| 货号 | 2013/50 |
| 别名 | Pregna-4,17(20)-diene-3,16-dione |
| 供应商 | Tocris |
| 生物活性 | 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). |
| 运输条件 | Blue Ice |
| 存放说明 | Ambient |
| 纯度 | >99 % |
| 计算分子量 | 312.45 |
| 分子式 | C21H28O2 |
| 可溶性/溶解性 | Soluble to 10 mM in ethanol with gentle warming |
| 参考文献 | Burriset al (2005) The hypolipidemic natural product guggulsterone is a promiscuous steroid receptor ligand. Mol.Pharmacol. 67 948. PMID: 15602004. Meyeret 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. 304191. |