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RPR260243

Chemical Structure : RPR260243

CAS No.: 668463-35-2

RPR260243 (RPR 260243;RPR-260243)

Catalog No.: PC-60839Not For Human Use, Lab Use Only.

RPR260243 is a potent, selective hERG potassium channel (Kv11.1) activator that dramatically slows current deactivation at 1-30 uM.

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    Biological Activity

    RPR260243 is a potent, selective hERG potassium channel (Kv11.1) activator that dramatically slows current deactivation at 1-30 uM.
    RPR260243-modified HERG currents is inhibited by dofetilide (IC50=58 nM), has little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes, and no activator-like effects on other voltage-dependent ion channels, including the erg3 K+ channel.
    RPR260243 completely reverses the action potential-prolonging effects of dofetilide in guinea pig myocytes.

    Physicochemical Properties

    M.Wt 510.513
    Formula C28H25F3N2O4
    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

    (3R,4R)-4-[3-(6-methoxyquinolin-4-yl)-3-oxo-propyl]-1-[3-(2,3,5-trifluoro-phenyl)-prop-2-ynyl]-piperidine-3-carboxylic acid

    References

    1. Kang J, et al. Mol Pharmacol. 2005 Mar;67(3):827-36.

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