Gαq GPCR assays

Gq -coupled G protein-coupled receptors (GPCRs) are a subset of GPCRs that couple with the Gαq protein subunit.

Gαq GPCRs are involved in numerous physiological processes, including neurotransmission, hormone regulation, and immune responses. Some drugs targeting Gq-coupled GPCRs include antidepressants, blood pressure medications, and allergy treatments, making them popular pharmacological targets for drug discovery.
When these receptors are activated by ligands such as hormones, neurotransmitters, or other signaling molecules, they initiate a signaling cascade that involves the activation of phospholipase C-β (PLC-β) and subsequent production of inositol trisphosphate (IP3), causing calcium release from intracellular stores into the cytoplasm. Using fluorescent, calcium-sensitive assays, this signaling pathway has been exploited for decades as a rapid and effective means of measuring GPCR activation.

ION offers a variety of fluorescent calcium indicators and calcium assays that are trusted for measuring Gq-coupled GPCR activation in high-throughput screening, on a microscope, or using fluorescence plate readers. Click here if you are interested in learning more about our calcium indicators.

On this page:
Go to Store

Gα16 GPCR assays

Gα16 is a promiscuous Gαq protein subunit that can couple to a wide variety of receptors including Gαi/o and Gα12/13 GPCRs. The downstream signaling cascade of GPCR ligand binding includes activation of phospholipase C-β, an increase in IP3, and a release of calcium from intracellular stores like other Gq-coupled GPCRs. This chimeric G protein can be over-expressed in HEK293 and other mammalian cell lines to enable calcium signaling as a functional readout of GPCR activity, and is commonly used to uncover native ligands for orphan GPCRs.

Calcium assays for GPCRs

A key signaling pathway for many GPCRs is via Ga,q-mediated activation of phospholipase C-β resulting in generation of inositol 1,4,5-trisphosphate (IP3) and subsequent activation of IP3 receptors causing release of calcium (Ca²⁺) from intracellular stores.

Using fluorescent, calcium-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 trusted for measuring GPCR activation in high-throughput screening, with microscopy or plate readers.

GPCR assay using Fura-2 AM to measure calcium flux. Dose dependent response of carbachol stimulation of the endogenous muscarinic M3 receptor in HEK cells.

Our Flex kit provides all necessary reagents in a format to maximize flexibility for your assay design and customization challenges. Brilliant Calcium Flex is a (EX 490 nm, EM 515 nm) high-throughput, no wash calcium mobilization assay. The most flexible solution for measuring the activity of GPCRs coupled to intracellular Ca²⁺ release.

GO TO PRODUCT

(EX 525 nm, EM 550 nm, Kd 400nM) Brilliant Calcium Gold is a calcium flux assay for multi-well plate-based, high throughput measurements of calcium mobilization mediated through a wide variety of plasma membrane and intracellular calcium channels. The kit includes our Fluo-Gold dye, which is red-shifted for compatibility with GFP and other green fluorescent indicators.

GO TO PRODUCT

Ratiometric Calcium Essentials kit provides 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.

(EX 340/380 nm, EM 505 nm, Kd 145nM) High-throughput, no wash ratiometric calcium (Ca²⁺) assay. No wash, compatible with plate reader and fluorescence microscopy applications.

GO TO PRODUCT

Be Brilliant! Explore our line of Products

View Product Table

Enquire now