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GS-5759

Chemical Structure : GS-5759

CAS No.: 1346653-91-5

GS-5759 (GS 5759, GS5759)

Catalog No.: PC-60211Not For Human Use, Lab Use Only.

GS-5759 is a novel bifunctional PDE4 inhibitor (IC50=5 nM) and long acting β2-adrenoceptor agonist (EC50=8 nM).

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    Biological Activity

    GS-5759 is a novel bifunctional PDE4 inhibitor (IC50=5 nM) and long acting β2-adrenoceptor agonist (EC50=8 nM).
    GS-5759 inhibits LPS-induced TNFα production in human PBMC (IC50=0.3 nM) and in human neutrophils fMLP-induced super oxide anion production (IC50=3 nM).
    GS-5759 also is a potent inhibitor of profibrotic and proinflammatory mediator release from human lung fibroblasts.

    Physicochemical Properties

    M.Wt 850.95
    Formula C47H42N6O8S
    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)-6-[(3-{[4-(5-{[2-Hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl]amino}pent-1-yn-1-yl)phenyl]carbamoyl}phenyl)sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methylquinoline-3-carboxamide

    References

    1. Tannheimer SL, et al. J Pharmacol Exp Ther. 2014 Apr;349(1):85-93.

    2. Joshi T, et al. J Pharmacol Exp Ther. 2017 Feb;360(2):324-340.

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