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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
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Size: Flex kit - 10 plate with cells
11100-a
$11,690.00
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Gio GPCR-GIRK Thallium Flux Assay
SKU: 11100 Categories: , Synonyms: , ,

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. Over the past 15 years, fluorescence-based measures of TI+ flux have brought about the discovery of small molecule modulators of a host of ion channels, transporters, GPCRs and other targets of interest. ION’s GPCR-GIRK Thallium Flux Assay generates high quality screening assays and EC50 values that are consistent with other methods.

GPCR-GIRK Thallium Flux Assay Principle.

GPCR-GIRK Thalliun Flux Assay Principle -1-1
GPCR-GIRK Thalliun Flux Assay Principle -2-1
GPCR-GIRK Thalliun Flux Assay Principle -3-1
GPCR-GIRK Thalliun Flux Assay Principle -4-3
Gi GPCR assay data for Dopamine D2 receptor, including a kinetic trace and dose response curve
Gi GPCR high throughput screening data for Dopamine D2 receptor, including a kinetic trace and Z’ analysis for hit discovery.
Gi GPCR 96-well dose response curves for Dopamine D2 receptor, Serotonin receptor (5HT1A), muscarinic receptor (M2), and delta opioid receptor.
Gi GPCR 384-well dose response curves for Serotonin receptor (5HT1A), muscarinic receptor (M2), and delta opioid receptor.

Documentation

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Learn more about thallium indicators
GPCR assays using thallium flux

References

Luscher C, Slesinger PA. Emerging roles for G protein-gated inwardly rectifying potassium (GIRK) channels in health and disease. Nat. Rev. Neurosci. 2010, 11(5):301-15.
Kano HK, Toyama Y, Imai S, Iwagashi Y, Mase Y, Yokogawa M, Osawa M, Shimada I. Structure mechanism underling G protein family-specific regulation of G protein-gated inwardly rectifying potassium channel. Nat. Commun. 2019, 10 (1):2008.
Tateyama M, Kubo Y. Gi/o-coupled muscarinic receptors co-localized with GIRK channel for efficient channel activation. PLoS One. 2018, 13(9):e0204447.
Gadgaard C, Jensen AA. Functional characterization of 5-HT1A and 5HT1B seeerotonin receptor signaling though Gprotein- activated inwardly rectifying K+ channels in a fluorescence-based membrane potential assay. Biochem. Pharmacol. 2020, 175:113870.
Weaver CD, Harden D, DWoretzky SI, Robertson B, Knoc RJ. A thallium-sensitive, fluorescence-based assay for detecting and characterizing potassium channel modulators in mammalian cells. J. Biomol. Screen. 2004, 9(8):671-7.
Niswender CM, Johnson KA, Luo Q, Ayala JE, Kim C, Conn PJ, Weaver CD. A novel assay of Gi/o-linked G proteincoupled receptor coupling to potassium channels provides new insights into the pharmacology of the group III metabotropic glutamate receptors. Mol. Pharmacol. 2008, 73(4):1213-24.
Weaver CD. Thallium Flux Assay for Measuring the Activity of Monovalent Cation Channels and Transporters. Methods Mol. Biol. 2018, 1684:105-114.
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