Cardiac assays to assess proarrhythmic liability of compounds

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𝗜𝗺𝗽𝗿𝗼𝘃𝗲 𝗲𝗳𝗳𝗶𝗰𝗶𝗲𝗻𝗰𝘆, 𝗿𝗲𝗱𝘂𝗰𝗲 𝗹𝗮𝘁𝗲-𝘀𝘁𝗮𝗴𝗲 𝗳𝗮𝗶𝗹𝘂𝗿𝗲𝘀, 𝗮𝗻𝗱 𝗮𝗹𝗶𝗴𝗻 𝘄𝗶𝘁𝗵 𝗿𝗲𝗴𝘂𝗹𝗮𝘁𝗼𝗿𝘆 𝘀𝘁𝗮𝗻𝗱𝗮𝗿𝗱𝘀 𝗯𝘆 𝗮𝘀𝘀𝗲𝘀𝘀𝗶𝗻𝗴 𝘁𝗵𝗲 𝗽𝗿𝗼𝗮𝗿𝗿𝗵𝘆𝘁𝗵𝗺𝗶𝗰 𝗹𝗶𝗮𝗯𝗶𝗹𝗶𝘁𝘆 𝗼𝗳 𝘆𝗼𝘂𝗿 𝗰𝗼𝗺𝗽𝗼𝘂𝗻𝗱𝘀 𝗲𝗮𝗿𝗹𝘆Metrion’s specialist scientists utilise single-point or four-point concentration-response assays to ensure you 𝗶𝗱𝗲𝗻𝘁𝗶𝗳𝘆 𝗽𝗿𝗼𝗮𝗿𝗿𝗵𝘆𝘁𝗵𝗺𝗶𝗰 𝗿𝗶𝘀𝗸𝘀 𝗲𝗮𝗿𝗹𝘆. The potency data derived from high-fidelity platforms such as automated patch-clamp and the gold standard manual patch-clamp technique, is suitable for use in 𝘪𝘯 𝘴𝘪𝘭𝘪𝘤𝘰 action potential models. Our full cardiac ion channel panel includes: • hERG (including a robust, dynamic hERG assay) • KᵥLQT1/minK • hKᵥ4.3/KChIP • hCaᵥ1.2 • hNaᵥ1.5 (peak and late) • hKᵢᵣ2.1 Screening services against hHCN4 and hKᵥ1.5, which play important roles in controlling human heart rate and atrial repolarisation, respectively, are also provided. Contact us today: https://hubs.la/Q033tZYy0

Improve efficiency, reduce late-stage failures, and align with regulatory standards by assessing the proarrhythmic liability of your compounds early. The potency data derived from high-fidelity platforms such as automated patch-clamp and the gold standard manual patch-clamp technique, is suitable for use in in silico action potential models. Our full cardiac ion channel panel includes: hERG (including a robust, dynamic hERG assay), KVLQT1/mink, hKV4.3/KChIP, hCaV1.2, hNaV1.5 (peak and late), hKIR2.1. Screening services against hHCN4 and hKV1.5, which play important roles in controlling human heart rate and atrial repolarisation, respectively, are also provided.

 

Learn more about our cardiac ion channel panel.

 


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Nav1.5 late current in WT and Nav1.5-ΔKPQ mutant channels: an automated patch clamp LQT3 electrophysiological assay comparison

The cardiac late Na+ current (late INa) generates persistent inward currents throughout the plateau phase of the ventricular action potential and is an important determinant of repolarisation rate, EADs and arrythmia risk¹. As inhibition of late INa can offset drug effects on hERG and other repolarising K⁺conductances, it is one of the key cardiac channels in the Comprehensive in vitro Pro-arrythmia Assay (CiPA) panel being developed by the FDA to improve human clinical arrythmia risk assessment²̛ ³.

Development of an impedance-based screening assay for cardiac safety and cardiotoxicity detection in stem cell-derived cardiomyocytes

Cardiac toxicity remains the leading cause of new drug safety side-effects. Current preclinical cardiac safety assays rely on in vitro cell-based ion channel assays and ex vivo and in vivo animal models⁽¹⁾. These assays provide an indication of acute risk but they do not always predict the effect of chronic compound exposure, as recently seen with oncology drugs. Therefore, new assays are required to characterise chronic structural and functional effects in human cells earlier in drug discovery. Impedance-based technology can provide more accurate chronic cardiotoxicity measurements in an efficient manner using human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs).

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Metrion Biosciences is a contract research organisation (CRO) specialising in high-quality preclinical drug discovery services.
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