small decreases in cAMP caused by receptor activation.

  • Higher Z’
  • Larger signal amplitude

Learn more

New to thallium flux assays, read our blog called How to analyze thallium flux assay data.

Documentation