Home / KCC2 Inhibitors / VU 0463271

VU 0463271

Catalog #: 4719
5 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
4719/10
4719/50
VU 0463271 | CAS No. 1391737-01-1 | KCC2 Inhibitors
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Description: Potent and selective KCC2 inhibitor

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

Purity: ≥98%

Product Details
Citations (5)
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Biological Activity

VU 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.

Technical Data

M.Wt:
382.5
Formula:
C19H18N4OS2
Solubility:
Soluble to 50 mM in DMSO
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
1391737-01-1

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

  1. 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
  2. Selective inhibition of KCC2 leads to hyperexcitability and epileptiform discharges in hippocampal slices and in vivo.
    Sivakumaran et al.
    J.Neurosci., 2015;35:8291
  3. Sortilin gates neurotensin and BDNF signaling to control peripheral neuropathic pain
    M Richner, LT Pallesen, M Ulrichsen, ET Poulsen, TH Holm, H Login, A Castonguay, LE Lorenzo, NP Gonçalves, OM Andersen, K Lykke-Hart, JJ Enghild, LCB Rønn, IJ Malik, Y De Koninck, OJ Bjerrum, CB Vægter, A Nykjær
    Sci Adv, 2019;5(6):eaav9946.

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Citations for VU 0463271

The citations listed below are publications that use Tocris products. Selected citations for VU 0463271 include:

5 Citations: Showing 1 - 5

  1. SNAP23 regulates KCC2 membrane insertion and activity following mZnR/GPR39 activation in hippocampalneurons.
    Authors: Israel Et al.
    iScience  2022;25:103751
  2. CLP290 promotes the sedative effects of midazolam in neonatal rats in a KCC2-dependent manner: A laboratory study in rats.
    Authors: Akiko Et al.
    PLoS One  2021;16:e0248113
  3. A Cellular Mechanism of Learning-Induced Enhancement of Synaptic Inhibition: PKC-Dependent Upregulation of KCC2 Activation.
    Authors: Sourav Et al.
    Sci Rep  2020;10:962
  4. Cl- out is a novel cooperative optogenetic tool for extruding chloride from neurons
    Authors: Alfonsa Et al.
    Nature Communications  2016;7:13495
  5. 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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