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GNE-3500

Chemical Structure : GNE-3500

CAS No.: 1537859-24-7

GNE-3500 (GNE3500;GNE 3500)

Catalog No.: PC-60453Not For Human Use, Lab Use Only.

GNE-3500 (GNE3500) is a potent, selective, and orally bioavailable RORγ inhibitor with IC50 of 47 nM in IL-17 promoter assays.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    GNE-3500 (GNE3500) is a potent, selective, and orally bioavailable RORγ inhibitor with IC50 of 47 nM in IL-17 promoter assays.
    GNE-3500 displays 75-fold selectivity over other ROR family members and >200-fold selectivity over 25 additional nuclear receptors.
    GNE-3500 inhibits the production of all three IL-17 subtypes in murine CD4+ T cells with EC50 of 0.27-1.8 uM, also inhibits the production of IL-17AA and -AF by ILCs.
    GNE-3500 shows in vitro ADME properties, in vivo PK, and dose-dependent inhibition of IL-17 in vivo.

    Physicochemical Properties

    M.Wt 459.58
    Formula C24H30FN3O3S
    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

    1-[4-[3-Fluoro-4-[[(3S,6R)-tetrahydro-3-methyl-1,1-dioxido-6-phenyl-2H-1,2-thiazin-2-yl]methyl]phenyl]-1-piperazinyl]ethanone

    References

    1. Fauber BP, et al. J Med Chem. 2015 Jul 9;58(13):5308-22.

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