Cat. No. 3888
Chemical Name: N-(4-Methyl-2-thiazolyl)-2-[(6-phen
Biological ActivityInhibitor 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.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
Deisz et al (2014) Effects of VU0240551, a novel KCC2 antagonist, and DIDS on chloride homeostasis of neocortical neurons from rats and humans. Neuroscience 277 831. PMID: 25086309.
Delpire et al (2012) Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe. Bioorg.Med.Chem.Lett. 22 4532. PMID: 22727639.
Delpire et al (2009) Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2. Proc.Natl.Acad.Sci.USA 106 5383. PMID: 19279215.
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Citations are publications that use Tocris products. Selected citations for VU 0240551 include:
Gagnon et al (2013) Chloride extrusion enhancers as novel therapeutics for neurological diseases. Nat Med 19 1524. PMID: 24097188.
Haam et al (2012) GABA is excitatory in adult vasopressinergic neuroendocrine cells. J Neurosci 32 572. PMID: 22238092.
Doyon et al (2011) Efficacy of synaptic inhibition depends on multiple, dynamically interacting mechanisms implicated in chloride homeostasis. Purinergic Signal 7 e1002149. PMID: 21931544.
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