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Category:
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Nuclear Receptors Other Nuclear Receptors
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Cat.No.
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Product Name
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2013 |
Guggulsterone
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Price and Availability
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Guggulsterone
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Chemical Name:
Pregna-4,17(20)-diene-3,16-dione |
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Biological Activity:
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 hypolipidaemic activity, likely via antagonism of the
receptor for bile acids (farnesoid X receptor; FXR).
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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References:
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. Burris et al (2005) The hypolipidemic natural product
guggulsterone is a promiscuous steroid receptor ligand. Mol.Pharmacol. 67
948. 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.
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Keywords: Guggulsterone, Other Nuclear Receptors, Broad Spectrum Steroid Receptor Ligand. Antagonises FXR & Displays Hypolipidaemic Activity, Tocris Bioscience
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