Ion Channel Screening
INQUIRYBOC Sciences is committed to providing high-quality ion channel screening services for various fields, including biomedicine, neuroscience, cardiovascular diseases, cancer research, and drug safety assessment. Ion channels play a central role in critical physiological processes such as cellular signal transduction, membrane potential regulation, neural transmission, and myocardial contraction. They are among the key therapeutic targets for numerous diseases, particularly in the development of central nervous system drugs, anti-arrhythmic drugs, and analgesics. With advanced platforms and a comprehensive technical system, BOC Sciences offers clients end-to-end solutions from early screening to candidate drug validation.
Service Highlights and Advantages
- Multi-platform integration: Combining automated patch clamp, fluorescence imaging, MEA, and VSFP for multidimensional screening.
- Broad channel target coverage: Over 30 mainstream ion channel targets spanning neuroscience, cardiovascular, immunology, oncology, and more.
- Cost-effective compound libraries: Screening available for up to 5 million lead compounds.
- Multi-mode support: Functional screening, affinity determination, electrophysiological kinetic analysis, selectivity validation, off-target screening, etc.
- Customized screening solutions: Experimental design, channel selection, dose setting, and data output format can all be flexibly customized to client needs.
- Strict quality control: All procedures follow strict SOPs, with QC standards at key steps to ensure data comparability and reproducibility.
Ion Channel Screening and Profiling Services
Our ion channel screening services are built upon various modern technological platforms, including but not limited to patch clamp electrophysiology, automated electrophysiology systems (such as QPatch, PatchXpress), fluorescence imaging analysis (e.g., FLIPR), membrane potential assays, and calcium flux assays. These platforms support multiple screening modes including agonist/antagonist functional testing, channel kinetics evaluation, dose-response analysis, and high-throughput screening (HTS), suitable for various ion channel types.
Automated Patch Clamp Systems
BOC Sciences employs internationally advanced automated patch clamp platforms, including QPatch, PatchXpress, and SyncroPatch. These platforms are widely used for dose-response analysis, IC₅₀/EC₅₀ determination, and electrophysiological characterization of ion channel drugs, offering the following advantages:
- High-throughput screening: Rapid parallel testing of hundreds of compounds.
- High data consistency and reproducibility: Standardized operational workflows significantly reduce manual errors.
- Compatibility with various cell types: Including stably expressing cell lines, primary cells, and iPSC-derived cells.
- Support for multiple channel types: Voltage-gated, ligand-gated, mechanosensitive channels, and more.
Fluorescent Membrane Potential Assays
We are equipped with the FLIPR® Tetra high-throughput fluorescence imaging platform, using membrane potential-sensitive dyes for rapid screening. This non-invasive and sensitive method is especially suitable for large-scale small molecule screening and structure-activity relationship (SAR) analysis of channel modulators. Applicable to:
- Functional screening of sodium, potassium, and chloride channel modulators.
- Real-time monitoring of membrane potential changes.
- High-throughput primary screening and secondary confirmation assays.
Calcium Flux Assay Platform
BOC Sciences utilizes calcium flux detection technology based on indicators such as Fluo-4 AM, in combination with the EnVision® multimode plate reader. This platform is well-suited for high-throughput screening of ligand-gated calcium channels (e.g., P2X, TRP families), enabling:
- Calcium signaling monitoring post activation of calcium channels and related GPCRs.
- Evaluation of intracellular calcium concentration changes following channel opening or blockage.
- Time-resolved analysis and multi-point parallel measurements.
Multi-Electrode Array (MEA) System
To assess the impact of drugs on cardiomyocytes or neuronal electrical activity, BOC Sciences offers services based on the Axion Maestro MEA system. MEA technology enables systematic evaluation of channel function, network behavior, and pharmacological effects by:
- Real-time recording of cell network firing frequency, pacing behavior, and electrophysiological features.
- Supporting QT interval prolongation prediction and arrhythmia risk screening.
- Compatible with lentiviral or AAV-mediated overexpression models of ion channels.
High-Throughput Screening (HTS) Systems
BOC Sciences is equipped with a complete high-throughput screening automation platform that integrates compound distribution, liquid handling, and data acquisition. This system significantly enhances screening efficiency and shortens the discovery-to-validation cycle for candidate compounds.
- Integrates FLIPR, automated patch clamp, and plate readers for unified screening of various channel mechanisms.
- Supports 384-well and even 1536-well plate formats to meet large-scale compound library screening needs.
- Customizable dose gradients, compound treatments, and dynamic data collection at multiple time points.
- Compatible with in-house or client-supplied channel-expressing cell lines for exclusive target screening.
Cellular Models & Assay Systems
BOC Sciences provides a variety of physiologically relevant cellular models and assay systems to support complex ion channel functional studies. We offer customized cell line construction and screening system design services based on client needs to ensure biological relevance and translational value of experimental outcomes.
- Stably transfected channel cell lines (e.g., Nav1.5, hERG, TRPV1, Cav1.2, etc.).
- iPSC-derived cardiomyocytes/neurons for safety evaluation.
- CRISPR/Cas9-edited models for mutant channel function studies.
- Multi-parameter functional assays combining membrane potential, calcium signals, electrical activity, and morphological indicators.
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BOC Sciences integrates innovative technologies to empower your drug discovery with strong momentum, fully dedicated to building next-generation drug screening platforms.
Ion Channel Targets Supported by BOC Sciences
BOC Sciences offers functional screening and mechanistic research services for a wide range of ion channel targets, covering core targets for conventional drug development as well as emerging and disease-specific channel types. We support a full pipeline from lead compound screening to mechanistic validation.
| Ion Channel Class | Representative Subtypes/Families | Functional Features | Drug Discovery Applications |
|---|---|---|---|
| Sodium Channels (Na⁺) | Nav1.1 – Nav1.9 | Voltage-gated; responsible for action potential initiation and propagation | Neuropathic pain, epilepsy, multiple sclerosis, arrhythmia |
| Potassium Channels (K⁺) | Kv1.x, Kv7.x, Kir, hERG | Maintain resting membrane potential and regulate action potential duration | Anti-epileptic, antihypertensive, anti-arrhythmic drugs; hERG for safety screening |
| Calcium Channels (Ca²⁺) | Cav1.x (L-type), Cav2.x, Cav3.x | Mediate Ca²⁺ influx, involved in signal transduction, contraction, neurotransmission | Cardiovascular diseases, neurodegeneration, pain therapeutics |
| TRP Channels | TRPV1, TRPM8, TRPA1, etc. | Mostly non-selective cation channels, responsive to temperature and chemical stimuli | Pain, inflammation, cancer; widely studied for novel analgesics |
| Ligand-Gated Ion Channels | GABA_A, NMDA, AMPA, 5-HT3 | Activated by neurotransmitters or small molecules; regulate neuronal signaling | Epilepsy, anxiety, depression; key CNS drug targets |
| ATP-Gated Ion Channels (P2X) | P2X1 – P2X7 | Activated by extracellular ATP; modulate inflammation and immune response | Inflammatory and autoimmune diseases, immunomodulators |
| Acid-Sensing Ion Channels (ASIC) | ASIC1a, ASIC2a, etc. | Respond to extracellular pH changes; involved in pain and ischemia | Stroke, inflammatory pain, neuroprotection |
| Cyclic Nucleotide-Gated Channels (CNG) | CNGA1, CNGB1, etc. | Activated by cAMP or cGMP; present in sensory neurons | Retinal diseases, olfactory disorders |
| Mechanosensitive Channels | Piezo1, Piezo2, NALCN | Respond to mechanical stress and ion changes; regulate cell volume and mechanosensation | Oncology, immunology, respiratory and neuroscience research |
| Chloride Channels (Cl⁻) | CFTR, ClC-2, ClC-K, ANO1 | Regulate osmotic pressure, secretion, and electrical stability | Cystic fibrosis, cancer, IBD, respiratory disorders |
| Proton Channels (H⁺) | HVCN1 | Regulate proton flow; maintain redox balance and immune activity | Tumor microenvironment, immune response, antibacterial development |
| Inward Rectifier K⁺ Channels (Kir) | Kir2.x, Kir6.x (K_ATP) | Modulate cardiac and pancreatic β-cell excitability | Diabetes, arrhythmia, metabolic disorders |
| Gap Junction Channels | Connexin 43, etc. | Enable intercellular transfer of small molecules and ions | Heart disease, cancer metastasis, neurodegeneration |
| Na⁺/Ca²⁺ Exchangers (NCX) | NCX1, NCX2 | Regulate intracellular calcium and membrane potential | Heart failure, ischemic stroke, neuroprotection |
| Ca²⁺-Activated K⁺ Channels (K_Ca) | BK (large-conductance), SK (small-conductance) | Activated by intracellular calcium; modulate excitability and vascular tone | Hypertension, Parkinson's disease, respiratory disorders |
| Zinc Channels (Zn²⁺) | ZIPs, ZnTs | Regulate intracellular zinc levels; involved in signaling and apoptosis | Neuroprotection, immune modulation, anticancer therapies |
| Na⁺/H⁺ Exchangers (NHE) | NHE1 – NHE9 | Mediate ion exchange to regulate intracellular pH and osmotic balance | Cardiovascular disease, cancer, metabolic disorders |
Project Workflow
Project Requirement Confirmation
Through in-depth communication with clients, we clarify ion channel types, detection methods, sample types, and sample quantities. This ensures clear project objectives and alignment with the client's research or drug development goals, laying the groundwork for effective execution.
Experimental Design and Platform Selection
Based on target characteristics and client needs, we select suitable platforms such as membrane potential assays, fluorescence imaging, or patch-clamp techniques. The focus is on sensitivity, reproducibility, and data accuracy to ensure reliable and high-quality experimental results.
Sample Preparation and Quality Control
We verify compound purity, prepare concentration gradients, and select or generate stable cell lines expressing the target ion channels. Strict quality control is applied throughout to maintain consistency and ensure both sample and cellular conditions are optimal.
Functional Assay and Data Acquisition
Using the selected platform, we perform functional assays to assess agonist or antagonist activity. Real-time data on currents, membrane potential, or calcium flux are collected, with each step documented to support detailed downstream analysis.
Data Analysis and Reporting
Our data team processes raw data to calculate IC₅₀/EC₅₀ values and generate dose-response curves. Comprehensive reports include methodology, data interpretation, and visualized results, enabling clients to quickly understand outcomes and make informed decisions.
Technical Support and Follow-up Services
We provide ongoing technical support, including result validation, cross-target selectivity testing, and assistance with mechanistic studies. Clients can customize extended services, ensuring professional support throughout ion channel screening and validation stages.
Applications of Ion Channel Screening
Drug Discovery Research
Ion channels are key targets in the treatment of many diseases. BOC Sciences utilizes high-sensitivity ion channel screening technologies to help drug development teams discover and validate agonists, antagonists, and modulators, thereby facilitating the identification and optimization of novel lead compounds and significantly improving the efficiency and success rate of drug development.
Drug Safety Evaluation
In drug safety evaluation, inhibition testing of the cardiac potassium channel hERG is particularly important. BOC Sciences offers professional electrophysiological testing platforms to screen cardiac toxicity risks of candidate drugs at an early stage, helping avoid potential safety issues and ensuring clinical safety of new drugs.
Discovery of Drug Tool Molecules
Through functional screening of ion channels, BOC Sciences supports the identification of specific drug tool molecules, providing essential tools for studying ion channel functions under physiological and pathological conditions. This facilitates deeper understanding of channel mechanisms and drug action modes, promoting both basic and translational research.
Disease Mechanism Research
Ion channels play a central role in neurological, cardiovascular, immune, and metabolic diseases. BOC Sciences uses various detection methods to assist researchers in analyzing abnormal expression and functional changes of ion channels, revealing mechanisms of disease onset and progression, and providing scientific evidence for targeted therapies.
FAQs
What types of ion channels can BOC Sciences screen?
We can screen a variety of voltage-gated and ligand-gated ion channels, including sodium channels (Na⁺), potassium channels (K⁺), calcium channels (Ca²⁺), chloride channels (Cl⁻), and ligand-gated ion channels (such as GABA, NMDA, nAChR). Customized target screening services are also available for specific research needs.
Can compounds other than small molecules be screened?
Yes. Our ion channel screening services are applicable to various molecular forms including small molecules, natural products, peptides, biologics, and antibodies. We select suitable cell models and detection platforms based on the molecular characteristics to ensure high-quality, reproducible functional screening data.
Do you support high-throughput compound library screening?
Yes. BOC Sciences is equipped with automated systems and high-throughput screening platforms capable of evaluating the ion channel activity of thousands of compounds in a single batch. This is especially suitable for large-scale primary screening in early drug discovery, with consistent and statistically reliable data.
Do you offer hERG and other safety screening services?
Yes. We provide hERG potassium channel inhibition assays to help clients identify potential cardiac toxicity risks at an early stage. Additionally, we can evaluate the function of other cardiac-related channels (e.g., Nav1.5, KCNQ1, Kv4.3) upon request.
How long does the experiment typically take?
The specific timeline depends on project complexity, sample quantity, and screening methods. Routine single-target functional screening usually takes 2–3 weeks, while high-throughput or multi-target cross-screening projects may take 4–6 weeks. We will confirm the detailed schedule with clients during project planning and maintain timely communication.
What does the experimental data report include?
We provide comprehensive experimental data reports covering experimental design and procedures, information on cell lines and channels used, detection platforms and reagents, data charts (e.g., dose-response curves), key parameters (e.g., IC₅₀/EC₅₀), summaries of raw data, and technical analysis suggestions. Reports are available in both PDF and Excel formats for archiving and subsequent research use.
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