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VTP-43742

Chemical Structure : VTP-43742

CAS No.: 1802706-04-2

VTP-43742 (Vimirogant;VTP43742)

Catalog No.: PC-60452Not For Human Use, Lab Use Only.

VTP-43742 (Vimirogant, VTP43742) is a highly potent, selective, oral RORγt inverse agonist with Ki/IC50 of 3.5/17 nM respectively.

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    Biological Activity

    VTP-43742 (Vimirogant, VTP43742) is a highly potent, selective, oral RORγt inverse agonist with Ki/IC50 of 3.5/17 nM respectively.
    VTP-43742 exhibits >1,000-fold selectivity versus the RORα and RORβ.
    VTP-43742 inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation.
    VTP-43742 inhibits the secretion of IL-17A from activated hPBMCs (IC50=18 nM) and human whole blood (IC50=192 nM).
    VTP-43742 shows potential for the treatment of autoimmune disorders, including multiple sclerosis and psoriasis.

    Physicochemical Properties

    M.Wt 552.657
    Formula C27H35F3N4O3S
    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)-N-((5-(ethylsulfonyl)pyridin-2-yl)methyl)-7-isopropyl-6-(((1r,4S)-4-(trifluoromethyl)cyclohexyl)methyl)-6,7-dihydro-5H-pyrrolo[3,4-b]pyridine-3-carboxamide

    References

    1. Pandya VB, et al. J Med Chem. 2018 Jul 16. doi: 10.1021/acs.jmedchem.8b00588.

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