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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-ROR-TAK-828F
TAK-828F

Chemical Structure : TAK-828F

CAS No.: 1854901-94-2

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TAK-828F (TAK828F;TAK-828)

货号: PC-63177Not For Human Use, Lab Use Only.

TAK-828F (TAK-828) is a potent, selective, orally available RORγt inverse agonist with binding IC50 of 1.9 nM and reporter IC50 of 6.0 nM, displays excellent selectivity (>5,000-fold) against other ROR isoforms and nuclear receptors.

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

    生物&药学活性

    TAK-828F (TAK-828) is a potent, selective, orally available RORγt inverse agonist with binding IC50 of 1.9 nM and reporter IC50 of 6.0 nM, displays excellent selectivity (>5,000-fold) against other ROR isoforms and nuclear receptors.
    TAK-828F shows robust and dose-dependent inhibition of IL-17A expression after oral administration at 0.3, 1 and 3 mg/kg bid in the mouse IL-23-induced cytokine expression model.
    TAK-828F also demonstrates dose-dependent inhibition of RORγt regulated gene expression such as IL-17F, IL-22, and IL23 receptor, but no effect against IFN-γ expression.
    TAK-828F significantly reduces the development of clinical symptoms in mouse experimental autoimmune encephalomyelitis model.

    物理化学性质&存储条件

    分子量 509.578
    分子式 C28H32FN3O5
    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

    2-((1S,3s)-3-((R)-5-((7-fluoro-1,1-dimethyl-2,3-dihydro-1H-inden-5-yl)carbamoyl)-2-methoxy-5,6,7,8-tetrahydro-1,6-naphthyridine-6-carbonyl)cyclobutyl)acetic acid

    参考文献

    1. Kono M, et al. J Med Chem. 2018 Mar 14. doi: 10.1021/acs.jmedchem.8b00061.

    2. Shibata A, et al. Biochem Pharmacol. 2018 Jan 30;150:35-45.

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