Achieve ROI in pain drug discovery with robust high-throughput NaV1.9 screening

Na_V1.9 is a key ion channel target for pain drug discovery, particularly for development of novel non-opioid treatments for chronic pain. However, the path to progressing therapies targeting Na_V1.9 has been blocked by lack of robust and reliable Na_V1.9 high-throughput screening assays.

Metrion has overcome these obstacles with a Na_V1.9 screening cascade, built upon a robust and stable hNa_V1.9 cell line, using automated patch-clamp technology and translational assays. This solution delivers high-quality reproducible data allowing rapid hit identification, hit expansion and SAR.

Unique approach to Na_V1.9 drug discovery for faster, smarter, cost-effective screening

Our Na_V1.9 suite of services supported by highly experienced electrophysiologists, lead by a Leadership team with over 100 years’ experience in drug discovery research, sets the Metrion service apart from others. The business case is clear for organisations looking to rapidly meet project milestones:

• Shorter timelines: High-quality screening assays accelerate project milestones.
• Lower costs: Reliable screening data to robustly support medicinal chemistry.
• Cost-effective outsourcing: Rapid, expert data interpretation ensures confident advancement of promising compounds.
• High confidence in Na_V1.9 screening cascade:
  • Identify high quality hits
  • Accelerate hit-to-lead discovery
  • Investigate mechanism of action via translational assays

For business leaders, this translates into:

• Higher ROI

Figure 1: Na_V1.9 screening cascade – Metrion’s unique, integrated approach to Na_V1.9 drug discovery.

Reliable, high-throughput Na_V1.9 screening for faster, consistent and accurate results

Our validated, high-throughput Na_V1.9 screening solution delivers consistent and accurate results. Key advantages:

• High-throughput Na_V1.9 screening for rapid compound testing: The CHO-hNa_V1.9 cell line, developed in-house by Metrion, enables automated patch-clamp screening using the Qube 384 platform. This system allows rapid testing of large compound libraries and hit-to-lead support.
• Reliable Na_V1.9 data, fewer setbacks: The stable and robust expression of Metrion’s Na_V1.9 cell line ensures high reproducibility and low assay variability. We have demonstrated high sensitivity, robustness and accuracy of Na_V1.9 screening data during the assay development with the testing of tool compounds and compound plates randomly spiked with a Na_V1.9 inhibitor.

The business challenge: Missed opportunities

The Na_V1.9 ion channel is a promising target for developing non-opioid chronic pain treatments, but challenges in establishing screening assays have slowed progress across the industry. Key issues include:

• Functional expression challenges: difficulty in expressing Na_V1.9 in stable heterologous systems.
• Biophysical properties: activation and inactivation kinetics of Na_V1.9 require voltage-control only offered by automated electrophysiological techniques.

Metrion's unique approach overcomes these challenges and unlocks the potential for increased ROI in pain drug discovery.

Contract research services for preclinical drug discovery beyond Na_V1.9

Beyond Na_V1.9, Metrion offers an extensive portfolio of ion channel screening services, including validated assays for the full Comprehensive in vitro Proarrhythmia Assay (CiPA) panel for cardiac safety assessment: hERG, hNav1.5, hCav1.2, hKir 2.1, hKv 4.3/KChIP, hKv LQT1/minK, Late Nav1.5.

This breadth allows customers to consolidate their ion channel research needs with a single provider, streamlining project management and communication.

Take the next step: Accelerate your drug discovery pipeline with Metrion

Don’t let Na_V1.9 screening challenges stall your pipeline. Partner with Metrion to access reliable, high-throughput solutions designed for success - contact us today: