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RORγt inverse agonist 22

Chemical Structure : RORγt inverse agonist 22

CAS No.: 1644029-01-5

RORγt inverse agonist 22

Catalog No.: PC-35413Not For Human Use, Lab Use Only.

RORγt inverse agonist 22 is a potent, subtype selective RORγt inverse agonist with binding IC50 of 18 nM, displays >192-fold selectivity over RORα and RORβ.

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

    Biological Activity

    RORγt inverse agonist 22 is a potent, subtype selective RORγt inverse agonist with binding IC50 of 18 nM, displays >192-fold selectivity over RORα and RORβ.
    RORγt inverse agonist 22 exhibits cellular potency in RORγt reporter gene assays with IC50 of 13 nM, also shows >250-fold selectivity over a panel of 20 nuclear receptors。
    RORγt inverse agonist 22 demonstrates in vivo potency to suppress the transcriptional activity of RORγt in a mouse PD model upon oral administration.

    Physicochemical Properties

    M.Wt 489.551
    Formula C23H25F2N3O5Si
    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

    (R)-N-(2-((3,5-Difluoro-4-(trimethylsilyl)phenyl) amino)-1-(4-methoxyphenyl)-2-oxoethyl)-3-hydroxy-N-methylisoxazole-5-carboxamide

    References

    1. Shirai J, et al. Bioorg Med Chem. 2018 Jan 15;26(2):483-500.

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