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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Farnesoid X Receptor (FXR)-ID166
ID166

Chemical Structure : ID166

CAS No.: 2247972-61-6

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ID166 (Lecufexor, ID119031166)

货号: PC-21879Not For Human Use, Lab Use Only.

Lecufexor (D119031166, ID166) is a novel potent, selective farnesoid X receptor (FXR) agonist with EC50 of 3 nM and 5 nM in TR-FRET FXR co-activator assay and FXR reporter assay, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    Lecufexor (D119031166, ID166) is a novel potent, selective farnesoid X receptor (FXR) agonist with EC50 of 3 nM and 5 nM in TR-FRET FXR co-activator assay and FXR reporter assay, respectively.
    ID166 induces SHP gene expression more strongly than obeticholic acid (OCA) (EC50 of 1 μM) with an EC50 value of 19 nM in human hepatocytes.
    ID166 is highly selective for FXR against a luciferase reporter assay on 19 human nuclear receptors up to 3 μM, also does not exhibit agonistic activities on either MRGPRX4 or TGR5 up to 100 μM.
    ID166 strongly increases the gene expression levels of the FXR target genes up to 14-fold in hamster liver and intestine in a dose-dependent manner, and plasma fibroblast growth factor 15 (FGF15) level is significantly increased by ID166 at a dose of 20 mg/kg/day.
    ID166 (30 mg/kg) ameliorates the NASH phenotype induced by the fed free choice diet.
    ID166 reduces total NAFLD activity and hepatic fibrosis score in NASH hamsters fed a free choice diet, modulates the relative abundance of gut microbes in NASH hamsters.

    物理化学性质&存储条件

    分子量 619.88
    分子式 C32H21Cl3N2O5
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    (5-((2-Chloro-4-((5-cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl)methoxy)phenyl)ethynyl)-2-cyclopropylbenzo[d]oxazole-7-carboxylic acid)

    参考文献

    1. Moon AN, et al. Biomed Pharmacother. 2024 Feb 29;173:116331.

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