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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-SX-517
SX-517

Chemical Structure : SX-517

CAS No.: 1240494-13-6

SX-517 (Phenylboronic Acid;SX 517;SX517)

货号: PC-60620Not For Human Use, Lab Use Only.

SX-517 is a potent, specific, noncompetitive dual CXCR1 and CXCR2 antagonist with IC50 of 38 nM (vs. CXCL1) and 36 nM (vs. CXCL8), respectively.

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

    生物&药学活性

    SX-517 is a potent, specific, noncompetitive dual CXCR1 and CXCR2 antagonist with IC50 of 38 nM (vs. CXCL1) and 36 nM (vs. CXCL8), respectively.
    SX-517 inhibits CXCL1-induced Ca(2+) flux in human PMNs but has no effect on the Ca(2+) flux induced by C5a, fMLF, or PAF; antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation in recombinant HEK293 cells expressed CXCR2.
    SX-517significantly inhibits inflammation in an in vivo murine model (0.2 mg/kg iv).

    物理化学性质&存储条件

    分子量 382.216
    分子式 C19H16BFN2O3S
    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

    2-[5-(4-Fluorophenylcarbamoyl)pyridin-2-ylsulfanylmethyl]phenylboronic Acid

    参考文献

    1. Maeda DY, et al. J Med Chem. 2014 Oct 23;57(20):8378-97.

    2. Schuler AD, et al. Bioorg Med Chem Lett. 2015 Sep 15;25(18):3793-7.

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