FXR Agonist Assay Kit (TR-FRET)

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.Assay PrincipleUpon binding of the agonist to the FXR, SRC-1-Biotin and FXR form a heterodimer, resulting in energy transfer from Tb donor to the dye labeled acceptor.

Product Specifications

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.

UniProt

Q96RI1

Format

CatalogNameAmountStorage100410FXR, GST-tag3 µg-80°CSRC-1, Biotin labeled (10 μM in DMSO) 20 µl-80°CCDCA (10 mM in DMSO) 50 µl-20°CFXR Binding Buffer20 ml-20°CTb donor2 x 10 µl-20°CDye labeled acceptor2 x 10 µl-20°C79969384-well plate, white, nonbinding1 EARoomTemp