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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Chloride Channel-CLC-2-IN-AK42
CLC-2-IN-AK42

Chemical Structure : CLC-2-IN-AK42

CAS No.: 2408824-56-4

CLC-2-IN-AK42 (CLC-2 inhibitor AK42, AK42)

货号: PC-72552Not For Human Use, Lab Use Only.

CLC-2-IN-AK42 (CLC-2 inhibitor AK42, AK42) is a potent, specific small-molecule inhibitor of voltage-gated chloride channel CLC-2 with IC50 of 17 nM (human CLC-2).

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

    生物&药学活性

    CLC-2-IN-AK42 (CLC-2 inhibitor AK42, AK42) is a potent, specific small-molecule inhibitor of voltage-gated chloride channel CLC-2 with IC50 of 17 nM (human CLC-2).
    AK42 displays unprecedented selectivity (>1,000-fold) over CLC-1, the closest CLC-2 homolog, and no off-target engagement a diverse panel of 61 CNS receptors, channels, and transporters expressed in brain tissue.
    AK-42 binds to an extracellular vestibule above the channel pore.
    AK-42 is almost three orders-of-magnitude more potent than MCFA, demonstrates high potency (IC50=14 nM for rat CLC-2) in manual patch-clamp experiments on CHO cells transiently transfected with rat CLC-2.
    AK-42 inhibits hyperpolarization-activated current in hippocampal cells, attenuates steady-state currents and eliminated relaxation currents in recorded neurons.
    AK-42 is a powerful tool for investigating CLC-2 neurophysiology.

    物理化学性质&存储条件

    分子量 389.232
    分子式 C19H14Cl2N2O3
    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

    2-((3-(benzyloxy)-2,6-dichlorophenyl)amino)nicotinic acid

    参考文献

    1. Anna K Koster, et al. Proc Natl Acad Sci U S A. 2020 Dec 22;117(51):32711-32721.

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