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JTE-151

Chemical Structure : JTE-151

CAS No.: 1404380-58-0

JTE-151 (JTE151)

Catalog No.: PC-20043Not For Human Use, Lab Use Only.

JTE-151 (JTE151) is a potent, selective RORγ antagonist with EC50 of 13 nM in RORγ luciferase assays.

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

    Biological Activity

    JTE-151 (JTE151) is a potent, selective RORγ antagonist with EC50 of 13 nM in RORγ luciferase assays.
    JTE-151 demonstrated >100-fold selectivity toward RORγ against 12 nuclear receptors (mGR, hAR, hERα, hPR, hVDR, hFXR, mLXRα, hPPARα, hPPARδ, hPPARγ, hRARα, hRXRα)。
    JTE-151 at 3 and 10 mg/kg suppressed IL-17 levels in both lymph node and plasma in mice with the myelin oligodendrocyte glycoprotein (MOG35–55)-induced EAE。
    JTE-151 suppressed the Th17 cell differentiation in mouse EAE model.

    Physicochemical Properties

    M.Wt 501.06
    Formula C28H37ClN2O4
    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

    (S)-6-((2-Chloro-4-methylphenyl)amino)-4-(4-cyclopropyl-5-(cis-3-neopentylcyclobutyl)isoxazol-3-yl)-6-oxohexanoic acid

    References

    1. Masayuki Kotoku, et al. J Med Chem. 2019 Mar 14;62(5):2837-2842.

    2. Nadim S Shaikh, et al. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2208-2217.

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