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

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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