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.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|ethanol||3.12||10 with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 312.45. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.1 mM||32.01 mL||160.03 mL||320.05 mL|
|0.5 mM||6.4 mL||32.01 mL||64.01 mL|
|1 mM||3.2 mL||16 mL||32.01 mL|
|5 mM||0.64 mL||3.2 mL||6.4 mL|
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
If you know of a relevant reference for Guggulsterone, please let us know.
View Related Products by Target
Keywords: Guggulsterone, Guggulsterone supplier, Broad, spectrum, steroid, receptors, ligands, Antagonizes, antagonists, FXR, hypolipidaemic, Other, Nuclear, Receptors, 2013, Tocris Bioscience
Citations for Guggulsterone
Citations are publications that use Tocris products.
Currently there are no citations for Guggulsterone. Do you know of a great paper that uses Guggulsterone from Tocris? Please let us know.
Reviews for Guggulsterone
There are currently no reviews for this product. Be the first to review Guggulsterone and earn rewards!
Have you used Guggulsterone?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.