The FLIPR system is an industry standard for high-throughput kinetic screening of GPCRs and ion channels linked to Ca2+. The instrument uses a cooled CCD camera imaging system to read each well of the microplate at sub-second intervals.
Molecular Devices offers a variety of homogeneous no-wash assay kits for calcium mobilization and membrane potential to support GPCR and ion channel discovery programs.
What Is It?
The FLIPR assay system has significantly increased screening throughput in kinetic assays compared to traditional PMT readers. The high sensitivity of the charge-coupled device (CCD) camera and the flexibility of the SoftMax Pro software allows for optimization of assay conditions and acquisition of data with the highest signal-to-noise ratio.
The assay format is designed to allow both agonists and antagonists to be distinguished from a single screen. A response observed immediately after the addition of test compound indicates agonist activity, while a lack of response to beta-alanine shows a pharmacological antagonist blockade
What Is An Assay Kit?
G-protein coupled receptors and ion channels have been linked to numerous disease states. However, the development of new drugs for these targets has been hampered by time-consuming assays such as radioisotope binding and single cell electrophysiological patch clamping.
FLIPR provides a streamlined and robust assay protocol for real-time kinetic cell assays, enabling high-throughput drug discovery screening. Our FLIPR Tetra System features a novel fluorescent indicator dye with superior masking technology and a simplified, homogeneous assay format to accelerate your drug discovery workflow.
Flipr Membrane Assay Kit
Membrane potential analysis is a key aspect of the functional evaluation of GPCRs and ion channels. Traditionally, electrophysiological patch clamping has been the method of choice for membrane potential monitoring, but it is a labor intensive approach with slow response times. To address this limitation, Molecular Devices offers a new membrane potential assay kit for the FLIPR Fluorometric Imaging Plate Reader system that provides highly informative data comparable to patch clamping with much faster instrument read times.
This kit utilizes a thallium-sensitive indicator dye that passively diffuses into cells as an acetoxymethyl ester. Cytoplasmic esterases cleave the dye into its fluorogenic form, and a proprietary masking agent minimizes background signal. The assay can be used to measure agonists, antagonists, or allosteric modulators of ion channel targets.
What Is A FLIPR Agonist Assay?
GPCRs and ion channels linked to Ca2+ release have been implicated in a variety of diseases. Modulation of Ca2+-permeable ion channels and GPCRs is now recognized as a valid therapeutic strategy. Historically, researchers relied on radioisotope receptor binding assays and single cell conventional patch clamping to identify compounds that modulate Ca2+-permeable GPCRs or ion channels. These methods are time consuming and labor intensive.
FLIPR Tetra enables high throughput kinetic screening assays using no-wash calcium mobilization protocols that cut screening time in half. The platform was demonstrated as a target-agnostic tool with a number of kinase targets including phosphate sensor assays.