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BMS-986251

Chemical Structure : BMS-986251

CAS No.: 2041841-30-7

BMS-986251 (BMS 986251)

Catalog No.: PC-38350Not For Human Use, Lab Use Only.

BMS-986251 is a potent, selective, orally active RORγt inverse agonist with EC50 of 12 nM in GAL-4 reporter assay in Jurkat cell line, and 24 nM in IL-17 human whole blood assay.

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

    Biological Activity

    BMS-986251 is a potent, selective, orally active RORγt inverse agonist with EC50 of 12 nM in GAL-4 reporter assay in Jurkat cell line, and 24 nM in IL-17 human whole blood assay.
    BMS-986251 displays high selectivity over ROR family members (RORα and RORβ) and other nuclear receptors (PXR, LXRα, and LXRβ) with IC50 >5,000 nM.
    BMS-986251 inhibits IL-17F production in IL-2/IL-23 stimulated mouse pharmacodynamic (PD) model.
    BMS-986251 reduces ear thickness in mouse acanthosis model, 15 mg/kg dose of BMS-986251 is comparable to the human anti-IL-23.

    Physicochemical Properties

    M.Wt 667.611
    Formula C30H29F8NO5S
    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

    (1R,3S,4R)-4-((3aR,9bR)-9b-((4-fluorophenyl)sulfonyl)-7-(perfluoropropan-2-yl)- 2,3,3a,4,5,9b-hexahydro-1H-benzo[e]indole-3-carbonyl)-3-methylcyclohexane-1-carboxylic acid

    References

    1. Cherney RJ, et al. ACS Med Chem Lett. 2020 Mar 31;11(6):1221-1227.

    2. Haggerty HG, et al. Toxicol Sci. 2021 Aug 30;183(1):93-104.

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