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Guggulsterone

Cat. No. 2013 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

Discontinued Product

2013 has been discontinued.

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说明： Broad spectrum steroid receptor ligand. Antagonizes FXR and displays hypolipidemic activity
化学名： Pregna-4,17(20)-diene-3,16-dione
纯度： ≥99% (HPLC)
说明书
引用文献
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生物活性 技术数据 说明书 参考文献

生物活性 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.

技术数据 for Guggulsterone

分子量 312.45
公式 C21H28O2
储存 Store at RT
纯度 ≥99% (HPLC)
CAS Number 95975-55-6
PubChem ID 146898
InChI Key WDXRGPWQVHZTQJ-NRJJLHBYSA-N
Smiles [H][C@@]12CC(=O)C(=CC)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CCC2=CC(=O)CC[C@]12C

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

参考文献 for Guggulsterone

参考文献是支持产品生物活性的出版物。

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

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关键词: Guggulsterone, Guggulsterone supplier, Broad, spectrum, steroid, receptors, ligands, Antagonizes, antagonists, FXR, hypolipidaemic, Other, Nuclear, Receptors, 2013, Tocris Bioscience

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