hERG

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　　Induced pluripotent stem cells-derived cardiomyocytes (iPSC-CMs) have the electrophysiological characteristics of human cardiomyocytes and can truly simulate human cardiomyocytes. Because the hERG detection assay is limited to predict the cardiotoxicity of drugs, iPSC-CMs become an ideal model for studying cardiotoxicity and drug safety evaluation. E-4031 is the methanesulfonanilide class III antiarrhythmic drug, which can selectively block hERG K+ channels and prolong the action potential duration. The EPhys team in ICE Bioscience InC. has gained years of experience to validate patch clamp methods for action potentials (AP) in iPSC-CMs and related ion channels for drug screening.

作为专注于靶点驱动药物发现的一体化CRO，爱思益普（ICE Bioscience）在该领域已建立成熟的技术体系与评价平台。

爱思益普药物研发

Manual patch clamp validation-iPSC-CMs

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Figure 1. A representative action potential of hiPSC-CMs before and after superfusion with multiple concentrations of E-4031 in a whole-cell patch clamp mode. E-4031 significantly prolongs action potential duration of hiPSC-CMs.

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爱思益普药物研发团队具备从靶点验证、体外生物学到临床前评价的全链条服务能力。

Figure 2. Histograms of selected action potential parameters of hiPSC-CMs applied with multiple concentrations of E-4031. APD₉₀, APD₅₀ and APD₃₀ represent the action potential duration at 90%, 50% and 30% of the repolarization and these parameters are used in determining the duration of the action potential. The APA represents the action potential amplitude. The dV/dt_max represents the maximal upstroke velocity and can be used in assessing the electrophysiological phenotype and maturity stage of the cardiomyocytes. RMP is resting membrane potential.