GPCR Assays

Comprehensive and versatile GPCR assays

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G protein-coupled receptors stand as the gatekeepers to cellular communication, representing the largest and most versatile family of drug targets. With recent advancements in GPCR pharmacology, understanding these receptors is more crucial than ever. With decades of experience in pharmacology, PharmaLegacy is ready to empower you to delve deeper into the world of GPCRs with a comprehensive suite of assays and services:

  • Extensive Cell Line Library: Choose from over 400 pre-characterized GPCR cell lines, covering a wide range of GPCR types (Gs, Gq, and Gi), readily available for your specific needs
  • Tailored Cell Line Engineering: Can’t find the perfect line? We offer a stable cell line generation service, including overexpression, knock out, knock in, knock down, mutation, and report gene integration, to create the ideal model for your research.
  • High-Throughput Screening: Accelerate your discovery process with our 384-well assay format, ensuring efficient and reliable data generation.

 

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GPCR Assays

MODELS / SERVICES

Gα (Gq)

  • Leads to increased Ca2+ by activation of the phospholipase C (PLC) pathway, ultimately producing IP3
  • Calcium flux assay using FLIPR
  • IP-1 HTRF assay

Gαs (Gs)

  • Leads to an increase in intracellular cAMP via the stimulation of adenylate cyclase (AC) pathway
  • cAMP HTRF assay

Gαi (Gi)

  • Leads to a decrease in intracellular cAMP via the inhibition of adenylate cyclase (AC) pathway
  • cAMP HTRF assay

Beta Arrestin Assay

  • Nano-BRET/Nano Bit
  • Enzyme fragment Complementation (EFC) technology

GPCR internalization

  • HiBit method
  • Gene synthesis, plasmid construction
  • Antibiotics kill curve
  • Transient transfection and selection
  • Cell clone selection with antibiotic
  • Function assay test in pooled cells to confirm positive signal
  • Obtained single cell clone and expand (0.5 cells/well in 96 well plate)
  • Primary single cell clone screening (agonist mode, single point)
  • Positive clone confirmation (agonist and antagonist mode, dose response)
  • Positive clone cell bank, mycoplasma detection, cell line QC
  • Cell line stability test (up to 25 passages)

 

Committed to quality:

  • FDA part 11 compliant
  • Animal studies strictly follow AAALAC and ILAC guidelines
  • Electronically managed, traceable research data
  • Rigorous adherence to international GLP and QA best practices
  • Clients have real-time remote monitoring of studies

Want your scientific discoveries to become treatments? PharmaLegacy’s the right partner for you.

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Providing Better Data For Critical Oncology Pipeline Decisions

To advance a compound from discovery to clinical, or to halt its development, is a huge and costly decision. For the benefit of you and your company, and for the well-being of patients in need of treatment, that decision needs to be based on correct information.

Download our Integrated In Vitro Oncology Assays brochure and see why over 300 pharmaceutical companies, including many global leaders, trust PharmaLegacy for the unbiased, accurate information they need to make critical oncology pipeline decisions.

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