Guggulsterone

Biological Activity

Guggulsterone is a broad spectrum steroid receptor ligand; binds with high affinity to mineralocorticoid receptors (K_i = 39 nM) and lower affinity to progesterone, androgen and glucocorticoid receptors (K_i values are 201, 240 and 224 nM respectively). Functions primarily as an antagonist of these receptors, with the exception of the progesterone receptor where it displays partial agonist effects. Also exerts hypolipidemic activity, likely via antagonism of the receptor for bile acids (farnesoid X receptor; FXR).

This compound is a mixture of (Z)- and (E)-Guggulsterone in a ratio of approximately 60:40.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Background References

1. The hypolipidemic natural product guggulsterone is a promiscuous steroid receptor ligand.
   Burris et al.
   Mol.Pharmacol., 2005;67:948
2. Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.
   Meyer et al.
   J.Med.Chem., 2005;48:6948
3. Guggulsterone antagonizes farnesoid X receptor induction of bile salt export pump but activates pregnane X receptor to inhibit cholesterol 7α-hydroxylase gene.
   Owsley and Chiang
   Biochem.Biophys.Res.Comm., 2003;304:191

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