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Benzopyran-G1

Chemical Structure : Benzopyran-G1

CAS No.: 865476-82-0

Benzopyran-G1 (Benzopyran G1, BP-G1)

Catalog No.: PC-73230Not For Human Use, Lab Use Only.

Benzopyran-G1 (Benzopyran G1, BP-G1) is a potent and selective small-molecule inhibitor targeting Kir3.1-containing channels, inhibits heteromeric Kir3.1/4 or Kir3.1/2 channels with IC50 of 10-30 nM.

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    Biological Activity

    Benzopyran-G1 (Benzopyran G1, BP-G1) is a potent and selective small-molecule inhibitor targeting Kir3.1-containing channels, inhibits heteromeric Kir3.1/4 or Kir3.1/2 channels with IC50 of 10-30 nM.
    Benzopyran-G1 (BP-G1) displays high selectivity over other cardiac channels, including homomeric Kir3 and Kir2 channels.
    Benzopyran-G1 (BP-G1) inhibits cardiac acetylcholine-activated inwardly rectifying K+ current (IKACh), composed of Kir3.1/Kir3.4 heterotetrameric and Kir3.4 homotetrameric channel subunits, selectively inhibits the Kir3.1 (GIRK1 or G1) subunit of the KACh channel.
    Benzopyran-G1 (BP-G1) inhibits the IKACh channel by blocking the central cavity pore.
    Benzopyran-G1 (BP-G1) interacts with Kir3.1 residues E141 and D173 through hydrogen bonds that proved critical for its inhibitory activity.
    Benzopyran-G1 (BP-G1) effectively blocked the IKACh channel response to carbachol in an in vivo rodent model and displayed good selectivity and pharmacokinetic properties.

    Physicochemical Properties

    M.Wt 392.499
    Formula C24H28N2O3
    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,4S)-7-(hydroxymethyl)-2,2,9-trimethyl-4-(2-phenylethylamino)-3,4-dihydropyrano[2,3-g]quinolin-3-ol

    References

    1. Meng Cui, et al. J Biol Chem. 2021 Jan-Jun:296:100535. 

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