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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-BMS-457
BMS-457

Chemical Structure : BMS-457

CAS No.: 946594-19-0

BMS-457 (BMS457)

货号: PC-63566Not For Human Use, Lab Use Only.

BMS-457 is a potent and selective CCR1 antagonist with binding IC50 of 0.8 nM, >1,000-fold selectivity against other CC family receptors.

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

    生物&药学活性

    BMS-457 is a potent and selective CCR1 antagonist with binding IC50 of 0.8 nM, >1,000-fold selectivity against other CC family receptors.
    BMS-457 displays single-digit nanomolar inhibition of chemotaxis induced by a number of CCR1 ligands, including MIP-1α( IC50=2.1 nM), Leukotactin-1 (IC50=4.4 nM), RANTES (IC50=1.0 nM), MPIF-1 (IC50=2.7 nM), and HCC-1 (IC50=4.0 nM).
    BMS-457 blocks the ligand-stimulated upregulation of the β2-integrin CD11b in whole blood, with IC50 of 46 nM (MIP-1α) and 54 nM (LKN-1).

    物理化学性质&存储条件

    分子量 451.004
    分子式 C24H35ClN2O4
    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

    (1R,3R)-N-[(1R)-1-[[(4S)-4-(4-Chlorophenyl)-4-hydroxy-3,3-dimethyl-1-piperidinyl]carbonyl]-2-methylpropyl]-3-hydroxy-cyclopentanecarboxamide

    参考文献

    1. Gardner DS, et al. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3833-40.

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