Discontinued Product

Guggulsterone (Cat. No. 2013) has been withdrawn from sale for commercial reasons.
Description: Broad spectrum steroid receptor ligand. Antagonizes FXR and displays hypolipidemic activity
Chemical Name: Pregna-4,17(20)-diene-3,16-dione
Purity: ≥99% (HPLC)

Biological Activity for Guggulsterone

Guggulsterone is a broad 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).

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

Technical Data for Guggulsterone

M. Wt 312.45
Formula C21H28O2
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 95975-55-6
PubChem ID 146898
Smiles [H][C@@]12CC(=O)C(=CC)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CCC2=CC(=O)CC[C@]12C

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.

Product Datasheets for Guggulsterone

References for Guggulsterone

References are publications that support the biological activity of the product.

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, Guggulsterone supplier, Broad, spectrum, steroid, receptors, ligands, Antagonizes, antagonists, FXR, hypolipidaemic, Other, Nuclear, Receptors, 2013, Tocris Bioscience

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