hERG Safety Evaluation

As a leading enterprise in the fields of pharmacology and biology, Creative Biolabs strives to provide you with a comprehensive hERG safety assessment, catering to your needs for safety pharmacology and cardiac toxicity screening with our profound expertise and cutting-edge technology platforms.

hERG Safety Assessment: Guidelines for Cardiac Toxicity

The hERG gene encodes the cardiac potassium channel, and its blockade by drug compounds can result in delayed rectifier potassium currents and diminished repolarization reserve, consequently prolonging the QT interval on surface electrocardiograms and potentially leading to Torsades de Pointes (TdP). Due to these detrimental cardiac effects, the current drug regulatory guidelines explicitly consider the impact on hERG channels as an indispensable component of preclinical drug development.

hERG Safety Evaluation. (Ridder, 2020) Fig 1. hERG Safety Evaluation.¹

hERG Safety Assessment Protocol

We have meticulously designed and optimized a robust hERG safety assessment protocol, employing comprehensive in vitro proarrhythmia assays, to promptly identify any potential hERG blockade associated with candidate compounds in early-stage drug discovery.

Analysis Approaches	Our recommended approach based on electrophysiology and automated planar patch clamp technology. Our platforms enable parallel execution of numerous independent whole-cell patch clamp experiments or perforated assays on hundreds of single-cell arrays, rivaling the performance of conventional single-cell patch clamp methodologies.
Sample Requirements	For standardized testing procedures, we mandate a minimum of 100 μL 10 mM solution samples. In addition to our extensive test library encompassing hundreds of distinct compounds, we also accommodate the incorporation of client-provided samples. For specific sample submission formats, kindly consult our esteemed technical team.
Testing Protocol	By default, stable transfected HEK293 cells will be employed to yield reproducible measurement outcomes. Each test compound will undergo a five-minute exposure test in two different cells, utilizing three sequentially escalating concentrations.
Quality Control	Our default testing protocol incorporates E-4031 as a positive control, a validated hERG potassium channel blocker. As for the negative control, we employ DMSO at preset concentrations.
Data Output	Sealing formation, cell perforation, and electrophysiological detection processes are meticulously controlled and meticulously recorded through our automated systems. In the event of relevance, we are also capable of presenting average inhibition percentages and IC50 determination data.

Our Services

Empowered by cutting-edge electrophysiology testing platforms, Creative Biolabs offers comprehensive assessment services to estimate the potency of compound-mediated hERG blockade. Our team of accomplished experts is unwaveringly committed to providing consistently high-quality predictive data on cardiotoxicity evaluation, and we remain flexible in accommodating specific protocol adjustments and tailored methodologies to align with your unique requirements.

Cardiotoxicity Evaluation by Cardiac Organoid Model

Cardiotoxicity Evaluation by Precision-Cut Human Heart Slice Model

Cardiotoxicity Evaluation by 3D Cardiac Spheroid Model

Cardiotoxicity Evaluation by Ex vivo Human Cardiovascular Tissue Model

Cardiotoxicity Evaluation by iPSC-derived Cardiomyocytes

hERG Safety Evaluation

At Creative Biolabs, we pride ourselves on fostering meaningful collaborations that drive scientific progress. Contact us today for any of your needs.

Reference

Ridder, B.; et al. A systematic strategy for estimating hERG block potency and its implications in a new cardiac safety paradigm. Toxicology and Applied Pharmacology. 2020, 394: 1114961.

Research Model

3D Biology Based Biomarker Discovery

3D Biology Based Drug Discovery and Development

3D Biology Based Toxicity Evaluation

Supporting Assays

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