Guggulsterone

Name: Guggulsterone
Brand: Tocris Bioscience
SKU: 2013

Tocris Bioscience, part of Bio-Techne | Catalog # 2013

COA / SDS

Broad spectrum steroid receptor ligand. Antagonizes FXR and displays hypolipidemic activity

Discontinued Product

2013 has been discontinued. View all Additional Nuclear Receptor Compounds products.

Key Product Details

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)
Molecular Weight:	312.45

View Full Technical Details for Guggulsterone

Technical Data
Citations

Biological Activity for Guggulsterone

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 for Guggulsterone

M. Wt	312.45
Formula	C₂₁H₂₈O₂
Storage	Store at RT
Purity	≥99% (HPLC)
CAS Number	95975-55-6
PubChem ID	146898
InChi Key	WDXRGPWQVHZTQJ-NRJJLHBYSA-N
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.

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References for Guggulsterone

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

Meyer Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. J.Med.Chem. 2005 PMID: 16250653
Owsley and Chiang 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.
Burris The hypolipidemic natural product guggulsterone is a promiscuous steroid receptor ligand. Mol.Pharmacol. 2005 PMID: 15602004

Guggulsterone

Tocris Bioscience, part of Bio-Techne | Catalog # 2013

Key Product Details

Biological Activity for Guggulsterone

Technical Data for Guggulsterone

Molarity Calculator

Dilution Calculator

Reconstitution Calculator

References for Guggulsterone

Product Documents for Guggulsterone

COA

Certificate of Analysis

SDS

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