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VU 0240551

Catalog #: 3888
8 Citations Datasheet / COA / SDS

Discontinued Product

3888 has been discontinued.
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VU 0240551 | CAS No. 893990-34-6 | KCC2 Inhibitors
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Description: KCC2 inhibitor

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

Purity: ≥99%

Product Details
Citations (8)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

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

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Product Datasheets

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Citations for VU 0240551

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

8 Citations: Showing 1 - 8

  1. Enhancing KCC2 activity decreases hyperreflexia and spasticity after chronic spinal cord injury.
    Authors: Marie-Pascale Et al.
    Exp Neurol  2021;338:113605
  2. Enhancing neuronal chloride extrusion rescues α2/α3 GABAA-mediated analgesia in neuropathic pain.
    Authors: Alfredo Et al.
    Nat Commun  2020;11:869
  3. Diminished KCC2 confounds synapse specificity of LTP during senescence.
    Authors: Ferando Et al.
    Nat Neurosci  2016;19:1197
  4. Potentiation of Synaptic GluN2B NMDAR Currents by Fyn Kinase Is Gated through BDNF-Mediated Disinhibition in Spinal Pain Processing.
    Authors: Yi Et al.
    Cell Rep  2016;17:2753-2765
  5. Enhancing K-Cl co-transport restores normal spinothalamic sensory coding in a neuropathic pain model.
    Authors: Lavertu Et al.
    Brain  2014;137:724
  6. Chloride extrusion enhancers as novel therapeutics for neurological diseases.
    Authors: Gagnon Et al.
    Nat Med  2013;19:1524
  7. GABA is excitatory in adult vasopressinergic neuroendocrine cells.
    Authors: Haam Et al.
    J Neurosci  2012;32:572
  8. 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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