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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Potassium Channel-Benzopyran-G1
Benzopyran-G1

Chemical Structure : Benzopyran-G1

CAS No.: 865476-82-0

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Benzopyran-G1 (Benzopyran G1, BP-G1)

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

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 392.499
    分子式 C24H28N2O3
    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

    (3R,4S)-7-(hydroxymethyl)-2,2,9-trimethyl-4-(2-phenylethylamino)-3,4-dihydropyrano[2,3-g]quinolin-3-ol

    参考文献

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

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