Catalog Number: 3888
Chemical Name: N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide
Biological Activity
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
  • M.Wt:
    342.43
  • Formula:
    C16H14N4OS2
  • Solubility:
    Soluble to 100 mM in DMSO and to 25 mM in ethanol
  • Purity:
    >99%
  • Storage:
    Store at +4°C
  • CAS No:
    893990-34-6
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. 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
  2. Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2.
    Delpire et al.
    Proc.Natl.Acad.Sci.USA, 2009;106:5383
  3. 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
Citations:

The citations listed below are publications that use Tocris products. Selected citations for VU 0240551 include:

3 Citations: Showing 1 - 3
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  1. Chloride extrusion enhancers as novel therapeutics for neurological diseases.
    Authors: Gagnon Et al.
    Nat Med 2013;19:1524
  2. GABA is excitatory in adult vasopressinergic neuroendocrine cells.
    Authors: Haam Et al.
    J Neurosci 2012;32:572
  3. 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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