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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-ROR-CD12681
CD12681

Chemical Structure : CD12681

CAS No.: 1952239-59-6

CD12681 (CD-12681;CD 12681)

货号: PC-35306Not For Human Use, Lab Use Only.

CD12681 (CD-12681) is a potent, selective RORγ inverse agonist with IC50 of 19 nM, displays no activity against a panel of nuclear receptors (RORα, RARγ, LXRβ, PPARγ and VDR).

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

    生物&药学活性

    CD12681 (CD-12681) is a potent, selective RORγ inverse agonist with IC50 of 19 nM, displays no activity against a panel of nuclear receptors (RORα, RARγ, LXRβ, PPARγ and VDR).
    CD12681 inhibits IL17 production in stimulated CD4 in human hepatocytes with IC50 of 10 nM.
    CD12681 inhibits ear swelling and IL-17 cell recruitment induced by IL-23 in mice model.
    CD12681 is a selective RORγ inverse agonist is sufficient to modulate an IL-23/IL-17-mediated skin inflammation.

    物理化学性质&存储条件

    分子量 471.616
    分子式 C25H33N3O4S
    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

    N-(2,4-dimethylphenyl)-N-isobutyl-2-oxo-1-[(tetrahydro-2H-pyran-4-yl)methyl]-2,3-dihydro-1H-benzo[d]imidazole-5-sulfonamide

    参考文献

    1. Baffert F, et al. Mol Cancer Ther. 2010 Jul;9(7):1945-55.

    2. Ringel F, et al. Acta Haematol. 2014;132(1):75-86.

    3. Cheon JH, et al. Biochem Biophys Res Commun. 2017 Sep 2;490(4):1176-1182.

    4. Haissaguerre M, et al. Front Pharmacol. 2018 May 15;9:527.

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