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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Potassium Channel-MK-0448
MK-0448

Chemical Structure : MK-0448

CAS No.: 875562-81-5

MK-0448 (MK0448)

货号: PC-62816Not For Human Use, Lab Use Only.

MK-0448 is a potent, specific I(Kur) current/Kv1.5 channel inhibitor with IC50 of 8.6 nM, potently inhibits IKur in human atrial myocytes with IC50 of 10.8 nM.

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

    生物&药学活性

    MK-0448 is a potent, specific I(Kur) current/Kv1.5 channel inhibitor with IC50 of 8.6 nM, potently inhibits IKur in human atrial myocytes with IC50 of 10.8 nM.
    MK-0448 also demonstrates a potent effect on currents associated with other Kv1.x and Kv2.x subunits, such as Kv1.7 and Kv2.1, with IC50 of 72 and 61 nM, respectively.
    MK-0448 displays >70-fold concentration than inhibition of IKur.
    MK-0448 significantly causes prolongation of the atrial refractory period in normal anesthetized dogs.

    物理化学性质&存储条件

    分子量 448.516
    分子式 C24H21FN4O2S
    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-{6-[(1S)-1-(4-fluorophenyl)-2,2-di(pyridin-3-yl)ethyl]pyridin-2-yl}methanesulfon- amide

    参考文献

    1. Pavri BB, et al. Circ Arrhythm Electrophysiol. 2012 Dec;5(6):1193-201.

    2. Loose S, et al. Front Pharmacol. 2014 Mar 4;5:26.

    3. Wolkenberg SE, et al. Bioorg Med Chem Lett. 2017 Feb 15;27(4):1062-1069.

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