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JTP-96193

Chemical Structure : JTP-96193

CAS No.: 1016257-48-9

JTP-96193 (JTP96193)

Catalog No.: PC-20476Not For Human Use, Lab Use Only.

JTP-96193 (JTP96193) is a potent, selective TNF-α converting enzyme (TACE/ADAM17) inhibitor with IC50 of 5.4 nM, >1800-fold selectivity against ADAM10.

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

    Biological Activity

    JTP-96193 (JTP96193) is a potent, selective TNF-α converting enzyme (TACE/ADAM17) inhibitor with IC50 of 5.4 nM, >1800-fold selectivity against ADAM10.
    JTP-96193 also displays >500-fold selectivity against other MMP family members such as MMP-1, -2, -3, -7, -8, -9, -10, -12, -13, -15, -16, -17, and -24.
    JTP-96193 (10 uM) completely inhibited LPS-induced TNF-α production in rat whole, with IC50 of 0.17 uM.
    JTP-96193 significantly inhibited TNF-α production in Lewis rats induced by LPS injection with ED50 3.8 mg/kg.
    JTP-96193 dose-dependently reduced the TNF-α release from fat tissue in DIO mice, prevented delay of sciatic MNCV without any effects on blood glucose or insulin levels in STZ-induced diabetic mice.

    Physicochemical Properties

    M.Wt 525.60
    Formula C26H28FN5O4S
    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

    4-((7,8-dimethyl-1,2,3,4-tetrahydroquinolin-5-yl)methoxy)-2-fluoro-N-((3S,4S)-1-formyl-4-(5-oxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)pyrrolidin-3-yl)benzamide

    References

    1. Maekawa M, et al. Biol Pharm Bull. 2019;42(11):1906-1912.

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