Chemical Structure : Benzopyran-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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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.
M.Wt | 392.499 | |
Formula | C24H28N2O3 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
1. Meng Cui, et al. J Biol Chem. 2021 Jan-Jun:296:100535.
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