G protein-coupled receptor (GPCR) assay technologies

GPCRs (aka 7-transmembrane receptors) are a large and diverse class of transmembrane signaling proteins. They have tremendously diverse functions ranging from neurotransmitter receptors to cellular adhesion. GPCRs mediate their physiological effects in a variety of ways, most famously by coupling to downstream effectors through the heterotrimeric G protein complex (Gα,β,γ) but also through other pathways such as β-arrestins. GPCRs have been very effectively targeted for therapeutics – making up ~30% of all approved drugs. Over the last decade-and-a-half, allosteric modulation of GPCRs and unanticipated pharmacological diversity has led to a new generation of intense interest in GPCRs as therapeutic targets, therefore rapid and effective ways of measuring GPCR activation are critically important.

 

Calcium (Ca²⁺) flux assays

A key signaling pathway for many GPCRs is via Gaq-mediated activation of phospholipase C-β resulting in generation of inositol 1,4,5-trisphosphate (IP3) and subsequent activation of IP3 receptor Ca²⁺ channels causing release of Ca²⁺ from intracellular stores. Using fluorescent, Ca²⁺-sensitive indicators, this signaling pathway has been exploited for decades as a rapid and effective means of measuring GPCR activation

ION offers a variety of fluorescent, Ca²⁺-sensitive indicators that are ideal for measuring GPCR activation using microscopy, flow cytometry, or plate readers.

 

(EX 490 nm/Em 515 nm, Kd 355 nM) is the most used and the most trusted of the single-wavelength Ca²⁺ indicators. It has been the indicator of choice for countless basic research studies and has been used to screen many tens-of-millions of compounds using high-throughput screening (HTS) to discover pharmacological tools and drugs for GPCRs, and a wide variety of Ca²⁺ permeable ion channels and transporters.

(EX 490 nm, EM 515 nm) High-throughput, no wash thallium (Ca²⁺) assay. The most flexible solution for measuring the activity of GPCRs coupled to intracellular Ca²⁺ release. 10 plates

(EX 490 nm/Em 515 nm, Kd 290 nM) Also known as Fluo-2 HA, Fluo-2 offers the same spectral properties as Fluo-4 combined with superior loading in many cell types as well as a slightly higher Ca²⁺ affinity. The improved loading and increased affinity can result in superior sensitivity. 

(EX 490 nm, EM 505 nm) High-throughput, no wash thallium (Tl⁺) assay. A streamlined solution for large-scale screening GPCRs coupled to intracellular Ca²⁺ release. 100 plates

Thallium (Tl⁺) flux assays

A key signaling pathway for another major class of GPCRs, Gi/o-coupled GPCRs, is through activation of G protein-gated Inward Rectifying Potassium (K⁺) channels, better known as GIRK channels. Not only is the GPCR-mediated modulation of GIRK channels of great physiological importance, it also provides a convenient means of measuring Gi/o GPCR activity using Tl⁺ flux. This GIRK assay approach offers some key advantages compared to other approaches used to measure the activity of Gi/o GPCRs. Unlike the most common approaches which utilize fixed-endpoint measures of cAMP, the GIRK assay is a real-time measure of GPCR activation and does not require non-physiological elevations of intracellular cAMP. Unlike approaches which utilize chimeric Gα subunits (e.g. Gqi5) to induced Gi/0 GPCRs to promote intracellular Ca2+ release, the GIRK assay enables measurement of Gi/o GPCR activity through their native Gβ/γ coupling mechanism.

ION offers Tl⁺ flux reagents and assay kits to help enable researchers to utilize GIRK-based GPCR activity assays.

 

(EX 490 nm, EM 515 nm) is the best-in-class Tl⁺-sensitive fluorescent indicator. It displays outstanding cell loading and excellent compatibility with a wide variety of detectors including fluorescent microscopes, plate readers, and flow cytometers using commonly available FITC filters.

(EX 490 nm, EM 505 nm) High-throughput, no wash thallium (Tl⁺) assay. A streamlined solution for large-scale screening of GPCRs using GIRK channels. 100 plates

(EX 490 nm, EM 505 nm) High-throughput, no wash thallium (Tl⁺) assay. The most flexible solution for measuring the activity of GPCRs using GIRK channels. 10 plates

Be Brilliant! Explore our line of GPCRs Assays

Our collection of G protein-coupled receptor assay technologies

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High-throughput, no wash calcium (Ca²⁺) assay. An optimal solution for measuring intracellular Ca²⁺ dynamics, including effectors such as GPCRs and protein transporters. 100 plates

490/515
FITC, GFP
$2,790.00

High-throughput, no wash calcium (Ca²⁺) assay. An optimal solution for measuring intracellular Ca²⁺ dynamics, including effectors such as GPCRs and protein transporters. 10 plates

490/515
FITC, GFP
$362.00

High-throughput, no wash thallium (Tl⁺) assay. An optimal solution for measuring flux through potassium (K⁺), sodium (Na⁺), and non-selective cation channels and their effectors including transporters and GPCRs. 100 plates

490/515
FITC, GFP
$3,270.00

High-throughput, no wash thallium (Tl⁺) assay. An optimal solution for measuring flux through potassium (K⁺), sodium (Na⁺), and non-selective cation channels and their effectors including transporters and GPCRs. 10 plates

490/515
FITC, GFP
$430.00

Green fluorescent, calcium (Ca²⁺) indicator, membrane permeable. Higher Ca²⁺ affinity than Fluo-4.

490/515
290
DMSO
FITC, GFP
$125.00

Green fluorescent, calcium (Ca²⁺) indicator, membrane permeable

490/515
355
DMSO
FITC, GFP
$140.00

The necessary reagents for conducting no wash, ratiometric calcium flux assays compatible with plate reader and fluorescence microscopy applications. Individual components are provided to give the user the flexibility needed to customize your assay.

340,380/505
145
DMSO
GFP/FITC, PI/Texas Red
$340.00

Best in class, green fluorescent, thallium (Tl⁺) indicator, membrane permeable. Works with potassium (K⁺), sodium (Na⁺), and monovalent cation channels, and transporters.

490/515
DMSO
FITC, GFP
$495.00
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