VU 0240551
Chemical Name: N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide
Purity: ≥99%
Biological Activity
VU 0240551 is an inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells). Exhibits selectivity over the Na-K-2Cl cotransporter, NKCCl. Also inhibits hERG and L-type Ca2+ channels.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Effects of VU0240551, a novel KCC2 antagonist, and DIDS on chloride homeostasis of neocortical neurons from rats and humans.
Deisz et al.
Neuroscience, 2014;277:831 -
Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe.
Delpire et al.
Bioorg.Med.Chem.Lett., 2012;22:4532 -
Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2.
Delpire et al.
Proc.Natl.Acad.Sci.USA, 2009;106:5383
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Citations for VU 0240551
The citations listed below are publications that use Tocris products. Selected citations for VU 0240551 include:
5 Citations: Showing 1 - 5
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Diminished KCC2 confounds synapse specificity of LTP during senescence.
Authors: Ferando Et al.
Nat Neurosci 2016;19:1197
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Enhancing K-Cl co-transport restores normal spinothalamic sensory coding in a neuropathic pain model.
Authors: Lavertu Et al.
Brain 2014;137:724
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Chloride extrusion enhancers as novel therapeutics for neurological diseases.
Authors: Gagnon Et al.
Nat Med 2013;19:1524
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GABA is excitatory in adult vasopressinergic neuroendocrine cells.
Authors: Haam Et al.
J Neurosci 2012;32:572
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Efficacy of synaptic inhibition depends on multiple, dynamically interacting mechanisms implicated in chloride homeostasis.
Authors: Doyon Et al.
Purinergic Signal 2011;7:e1002149
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