Guggulsterone

Product Description

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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	6.40 mL	32.01 mL	64.01 mL
1 mM	3.20 mL	16.00 mL	32.01 mL
5 mM	0.64 mL	3.20 mL	6.40 mL

Calculators

Background References

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