Chemical Name: N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide
Biological ActivityVU 0463271 is a potent and selective inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 61 nM); displays >100-fold selectivity versus the Na-K-2Cl cotransporter 1 (NKCC1) and no activity against a panel of 68 GPCRs, ion channels and transporters.
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Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe.
Delpire et al.
Selective inhibition of KCC2 leads to hyperexcitability and epileptiform discharges in hippocampal slices and in vivo.
Sivakumaran et al.
Citations for VU 0463271
The citations listed below are publications that use Tocris products. Selected citations for VU 0463271 include:
2 Citations: Showing 1 - 2
Cl- out is a novel cooperative optogenetic tool for extruding chloride from neurons
Authors: Alfonsa Et al.
Nature Communications 2016;7:13495
Appearance of fast astrocytic component in voltage-sensitive dye imaging of neural activity.
Authors: Pál Et al.
Mol Syst Biol 2015;8:35
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