Consider Eurofins DiscoverX’s custom development capabilities for custom cell lines, assays, & enzyme development.
Obesity and Diabetes Product Solutions
Accelerate the Development of Next-generation Therapeutics for Obesity and Diabetes with MOA-reflective Assays
Obesity and type 2 diabetes (T2D) continue to be a pressing global health crisis. The therapeutic landscape has been profoundly transformed by the success of incretin-based peptide agonists, such as the GLP-1 targeting semaglutide (Ozempic®, Wegovy®) and the dual GLP-1/GIP agonist tirzepatide (Mounjaro®, Zepbound®). Further advancements, such as the retatrutide triple-agonist [GLP-1/GIP/GCG] and amylin receptor combination therapies (e.g., CagriSema, Amycretin), aim for even greater benefits. Drug discovery programs explore emerging mono- and combination therapies targeting receptors such as peptide YY (PYY) and melanocortin 4 (MC4) receptors alongside small molecules and biosimilars designed to modulate these same pathways. This surge in clinical development underscores the need for robust, mechanism of action (MOA)–reflective tools that can accelerate progress from early discovery to late-stage development.
Eurofins DiscoverX® supports this evolving therapeutic landscape with a comprehensive portfolio of cell-based assays tailored for various peptide therapeutics, small molecules, and other modalities targeting GLP-1, GIP, GCG, PYY, and AMY receptors as well as other related obesity and diabetes targets. These cell-based assays are MOA-reflective and support all stages of the drug development lifecycle — from early discovery and lead optimization through clinical development, commercialization, and stability testing — enabling precise bio-identity and potency assessment. Widely adopted in global drug development programs and cited in peer-reviewed publications, patents, and regulatory filings, Eurofins DiscoverX assays align with industry standards and regulatory requirements, ensuring robust characterization to advance therapeutic candidates toward approval.
Product Highlights
- Qualified Bioassays – ICH (International Council for Harmonization)-compliant assay qualification to ensure accuracy, reliability, and regulatory confidence
- Accurate Pharmacology for Regulatory Filings – Your therapeutics’ MOA measured with precision with industry standards
- Assay Transfer Support to CRO/CDMOs – Seamless end-to-end assay transfer of your commercial release and stability programs available across global sites
- Multiple Assay Formats – Cell lines, assay ready kits, and more – your complete toolkit for Obesity & Diabetes drug discovery and development
Products
GLP-1 & GIP
Glucagon
Amylins
PPY & Others
Resources
Related Pages
Products
Eurofins DiscoverX offers a comprehensive portfolio of products for obesity- and diabetes-related targets including GLP-1, GIP, GCG, MC4, PYY, and AMY receptors — featuring human and ortholog cell lines, ready-to-use eXpress assay kits, membrane preparations, and qualified and target-based bioassays to support peptide therapeutics, small molecules, and other modalities.
Product Types
- Bioassay Kits - Ready-to-use cell-based assay kits with an easy to run, homogeneous protocol. These physiologically relevant, robust bioassays are fit-for-purpose for screening and characterization, as well as potency testing, in quality control lot-release programs.
- Stable Cell Lines - Stable cell lines (continuous culture) developed to reflect the target’s mechanism of action (cAMP, β-arrestin, and receptor internalization) with a drug interaction in a standard cell line background.
- eXpress Assay Kits - Ready-to-use cell-based assay kits for quick analysis and implementation in early discovery phases for screening applications, proof-of-concept, mechanism of action confirmation (cAMP, β-arrestin, and receptor internalization), and rank-ordering studies.
- Ready-to-Assay Frozen Cells - Simple, thaw-and-assay cell format for use in studying drug candidates (small molecules or biologics) targeting GPCRs.
- Membrane Preparations - Derived from proprietary stable recombinant cells to ensure high levels of receptor surface expression. Ideal for screening for ligand binding affinities.
Applications
- cAMP Accumulation - Explore a full suite of products designed to quantify cAMP in response to GPCR activation.
- β-Arrestin Recruitment - Characterize GPCR function and ligand bias with β-arrestin assays.
- Internalization Assays - Study GPCR internalization with activated and total GPCR internalization tools in both stable cell line formats and eXpress kits.
- Binding Affinity Screening - Membrane preparations to screen for ligand binding affinities using a competitive radio-labeled ligand approach or to screen for GPCR activity using GTPγS assays.
- Calcium Flux Assays - Assess ligand-based activation of GPCR through detection of increasing levels of intracellular calcium.
- Receptor Dimerization - Tools to study ligand-induced dimerization of RTKs like activins
Typical Assay Workflow
Eurofins DiscoverX assays are designed for simplicity and efficiency, enabling reliable results with minimal hands-on time. The workflow follows a straightforward sequence — cells are thawed and plated, compounds are added, and the signal is detected – making it easy to generate robust, reproducible data without the need for complex preparation steps.
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Publications
Publications Citing DiscoverX Assays for Characterizing Therapeutics Targeting Obesity and T2D
DiscoverX assays are extensively employed in global drug development programs for innovator, biosimilar, and biobetter drugs. Researchers and drug developers consistently cite these assays in numerous publications for comprehensive characterization and demonstrating signaling bias of peptide therapeutics.
Novel GLP-1 Receptor Analogs Studies
- Characterization of Ecnoglutide- a novel, cAMP-biased GLP-1 peptide using Eurofins DiscoverX’s cAMP, β-arrestin-2 recruitment, and receptor internalization assays. Guo W, et al., Mol Metab. 2023 Sep;75:101762. doi:10.1016/j.molmet.2023.101762. Epub 2023 Jun 24. PMID: 37364710; PMCID: PMC10339203.
- Characterizing GL0034- A Novel, Long-acting GLP-1 Receptor Agonist using Eurofins DiscoverX’s β-arrestin-2 recruitment assay. Jones B, et al., Diabetes Obes Metab. 2022 Nov;24(11):2090-2101. doi: 10.1111/dom.14794. Epub 2022 Jul 18. PMID: 35676825; PMCID: PMC9796023.
- Characterization Of Danuglipron, a Novel Small-Molecule, GLP-1R agonist using Eurofins DiscoverX’s β-arrestin-1 and β-arrestin-2 recruitment assay. David A. Griffith et al., J Med Chem. 2022 Jun 23;65(12):8208-8226. doi: 10.1021/acs.jmedchem.1c01856. Epub 2022 Jun 1. PMID: 35647711; PMCID: PMC9234956.
- Characterization of LY3502970, a Potent and Selective Small-molecule GLP-1R Agonist using Eurofins DiscoverX’s β‐arrestin‐2 recruitment assay. Takahiro Kawai et al., PNAS 2020 Nov 11; 117(47):29959-29967. doi:10.1073/pnas.2014879117.
- Assessment of Ligand Bias of a GLP-1R Agonist using Eurofins DiscoverX’s β-arrestin-1 and β-arrestin-2 recruitment assay. Zhang, H., Sturchler, E., Zhu, J. et al. Nat Commun 6, 8918 (2015). https://doi.org/10.1038/ncomms9918
Novel GLP-1, GIP, or GCG Receptor Co-agonists Studies
- Signaling Bias of Tirzepatide- a novel, GLP-1/GIP dual agonist peptide using Eurofins DiscoverX’s β-arrestin-2 recruitment assays. Willard FS et al., JCI Insight. 2020 Sep 3;5(17):e140532. PMID: 32730231; PMCID: PMC7526454.
- A Novel Triple Glucagon, GIP, and GLP-1 Receptor Agonist using Eurofins DiscoverX’s β-arrestin-2 recruitment assays. Coskun T, et al., Cell Metab. 2022 Sep 6;34(9):1234-1247.e9. doi: 10.1016/j.cmet.2022.07.013. Epub 2022 Aug 18. PMID: 35985340.
Frequently Asked Questions
- Which is the preferred assay for testing GPCR-based obesity or diabetes therapeutics in potency and lot-release applications?
Regulatory guidelines, such as those from the FDA (US Food and Drug Administration) and EMEA (European Medicines Evaluation Agency), emphasize the importance of potency assays that adequately measure the relevant mechanism of action (MOA) of drug therapeutics. For various peptide therapeutics directed at the three key GPCR targets (GLP-1, GIP, and glucagon (GCG) receptors), this typically involves demonstrating the ability to stimulate cAMP production in a manner consistent with their intended pharmacological effects on insulin secretion and glucose metabolism.
Measuring cAMP production is a classical method to assess GPCR receptor activity since it reflects the activation of the Gαs-mediated signaling pathway downstream of the receptor and provides a direct and quantitative readout of receptor-mediated signaling. This measurement can be used to compare the potency of different agonists such as semaglutide, tirzepatide, liraglutide, etc.
Eurofins DiscoverX offers MOA-reflective, thaw-and-use cAMP Hunter bioassays that are phase-appropriate for potency testing for GLP-1R and GIPR activation and are rigorously qualified with innovator drugs such as semaglutide, tirzepatide, and retatrutide to establish fit-for-purpose assays for potency and stability testing studies. - How do β-arrestin recruitment and receptor internalization assays contribute to establishing pharmacological profiles for biased agonists targeting the GLP-1, GIP, and glucagon receptors?
The use of dual and triple agonists to initiate synergistic effects in treating obesity and other metabolic diseases is an emerging area of interest. To establish accurate pharmacology for these therapeutics, the three key GPCR readouts – cAMP, β-arrestin, and receptor internalization – are evaluated.
Quantifying β-arrestin activity (recruitment) in response to GPCR activation is a stoichiometric, sustained, and non-amplified readout that closely reflects the in vivo response to receptor activation, while internalization assays track receptor activation and recycling. This dual analysis is instrumental in optimizing multi-agonist therapies, such as achieving the right balance between GLP-1R and GIPR activity to maximize therapeutic effects and minimize side effects.
An example is tirzepatide, recently approved by the FDA that acts as a biased dual agonist, favoring GIPR over GLP-1R activity. The therapeutic exhibits a pronounced cAMP signaling bias over β-arrestin recruitment at the GLP-1R, thereby reducing GLP-1R internalization. - How does overexpression of the GLP-1 receptor impact the potency of the cAMP readout?
Overexpression of the GLP-1 receptor can impact the potency of the cAMP readout. When GLP-1 receptors are overexpressed, the increased receptor density can enhance the sensitivity of the cAMP signaling pathway. This often results in a lower EC50 value, indicating a higher apparent potency of agonists. However, this effect may not accurately reflect the in vivo pharmacological activity, as it is an amplified read-out.
To address this, using a doxycycline-inducible GLP-1R cell line, stimulation with defined concentrations of doxycycline results in reproducible differences in receptor expression – correlating with low, medium, and high receptor densities – providing a more accurate estimation of cAMP EC50. This approach allows for the assessment of agonist potency across different receptor densities, offering a clearer understanding of how receptor expression levels influence signaling. By utilizing these inducible cell lines, researchers can better interpret potency data and ensure that it is relevant and translatable to physiological conditions.
View more Frequently Asked Questions for about Eurofins DiscoverX’s bioassays vs cell lines, Cell Banking Program (including long term support for bioassays), custom method development and qualification services, assay transfer support to CRO/CDMO sites, and more.