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TNF inhibitor TIM1c

Chemical Structure : TNF inhibitor TIM1c

CAS No.: 1171311-99-1

TNF inhibitor TIM1c (TIM1c)

Catalog No.: PC-49446Not For Human Use, Lab Use Only.

TNF inhibitor TIM1c is an orally active small molecule inhibitor of TNF, potently inhibit TNF-induced cell death and cytokine secretion, prevents homotrimerization of TNF by directly binding to the TNF monomer with SPR KD of 1.55 and 0.68 uM for rmTNF and rhTNF, respectively.

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    Biological Activity

    TNF inhibitor TIM1c is an orally active small molecule inhibitor of TNF, potently inhibit TNF-induced cell death and cytokine secretion, prevents homotrimerization of TNF by directly binding to the TNF monomer with SPR KD of 1.55 and 0.68 uM for rmTNF and rhTNF, respectively.
    TNF inhibitor TIM1c stably occupies the TNF homodimer through nonpolar interactions.
    TNF inhibitor TIM1c displays negligible cytotoxicity and great inhibition of TNF-driven induction of IL-8 and IL-6 in human dermal fibroblasts.
    TNF inhibitor TIM1c (20 mg/kg) showed oral bioactivity in a mouse model of collagen-induced polyarthritis (CIA) and suppressed arthritis symptoms, reduces IL-1β and IL-6 immunopositive cells.
    TNF inhibitor TIM1c is a specific and potent disruptor of TNF homotrimerization.

    Physicochemical Properties

    M.Wt 436.534
    Formula C22H24N6O2S
    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

    N-(2,5-dimethyl-3-(2-(propylamino)thiazol-4-yl)-1H-pyrrol-1-yl)-3-methyl-4-oxo-3,4-dihydrophthalazine-1-carboxamide

    References

    1. Javaid N, et al. Sci Signal. 2022 Nov 8;15(759):eabi8713.

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