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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-BL5923
BL5923

Chemical Structure : BL5923

CAS No.: 868408-20-2

BL5923 (BL 5923;BL-5923)

货号: PC-35358Not For Human Use, Lab Use Only.

BL5923 (BL-5923) is a potent, highly specific, orally available inhibitor of CCR1 with IC50 of 20.4 and 22.8 nM for human and mouse CCR1, resepctively.

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

    生物&药学活性

    BL5923 (BL-5923) is a potent, highly specific, orally available inhibitor of CCR1 with IC50 of 20.4 and 22.8 nM for human and mouse CCR1, resepctively.
    BL5923 displays excellent selectivity against a panel of additional chemokine receptors including human CCR2, CCR4, CCR5, CCR6, CCR7, CXCR1, CXCR2, and CXCR3.
    BL5923 suppresses colon cancer liver metastasis by blocking accumulation of immature myeloid cells in a mouse mode.
    BL5923 ameliorates the progression of lupus nephritis in NZB/W mice; also improves survival, decreases the kidney fungal burden and protects from renal tissue injury in Candida-infected mice.

    物理化学性质&存储条件

    分子量 487.956
    分子式 C25H27ClFN3O4
    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

    (E)-N-(5-chloro-2-(3-(9-(4-fluorobenzyl)-3-oxa-7,9-diazabicyclo[3.3.1]nonan-7-yl)-3-oxoprop-1-en-1-yl)-4-methoxyphenyl)acetamide

    参考文献

    1. Kitamura T, et al. Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13063-8.

    2. Revesz L, et al. Bridged piperazines and piperidines as CCR1 antagonists with oral activity in models of arthritis and multiple sclerosis. Lett Drug Des Discov. 2006;3:689–694.

    3. Bignon A, et al. J Immunol. 2014 Feb 1;192(3):886-96.

    4. Lionakis MS, et al. Antimicrob Agents Chemother. 2017 Feb 23;61(3). pii: e02365-16.

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