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CD12681

Chemical Structure : CD12681

CAS No.: 1952239-59-6

CD12681 (CD-12681;CD 12681)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 471.616
    Formula C25H33N3O4S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    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

    References

    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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