Authors
Creative Bioarray
Summary
FluxOR™ thallium assay has been widely recognized for hERG activity test. This assay is optically based and can be performed on 96-well or 384-well plates as a homogenous assay for high-throughput screening (HTS) measurements of potassium ion channel and transporter activities.
Acroscell provides FluxOR™ assays and services for HTS measurements of potassium ion channels in evaluating drug effects on potassium channel activity.
Introduction
FluxOR™ thallium assay is carried out in a physiological, normal-chloride saline. Multiple potassium channels including Kv1.3, Kv7.2/Kv7.3, Kv11.1 (hERG), Kir1.1, Kir2.1, Kv1.1, Kv2.1 are expressed in cell lines. Using these cells, FluxOR™ assay can be run to identify and characterize channel-specific inhibitory compounds provided by customers. The FluxOR™ assay has been proven identified several known specific inhibitors of Kv7.2/7.3 or hERG, highlighting its potential to identify novel and more efficacious small-molecule modulators.
This assay is based on the permeability of potassium channels to thallium. To run the assay, cells are loaded with non-fluorescent, thallium-specific FluxOR™ dye. The thallium ions flow freely through open potassium channels, acting as a surrogate indicator of potassium ion channel activity. When potassium channels are opened by a stimulus, the activation of FluxOR™, a novel fluorescent dye with a high affinity for thallium can report channel activity showing a large fluorogenic response that is proportional to the number of open potassium channels on the cell, making it extremely useful for studying K+ channel targets.
The activity of ion channels and transporters that are permeant to thallium can be quantitatively indicated by the fluorogenic signal change. Fluorescence reported in the FluxOR™ system thus becomes a surrogate indicator of activity for any ion channel or transporter that is permeable to thallium.
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