GPCR Calcium Product Solutions

Measure Calcium Mobilization Using a Homogeneous, Dye-based Assay with Stable GPCR Cell Lines

Cell-based calcium assays measure intracellular calcium ion flux from the endoplasmic reticulum (ER) to the cytosol upon ligand- or therapeutic-activation or inhibition of GPCRs or calcium ion channels in a dose-dependent manner. Eurofins DiscoverX® offers traditional and native Gq-coupled GPCR cell lines, ready-to-assay frozen GPCR cells, and a Calcium No WashPLUS detection kit.

The cell lines and frozen cells are qualified for use with FLIPR® or the homogeneous fluorescent dye-based detection kit. Rank order potential leads and perform high throughput screening (HTS) calcium mobilization analysis with the Calcium No WashPLUS detection kit and obtain large assay windows and wide dynamic ranges.

Product Highlights
  • Optional Formats – Select from hundreds of stable cell lines and frozen ready-to-assay cells, as well as the accompanying Calcium No WashPLUS fluorescent detection kit for calcium mobilization analysis in response to agonist or antagonist stimulation
  • Optimized Assays – Native cell lines with overexpressed naturally Gq-coupled, wild-type GPCRs optimized for use with the Calcium No WashPLUS detection kit
  • Multiplexing Capabilities – Perform calcium detection and β-arrestin recruitment assays using the same cell line in the same well for multiple readouts
  • Quick Analysis – Perform single-step, HTS with Calcium No WashPLUS assays in adherent or suspension cells for both GPCRs and calcium ion channels

Consider Eurofins DiscoverX’s custom development capabilities for custom cell lines, assays, & enzyme development.

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Products

Product Types

  • Calcium No WashPLUS Detection Kit – Rapidly quantify calcium flux with homogeneous, fluorescent dye-based assays qualified for use with all Gq-coupled cell lines
  • Coelenterazine H – Utilize a derivative of native coelenterazine that is significantly more sensitive to calcium and provides enhanced performance in aequorin-based luminescent HTS calcium assays. Note aequorin-based luminescence assays require addition of a coelenterazine substrate like coelenterazine H.
  • Calcium Gq-coupled Cell Lines – Naturally coupled, stable Gq-coupled cell lines and qualified for use with the Calcium No WashPLUS Assay, AssayComplete™ cell culture reagents, and control ligands.
  • ChemiSCREEN stable cell lines, parental cell lines, and ready-to-assay frozen cells – Cells based on our proprietary Chem-1 and related host cell backgrounds that contain an endogenous expression of Gα15. Gα15 is a promiscuous G protein to help funnel signaling to a common calcium readout, regardless of G protein coupling status. Use cell lines or frozen cells with chemiluminescent or fluorescent assays, and parental cell lines to generate your own GPCR stable cell lines. Additional second messenger signaling, e.g. cAMP, and ERK phosphorylation, for most targets can be used to perform orthogonal assay confirmation.
  • ChemiBRITE stable cell lines and ready-to-assay frozen cells – Cells engineered to flash with added brightness upon GPCR activation and developed to provide the greatest readout flexibility, including luminescent and fluorescent calcium flux as well as cAMP. These cells express a proprietary mutant version of clytin, a calcium activated photoprotein.

Application Related Assays

  • β-Arrestin Assays – Universal G-protein independent cell-based assays to quantify GPCR activation based on the recruitment of β-arrestin. Ideal for ligand bias analysis, antagonist mode screening, and studying virtually any GPCR including orphan receptors.
  • cAMP Assays – Detect cellular cAMP levels via GPCR signaling by biologics or small molecule therapeutics using robust, simple, homogeneous, and HTS assays.
  • GPCR Internalization Assays – Secondary, orthogonal screening cell-based assays for measuring GPCR desensitization and recycling as well as uncovering novel classes of compound pharmacologies and identifying safer drugs without imaging or antibodies.
  • Pharmacotrafficking Assays – Quantitative cell-based assays to identify small molecule pharmacochaperones that act as therapeutic agents to stabilize and correct disease-relevant mutant GPCRs, ion channels, or transporters.
  • Membrane Preparations – Purified membrane preps for obtaining GPCR and ion channel ligand binding affinities and evaluating GPCR activity through GTPγS functional studies in response to the addition of a ligand or therapeutic.
  • Obesity/Diabetes Assays – Accelerate the development of GPCR peptide therapeutics like GLP-1, GIP and glucagon for obesity and diabetes with MOA-reflective assays.