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Chemical Structure : 3hi2one-G4
Catalog No.: PC-38639Not For Human Use, Lab Use Only.
3hi2one-G4 is a highly selective small molecule activator targeting GIRK4 homomeric channels, does not activate GIRK2, GIRK1/2 or GIRK1/4 channels.
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3hi2one-G4 is a highly selective small molecule activator targeting GIRK4 homomeric channels, does not activate GIRK2, GIRK1/2 or GIRK1/4 channels.
3hi2one-G4 activated GIRK4 whole-cell currents in a dose-dependent manner, with an EC50 of 12.74 μM in TEVC experiments in Xenopus oocytes, and 5.15 μM in whole-cell patch-clamp experiments in HEK293 cells, respectively.
3hi2one-G4 binds the TM1, TM2, and slide helix (S-HLX) regions of the GIRK4 channel, and enhances GIRK4 channel interactions with PIP2.
3hi2one-G4 activates the GIRK4 channel in a G protein-independent manner, activates aldosteronism disease related GIRK4 channel mutants (G247R).
| M.Wt | 467.521 | |
| Formula | C29H25NO5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Meng Cui, et al. J Biol Chem. 2022 May 4;102009. doi: 10.1016/j.jbc.2022.102009.
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