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T0901317是一种双效肝X受体/法尼醇X受体激动剂。

T0901317 is a dual LXR/FXR agonist.

作者信息

Houck Keith A, Borchert Kristen M, Hepler Christopher D, Thomas Jeffrey S, Bramlett Kelli S, Michael Laura F, Burris Thomas P

机构信息

RTP Laboratories, Eli Lilly & Company, Research Triangle Park, NC 27709, USA.

出版信息

Mol Genet Metab. 2004 Sep-Oct;83(1-2):184-7. doi: 10.1016/j.ymgme.2004.07.007.

Abstract

We characterize the ability of the liver X receptor (LXRalpha [NR1H3] and LXRbeta [NR1H2]) agonist, T0901317, to activate the farnesoid X receptor (FXR [NR4H4]). Although T0901317 is a much more potent activator of LXR than FXR, this ligand actually activates FXR more potently than a natural bile acid FXR ligand, chenodeoxycholic acid. Thus, the FXR activity of T0901317 must be considered when utilizing this agonist as a pharmacological tool to investigate LXR function.

摘要

我们对肝脏X受体(LXRα [NR1H3] 和LXRβ [NR1H2])激动剂T0901317激活法尼醇X受体(FXR [NR4H4])的能力进行了表征。尽管T0901317作为LXR的激活剂比作为FXR的激活剂效力要强得多,但该配体实际上激活FXR的效力比天然胆汁酸FXR配体鹅去氧胆酸更强。因此,在将该激动剂用作研究LXR功能的药理学工具时,必须考虑T0901317的FXR活性。

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