hERG Safety Assay
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The human Ether-à-go-go-Related Gene (hERG) encodes the voltage-gated potassium channel (IKr), a central regulator of cardiac action potential repolarization. Drug-induced inhibition of hERG channels delays myocardial repolarization, prolonging the QT interval and triggering life-threatening ventricular arrhythmias such as Torsade de Pointes (TdP). Historical data reveals that more than 30% of drug withdrawal cases result from hERG-related cardiotoxicity which highlights the essential requirement for early-stage hERG liability screening in drug development.
Our hERG Safety Assay Service
QPatch platforms
Our hERG Safety Assessment integrates automated patch clamp platforms (QPatch) with biochemical and fluorescence polarization assays, offering a tiered strategy for cardiac risk mitigation:
- pA-Level Sensitivity: Direct measurement of native hERG currents in physiological saline (>1 GΩ seal, no additives).
- Dynamic Exposure Simulation: 0.5-sec microfluidic gradient perfusion for precise in vivo PK simulation (Cmax peak).
- High-Throughput Precision: 48-channel parallel detection (200+ samples/day) with >95% concordance to manual patch clamp (R²).
Workflow
Step 1: Compound Reception and Preparation
Compounds provided by the client will undergo rigorous quality testing and concentration verification.
Step 2: Experiment Setup
Choose the cell line and set the inhibition test concentration according to the experimental design.
Step 3: Data Collection
Use QPatch to analyze electrophysiological parameters of the samples.
Step 4: Result Analysis
Calculate the inhibition rate and half-maximal inhibitory concentration (IC50).
Step 5: Report Generation
Provide a detailed experimental report and data interpretation.
Protocol
| Parameter | Standard Protocol | Customizable Options |
| Instrument | QPatch Automated Patch Clamp System | Manual patch clamp (upon request) |
| Analysis Method | Whole-cell voltage clamp mode | Custom voltage protocols |
| Cell Line | CHO-hERG, HEK293-hERG | iPSC-derived cardiomyocytes (pre-assessment required) |
| Test Concentration Range | 0.1, 1, 10 μM | Client-specified concentrations or extended ranges |
| Sample Requirements | 100 μL of 10 mM DMSO solution | Special handling for low-solubility compounds |
| Data Delivery | - Raw current traces & concentration-response curves - Mean inhibition rate ± SEM - IC50 calculation (four-parameter logistic fit) |
Raw data files |
Features
High-Throughput Screening
Quickly process a large number of compounds, ideal for large-scale screening projects.
Experienced Team
Our scientific team has extensive experience in hERG research and can provide professional advice to clients.
Comprehensive Support
Provide full-service support from detection to result analysis, meeting the needs of different clients.
FAQ
1. Why is the study of hERG inhibition important?
Studying hERG inhibition is crucial because the hERG potassium channel is essential for cardiac repolarization. Inhibition of this channel can prolong the QT interval on an electrocardiogram, potentially leading to life-threatening ventricular arrhythmias such as Torsade de Pointes. Identifying compounds that inhibit hERG early in drug development helps prevent late-stage clinical failures and ensures the cardiac safety of new pharmaceuticals.
2. What is the relationship between in vitro hERG inhibition and in vivo cardiac toxicity?
The purpose of in vitro hERG inhibition assays is to forecast whether a compound might extend the QT interval in living organisms leading to cardiac toxicity. When scientists conduct tests on compounds using in vitro methods they determine how those compounds interact with hERG channels and can forecast potential cardiac side effects in humans. The correlation of in vitro results with in vivo effects represents an essential step in the assessment of a drug's safety profile before starting clinical trials.
3. How does hERG support drug development?
During the drug discovery phase hERG screening helps drug development by pinpointing cardiac safety risks at an early stage. Researchers can select drug candidates with minimal safety risks by analyzing their interactions with the hERG channel which decreases the chance of failures during later development stages. Additionally, insights from hERG research direct medicinal chemistry strategies to enhance compound safety which facilitates the development of safer therapeutic drugs.
4. Does showing inhibition in the hERG Safety Assay mean the compound cannot proceed to clinical trials?
Not necessarily. While hERG inhibition is a potential marker for cardiac toxicity, it must be evaluated in conjunction with other experimental data (such as in vivo studies and preclinical pharmacological research). In some cases, cardiac toxicity risk can be reduced through structural optimization or adjustments to the dosing regimen.
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