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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-GSK812397
GSK812397

Chemical Structure : GSK812397

CAS No.: 878197-98-9

GSK812397 (GSK 812397;GSK-812397)

货号: PC-35088Not For Human Use, Lab Use Only.

GSK812397 is a potent, selective, noncompetitive, orally available antagonist of CXCR4 receptor, inhibits entry of X4-tropic strains of HIV-1 with IC50 of 4.60 nM and 1.50 nM in PBMCs and HOS assays, respectively.

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

    生物&药学活性

    GSK812397 is a potent, selective, noncompetitive, orally available antagonist of CXCR4 receptor, inhibits entry of X4-tropic strains of HIV-1 with IC50 of 4.60 nM and 1.50 nM in PBMCs and HOS assays, respectively.
    GSK812397 does not block CCR5-mediated viral entry in the R5 viral HOS assay (IC50>25 uM).
    GSK812397 produces a concentration-dependent decrease in both an SDF-1-mediated chemotaxis and intracellular calcium release (IC50=0.34 nM and 2.41 nM, respectively) in cell-based functional assays.
    GSK812397 demonstrates antiviral activity against a broad range of X4-utilizing strains of HIV-1.

    物理化学性质&存储条件

    分子量 420.561
    分子式 C24H32N6O
    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

    (S)-(2-((methyl(5,6,7,8-tetrahydroquinolin-8-yl)amino)methyl)-5-(4-methylpiperazin-1-yl)imidazo[1,2-a]pyridin-3-yl)methanol

    参考文献

    1. Jenkinson S, et al. Antimicrob Agents Chemother. 2010 Feb;54(2):817-24.

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