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Applications: Useful for screening small molecular FXR agonists for drug discovery and HTS applications.
Background: Nonalcoholic fatty liver disease (NAFLD) is a characterized by the aberrant accumulation of triglycerides in hepatocytes, even in the absence of significant alcohol consumption or viral infection. The FXR is a nuclear receptor that maintains bile acid homeostasis, and aberrant bile acid signaling via activation of FXR contributes liver disease. Several small molecule agonists have been developed and tested in clinical trials for NASH (Non-Alcoholic SteatoHepatitis), and the FXR pathway is also a molecular target in the search for novel cholesterol lowering agents.
Description: The FXR (Farnesoid X Receptor) Agonist Assay Kit (TR-FRET) is designed to measure binding of the FXR and SRC-1 (Steroid Receptor Coactivator 1) for screening FXR agonists using TR-FRET technology. With this homogeneous kit, the FXR agonist assay can be performed by adding all materials, including the detection reagents, to the wells and incubating the plate for 2-hours at room temperature followed by reading the TR-FRET signal.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Supplied As: 384 reaction format
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: 1. Angela D., et al. Targeting Bile Acid Receptors: Discovery of a Potent and Selective Farnesoid X Receptor Agonist as a New Lead in the Pharmacological Approach to Liver Diseases. Front Pharmacol. 2017; 8(162):1-13.
2. Sills M., et al. A Comparison of ALPHAScreen, TR-FRET, and TRF as Assay Methods for FXR Nuclear Receptors. J Biomol Screen. 2002; 7(1):3-10
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