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TMEM16A blocker 1PBC

Chemical Structure : TMEM16A blocker 1PBC

CAS No.: 362602-12-8

TMEM16A blocker 1PBC (TMEM16A blocker)

Catalog No.: 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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    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 277.206
    Formula C13H6F3N3O
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

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

    References

    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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