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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-GS-5759
GS-5759

Chemical Structure : GS-5759

CAS No.: 1346653-91-5

GS-5759 (GS 5759, GS5759)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 850.95
    分子式 C47H42N6O8S
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    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

    参考文献

    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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