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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
|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.
Solubility Data for Guggulsterone
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|ethanol||3.12||10 with gentle warming|
Preparing Stock Solutions for Guggulsterone
The following data is based on the product molecular weight 312.45. Batch specific molecular weights may vary from batch to batch due to the degree 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 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
If you know of a relevant reference for Guggulsterone, please let us know.
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Keywords: Guggulsterone, Guggulsterone supplier, Broad, spectrum, steroid, receptors, ligands, Antagonizes, antagonists, FXR, hypolipidaemic, Other, Nuclear, Receptors, 2013, Tocris Bioscience
Citations for Guggulsterone
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