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CP-628006

Chemical Structure : CP-628006

CAS No.: 305822-08-6

CP-628006 (CP628006)

Catalog No.: PC-72256Not For Human Use, Lab Use Only.

CP-628006 (CP628006) is a small molecule CFTR potentiator, potentiates low temperature-rescued F508del-CFTR with EC50 of 0.4 uM.

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    Biological Activity

    CP-628006 (CP628006) is a small molecule CFTR potentiator, potentiates low temperature-rescued F508del-CFTR with EC50 of 0.4 uM.
    CP-628006 potentiated wild-type (EC50=24 nM), F508del-CFTR (EC500=400 nM), and G551D-CFTR (EC50=380 nM) by increasing the frequency and duration of channel openings in excised inside-out membrane patches assays.
    CP-628006 efficaciously potentiated CFTR function in epithelia from cultured hBE cells. Its effects on the predominant CFTR variant F508del-CFTR were larger than those with the gating variant G551D-CFTR.
    Combinations of CP-628006 and ivacaftor enhances the potentiation of G551D-CFTR, but not F508del-CFTR.
    CP-628006 restores ATP-dependent channel gating to G551D-CFTR.
    CP-628006 efficaciously potentiated the CFTR-mediated Cl− currents of plasma membrane-rescued F508del- and G551D-CFTR.

    Physicochemical Properties

    M.Wt 536.639
    Formula C32H35F3N2O2
    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

    (4bS,7S,8aR)-4b-benzyl-7-hydroxy-N-((2-methylpyridin-3-yl)methyl)-7-(3,3,3-trifluoropropyl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-2-carboxamide

    References

    1. Jia Liu, et al. Br J Pharmacol. 2021 Oct 13.

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