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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-BMS-687681
BMS-687681

Chemical Structure : BMS-687681

CAS No.: 847998-92-9

BMS-687681 (BMS687681, BMS-681)

货号: PC-60322Not For Human Use, Lab Use Only.

BMS-687681 (BMS-681) is a potent and orally bioavailable dual antagonist of CCR2 and CCR5 with binding IC50 of 0.7 nM and 2.4 nM, respectively.

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

    生物&药学活性

    BMS-687681 (BMS-681) is a potent and orally bioavailable dual antagonist of CCR2 and CCR5 with binding IC50 of 0.7 nM and 2.4 nM, respectively.
    BMS-681 exhibits high selectivity against other chemokine receptors and GPCRs.
    BMS-681 shows CCR2 functional assays of monocyte chemotaxis (IC50=0.24 nM) and CD11b upregulation (whole blood IC50=4.7 nM), CCR5 functional assays of human T-cells (IC50=2.3 nM) and whole blood CCR5-mediated CD11b upregulation (IC50=4.3 nM),
    BMS-681 is suitable for use in both murine and monkey models of inflammation.

    物理化学性质&存储条件

    分子量 491.603
    分子式 C26H36F3N5O
    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

    1-((1S,2R,4R)-4-(isopropyl(methyl)amino)-2-propylcyclohexyl)-3-((6-(trifluoromethyl)quinazolin-4-yl)amino)pyrrolidin-2-one

    参考文献

    1. Zheng Y, et al. Nature. 2016 Dec 15;540(7633):458-461.

    2. Carter PH, et al. ACS Med Chem Lett. 2015 Mar 4;6(4):439-44.

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