FXR Human Liver X Receptor-Like NHR Functional Agonist Coactivator LeadHunter Assay - TW

Item: 311600-0

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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:

Agonist

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 Activator:

CDCA

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:

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

23696998

Name

CDCA

Measurement

9.3μM - EC50

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