The Liver X receptor-like (LXR) family of NRs (Nuclear, Class 1, Thyroid Hormone Receptor-like) hosts 3 members, including the Farnesoid X receptor (FXR). High expression of LXRα is restricted to spleen, liver, adipose tissue, intestine, kidney and lung whereas LXRβ is expressed in all tissues examined. Upon ligand-induced activation both isoforms form obligate heterodimers with the retinoid X receptor (RXR) and regulate gene expression through binding to LXR response elements (LXREs) in the promoter regions of the target genes.  Identification of oxysterols as endogenous LXR ligands pointed to a role for these receptors in regulating expression of genes involved in cholesterol homeostasis, and lead to the hypothesis that activation of these receptors might have an antiatherosclerotic effect[1]. The FXR, besides a key regulator of cholesterol homeostasis like the LXRs, is also involved in triglyceride synthesis and lipogenesis[2]. Since the recognition that FXR has a significant role in the regulation of bile acids, numerous efforts have been undertaken to search for and design potent and selective FXR agonists.

[1] Biological role for Liver X Receptors. M. Baranowski. J. Physiol. Pharm. 2008, 59, 31-55.
[2] Farnesoid X receptor modulators: a patent review. M.L. Crawley. Exp. Opin. Ther. Pat. 2010, 20, 1047-1057.

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Axon ID Name Description From price
2561 DY 268 Highly potent FXR antagonist with a promising in vitro profile €120.00
3174 Obeticholic acid Potent and selective FXR agonist €60.00
2152 PX 20350 Potent farnesoid X receptor (FXR) agonist €105.00
1749 WAY 362450 Farnesoid X receptor (FXR) agonist €125.00

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