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TMEM16A blocker 1PBC

Chemical Structure : TMEM16A blocker 1PBC

CAS No.: 362602-12-8

TMEM16A blocker 1PBC (TMEM16A blocker)

货号: PC-49192Not For Human Use, Lab Use Only.

1PBC is a small molecule blocker of calcium-activated chloride channel TMEM16A, blocks TMEM16A completely with an IC50 of 4 uM at zero mV and saturating Ca2+ concentration (2 uM).

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

    生物&药学活性

    1PBC is a small molecule blocker of calcium-activated chloride channel TMEM16A, blocks TMEM16A completely with an IC50 of 4 uM at zero mV and saturating Ca2+ concentration (2 uM).
    1PBC inhibits WT TMEM16A with micromolar range potentcy (IC50=13.1 uM), mutants R617A and R784A confers greater potency to 1PBC compared with the WT (IC50, 2.2 and 5.8 uM).
    1PBC binds with an apparent valence of ~0.27 and a Kd of ~3.6 µM at zero mV.

    物理化学性质&存储条件

    分子量 277.206
    分子式 C13H6F3N3O
    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

    1-Hydroxy-3-(trifluoromethyl)pyrido[1,2-a]benzimidazole-4-carbonitrile

    参考文献

    1. Christian J Peters, et al. Proc Natl Acad Sci U S A. 2015 Mar 17;112(11):3547-52.

    2. Andy K M Lam, et al. Nat Commun. 2022 May 19;13(1):2798.

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