Recombinant GPCR Proteins

Recombinant Active, Purified Full-length GPCRs for Ligand Discovery, Structural Biology, and Mechanism of Action Studies

G protein-coupled receptors (GPCRs) are the largest family of membrane proteins involved in signal transduction and are the most important targets in drug discovery. These 7-transmembrance receptors convert extracellular signals — such as hormones, neurotransmitters, lipids, and peptides — into intracellular responses via heterotrimeric G proteins and β-arrestin pathways. GPCR signaling regulates key physiological processes, including neurotransmission, metabolism, cardiovascular function, immune activity, and sensory perception. As a result, GPCRs account for a over 40% of approved drugs and remain a central focus of therapeutic development, particularly in the areas of metabolic diseases (obesity/diabetes), oncology and neurodegenerative conditions.

Despite their importance, GPCRs are among the most challenging proteins to study biochemically due to their membrane-embedded architecture, structural flexibility, and dependence on lipid environments for functional stability. High-quality, recombinant full-length GPCRs that retain native conformation and pharmacological activity are therefore critical tools for ligand discovery, structural analysis, and mechanism of action (MOA) investigations.

Leveraging the membrane protein engineering and stabilization expertise of Eurofins CALIXAR, Eurofins DiscoverX provides a growing portfolio of purified, recombinant full-length GPCR proteins and custom protein production capabilities. These receptors are produced using specialized expression and purification technologies designed to maintain structural integrity, correct folding, and functional activity. Each receptor is validated through biochemical characterization including ligand-binding analysis and pharmacological evaluation using agonists and antagonists.

Partner with us to integrate high-quality, research-ready GPCR biochemistry into your discovery workflow and accelerate your path from target validation to therapeutic insight.

Product Highlights
  • Full-Length, Transmembrane GPCR Proteins - Purified receptors retain complete transmembrane architecture, preserving native conformational states important for ligand recognition and signaling studies.
  • Functionally Validated Activity - Each receptor is validated through ligand-binding assays and pharmacological characterization using known agonists and antagonists.
  • Native Structural Integrity - Produced using advanced membrane protein expression and stabilization technologies developed through Eurofins DiscoverX–Calixar expertise.
  • Optimized for Biophysical and Screening Applications - Suitable for biochemical/biophysical assays, structural studies, ligand discovery, and orthogonal validation experiments.

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

SHOP PRODUCTS

Products

New Products

  • A2AR - The A2AR receptor (adenosine A2A receptor) is widely studied for its roles in immunoregulation, inflammation, and central nervous system signaling, emerging as a promising target for Parkinson’s disease, ischemia, and cancer immunotherapy.
  • APLNR - The APLNR receptor (Apelin receptor) is heavily studied for its roles in cardiovascular regulation, metabolism, and angiogenesis, emerging as a promising target for obesity, heart failure, and cancer therapies.
  • GLP-1R - The GLP-1R receptor is intensively studied for its role in glucose regulation and appetite suppression, driving blockbuster obesity and diabetes treatments.
  • MRGPRX1 - The MRGPRX1 receptor is increasingly studied for its roles in pain signalling and neurogenic inflammation, emerging as a promising target for pain management, skin irritation, and inflammatory disorders.
  • MRGPRX2 - The MRGPRX2 receptor is studied for its roles in mast cell activation and allergic responses, emerging as a promising target for chronic skin irritation, drug-induced hypersensitivity, and inflammatory disorders.
  • NK1R - The NK1R receptor is extensively studied for its roles in pain transmission, inflammation, and stress responses, emerging as a promising target for chronic pain, depression, and chemotherapy-induced nausea.

Applications

Eurofins CALIXAR, a Eurofins DiscoverX company, is a leading custom services and products provider with extensive expertise in membrane protein production. GPCR recombinant proteins are offered as off the shelf, ready to use products and rigorously optimized and tested to deliver the highest quality GPCR proteins. These proteins can be used for various applications, such as:

  • Ligand Discovery and Screening — Perform biochemical screening of small molecules, peptides, or biologics targeting GPCR binding sites.
  • Agonist and Antagonist Pharmacology — Characterize receptor activation, inhibition, and ligand selectivity using purified receptor systems.
  • Structural Biology — Support structural studies including cryo-EM, X-ray crystallography, and advanced biophysical analyses.
  • Biophysical Characterization — Study receptor-ligand interactions using techniques such as SPR, MST, or thermal stability analysis.
  • MOA Studies — Investigate ligand binding kinetics, conformational stabilization, and receptor pharmacology.

Product Portfolio

  • Expanding Panel of Therapeutically Relevant GPCRs — Includes receptors implicated in metabolic regulation, inflammation, neurobiology, cardiovascular function, and immune signaling.
  • Purified, Active Transmembrane Receptors — Designed to support ligand discovery, structural biology, and MOA research.
  • Need a receptor not listed? Visit custom protein production and contact us for your request.

Credibility

Eurofins CALIXAR, delivers proven, functional GPCR proteins, trusted by pharma and biotech leaders worldwide.

  • Developed using Eurofins DiscoverX and Eurofins CALIXAR membrane protein engineering expertise.
  • Trusted by leading pharmaceutical and biotechnology organizations for drug discovery, lead optimization, and mechanistic research.
  • Supported by extensive technical documentation, assay data, and expert scientific support.