Molecular structure of Guggulsterone, CAS Number: 95975-55-6
Guggulsterone (CAS 95975-55-6)
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Alternate Names:
Pregna-4,17(20)-diene-3,16-dione
Application:
Guggulsterone is a broad spectrum steroid receptor ligand
CAS Number:
95975-55-6
Molecular Weight:
312.45
Molecular Formula:
C21H28O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
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). Guggulsterone functions primarily as an antagonist of these receptors, with the exception of the progesterone receptor where it displays partial agonist effects. Guggulsterone also exerts hypolipidemic activity, likely via antagonism of the receptor for bile acids (farnesoid X receptor; FXR).
Guggulsterone (CAS 95975-55-6) References
Owsley and Chiang (2003) Guggulsterone antagonizes farnesoid X receptor induction of bile salt export pump but activates pregnane X receptor to inhibit cholesterol 7a-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.Inhibitor of:
ACOT10, ACOT3, Androgen Receptor, Cytokeratin 18, FXRβ, GR, Hepatic Lipase, LIMP I, MCR, Nkx-2.4, OSTβ, Progesterone Receptor, RIP15, RLD-1, SR-B1, SR-BI, TGR5, and V1RF2.Activator of:
DR3, EDEM, LDLR, Mdr-3, NR5A2, SHP, TMC5, ZBTB6, and ZNF484.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Guggulsterone, 10 mg | sc-203990 | 10 mg | $145.00 | |||
Guggulsterone, 50 mg | sc-203990A | 50 mg | $615.00 |