SRP2137

FXR, ligand binding domain (222-472), GST tagged human

recombinant, expressed in E. coli, ≥70% (SDS-PAGE)

• Synonym(s): FXR, NR1H4, farnesol receptor HRR-1, retinoid receptor
• UNSPSC Code: 12352200
• NACRES: NA.26

Properties

• biological source: human
• recombinant: expressed in E. coli
• Assay: ≥70% (SDS-PAGE)
• form: frozen liquid
• mol wt: ~56.3 kDa
• packaging: pkg of 10 μg
• storage condition: avoid repeated freeze/thaw cycles
• concentration: 400 μg/mL
• color: colorless to clear
• NCBI accession no.: U68233
• UniProt accession no.: Q96RI1
• shipped in: dry ice
• storage temp.: −70°C
• Gene Information: human ... HRR-1(9971)

Description

Biochem/physiol Actions

Farnesoid-X-activated receptor (FXR) was originally identified and cloned in rat as an orphan nuclear hormone receptor based on hybridization with a degenerate oligonucleotide designed from the highly conserved nuclear hormone receptor DNA binding domain. FXR functions as a heterodimer with RXR and binds to sequence elements in the promoters of target genes. The FXR/RXR heterodimer binds with highest affinity to inverted repeats separated by 1 bp (IR-1) and with low affinity to direct repeats separated by 4 and 5 bp (DR-4 and DR-5). As is the case for other nuclear hormone receptors, FXR regulates target gene activity in response to ligand. While initial studies suggested that farnesol and retinoid metabolites were likely ligands for FXR, current data support the notion that FXR is a bile acid sensor that plays an integral role in bile acid synthesis and transport. In the small intestine, FXR regulates bile acid uptake through the upregulation of the ileal bile acid binding protein gene via binding to an upstream response element. The FXR/RXR heterodimer can be activated by the bile salt chenodeoxycholic acid (CDCA) and FXR is required for the bile salt-dependent transcriptional control of the human ABCB11 gene (the bile salt export pump). In addition, FXR has been shown to inhibit the cholesterol 7-hydrolase gene (CYP7A1) transcription.

Physical form

Clear and colorless frozen liquid solution

Preparation Note

Use a manual defrost freezer and avoid repeated freeze-thaw cycles. While working, please keep sample on ice.

Safety Information

• Storage Class Code: 10 - Combustible liquids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable