FXR Human Liver X Receptor-Like NHR Functional Antagonist Coactivator LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
The farnesoid X receptor (FXR) is a member of the nuclear hormone receptor family of steroid receptors. The FXR receptor forms heterodimers with the retinoid X receptor (RXR) that are activated by bile acid. It is more highly expressed in liver, kidney and intestine and plays an important role in the regulation of the cholesterol 7 alpha hydroxylase, a key enzyme in the bile acid synthesis. When activated, FXR reduces bile acid synthesis and excretion by activation of canalicular transporters in the hepatocytes.
FXR agonists have been shown to be hepatoprotective in cholestatic rat models and in the treatment of chronic cholestatic conditions.
Family:
NHR
Sub Family:
Liver X Receptor-Like
Class:
Non-Steroid
Protein Name:
FXR
Uniprot Number:
Q96RI1
Protein Aliases:
farnesoid X receptor
Gene Name:
NR1H4
Gene ID:
9971
Gene Aliases:
FXR|RIP14|HRR1|HRR-1
Accession Number:
NM_005123
Organism:
Human
Construct Details:
LBD, Recombinant
Assay Information
Assay Type:
Functional
Assay Sub Type:
Protein-Protein Interaction
Functional Mode:
Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Test compound or vehicle is incubated with the farnesoid X receptor (FXR)-LBD and coactivator peptide for 60 minutes at RT. Determination of the amount of complex formed is read spectrofluorimetrically (excitation: 337 nm, emission: 520/490 nm). Test compound-induced increase in TR-FRET ratio by 50 percent or more (≥50%) relative to the 100 µM CDCA response indicates possible FXR receptor agonist activity. Test compound-induced inhibition of 50 µM CDCA-induced fluorescence response by 50 percent or more (≥50%) indicates possible FXR receptor antagonist activity.
Incubation:
1 hr at RT
Control Inhibitor:
DY268
Criteria For Significance:
≥ 50% increase in fluorescence relative to CDCA response, ≥ 50% Inhibition of CDCA-induced fluorescence
Test Concentration / Dose:
Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM
Test Sample Requirements:
75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)
Minimum Order Quantity:
16
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Adverse / Beneficial Action:
FXR agonists have been shown to be hepatoprotective in cholestatic rat models and in the treatment of chronic cholestatic conditions
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
FXR Human Liver X Receptor-Like NHR Functional Agonist Coactivator LeadHunter Assay - TW
Item: 311600-0
FXR Human Liver X Receptor-Like NHR Functional Agonist & Antagonist Coactivator LeadHunter Assay - TW
Item: 311600
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