TUG-2015(TUG-2015) - 药物靶点：FFAR3_在研适应症：炎症，代谢性疾病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

FFAR3

作用机制

FFAR3调节剂(free fatty acid receptor 3 modulators)

治疗领域

内分泌与代谢疾病其他疾病

在研适应症

炎症代谢性疾病

非在研适应症-

原研机构

IT-Universitetet I København

在研机构

University of Glasgow

University of Southern Denmark

IT-Universitetet I København

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 TUG-2015 相关的临床结果

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100 项与 TUG-2015 相关的转化医学

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100 项与 TUG-2015 相关的专利（医药）

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1

项与 TUG-2015 相关的文献（医药）

2020-04-09·Journal of Medicinal Chemistry1区 · 医学

Structure–Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators

1区 · 医学

Article

作者: Quon, Tezz ; Hudson, Brian D. ; Bielefeldt, Line Ø. ; Milligan, Graeme ; Barki, Natasja ; Dutta, Palash ; McKenzie, Christine J. ; Hansen, Anders Højgaard ; Ulven, Elisabeth Rexen ; Sergeev, Eugenia ; Ulven, Trond ; Brvar, Matjaz ; Tobin, Andrew B.

Free fatty acid receptor 3 (FFA3, previously GPR41) is activated by short-chain fatty acids, mediates health effects of the gut microbiota, and is a therapeutic target for metabolic and inflammatory diseases. The shortage of well-characterized tool compounds has however impeded progress. Herein, we report structure-activity relationship of an allosteric modulator series and characterization of physicochemical and pharmacokinetic properties of selected compounds, including previous and new tools. Two representatives, 57 (TUG-1907) and 63 (TUG-2015), showed improved solubility and preserved potency. Of these, 57, with EC₅₀ = 145 nM and a solubility of 33 μM, showed high clearance in vivo but is a preferred tool in vitro. In contrast, 63, with EC₅₀ = 162 nM and a solubility of 9 μM, showed lower clearance and seems better suited for in vivo studies. Using 57, we demonstrate for the first time that FFA3 activation leads to calcium mobilization in murine dorsal root ganglia.

100 项与 TUG-2015 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
代谢性疾病	临床前	英国	University of Glasgow	2020-03-06
代谢性疾病	临床前	丹麦	University of Southern Denmark	2020-03-06
炎症	临床前	丹麦	IT-Universitetet I København	-