VU 0463271

Cat. No. 4719

VU 0463271  [1391737-01-1]

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Chemical Name: N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide

Biological Activity

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.

Technical Data

Soluble to 50 mM in DMSO and to 10 mM in ethanol with gentle warming
>98 %
Store at +4°C

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 / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

Sivakumaran et al (2015) Selective inhibition of KCC2 leads to hyperexcitability and epileptiform discharges in hippocampal slices and in vivo. J.Neurosci. 35 8291. PMID: 26019342.

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.

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Citations are publications that use Tocris products. Selected citations for VU 0463271 include:

Pál et al (2015) Appearance of fast astrocytic component in voltage-sensitive dye imaging of neural activity. Mol Syst Biol 8 35. PMID: 26043770.

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Keywords: VU 0463271, supplier, VU0463271, potent, selective, inhibitors, inhibits, neuronal, K-Cl, cotransporters, KCC2, Tocris Bioscience, K+/Cl-Cotransporter 2 Inhibitor products

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