Cat. No. 2013
Chemical Name: Pregna-4,17(20)-diene-3,16-dione
Biological ActivityBroad spectrum steroid receptor ligand; binds with high affinity to mineralocorticoid receptors (Ki = 39 nM) and lower affinity to progesterone, androgen and glucocorticoid receptors (Ki 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).
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Burris et al (2005) The hypolipidemic natural product guggulsterone is a promiscuous steroid receptor ligand. Mol.Pharmacol. 67 948. PMID: 15602004.
Meyer et al (2005) Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. J.Med.Chem. 48 6948. PMID: 16250653.
Owsley and Chiang (2003) Guggulsterone antagonizes farnesoid X receptor induction of bile salt export pump but activates pregnane X receptor to inhibit cholesterol 7α-hydroxylase gene. Biochem.Biophys.Res.Comm. 304 191.
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Keywords: Guggulsterone, supplier, Broad, spectrum, steroid, receptors, ligands, Antagonizes, antagonists, FXR, hypolipidaemic, Tocris Bioscience, Other Nuclear Receptor products
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