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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-CP-481715
CP-481715

Chemical Structure : CP-481715

CAS No.: 212790-31-3

CP-481715 (CP481715)

货号: PC-61967Not For Human Use, Lab Use Only.

CP-481715 is a potent and selective CCR1 antagonist with Ki of 9.2 nM and IC50 of 74 nM, lacks intrinsic agonist activity.

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

    生物&药学活性

    CP-481715 is a potent and selective CCR1 antagonist with Ki of 9.2 nM and IC50 of 74 nM, lacks intrinsic agonist activity.
    CP-481715 displays >100-fold selectiveity over a panel of GPCRs including related chemokine receptors.
    CP-481715 fully blocks the ability of CCL3 and CCL5 to stimulate receptor signaling (calcium mobilization, IC50=71 nM), monocyte chemotaxis, IC50= 55 nM, and MMP 9 release, IC50= 54 nM).
    CP-481715 inhibits cell infiltration and inflammatory responses in human CCR1 transgenic mice.

    物理化学性质&存储条件

    分子量 482.556
    分子式 C26H31FN4O4
    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

    N-[(2S,3S,5R)-5-carbamoyl-1-(3-fluorophenyl)-3,8-dihydroxy-8-methylnonan-2-yl]quinoxaline-2-carboxamide

    参考文献

    1. Gladue RP, et al. J Biol Chem. 2003 Oct 17;278(42):40473-80.

    2. Gladue RP, et al. J Immunol. 2006 Mar 1;176(5):3141-8.

    3. Gilchrist A, et al. Br J Pharmacol. 2014 Nov;171(22):5127-38.

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