VU 0240551

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Cat.No. 3888 - VU 0240551 | C16H14N4OS2 | CAS No. 893990-34-6
Description: KCC2 inhibitor
Chemical Name: N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide
Purity: ≥99% (HPLC)
Datasheet
Citations (5)
Reviews
Literature

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
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 893990-34-6
PubChem ID 7211972
InChI Key WJRWSLORVIHRNX-UHFFFAOYSA-N
Smiles O=C(NC3=NC(C)=CS3)CSC(C=C2)=NN=C2C1=CC=CC=C1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 34.24 100
ethanol 8.56 25

Preparing Stock Solutions

The following data is based on the product molecular weight 342.43. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.92 mL 14.6 mL 29.2 mL
5 mM 0.58 mL 2.92 mL 5.84 mL
10 mM 0.29 mL 1.46 mL 2.92 mL
50 mM 0.06 mL 0.29 mL 0.58 mL

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References

References are publications that support the biological activity of the product.

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

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

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


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5 Citations for VU 0240551

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

Doyon et al (2011) Efficacy of synaptic inhibition depends on multiple, dynamically interacting mechanisms implicated in chloride homeostasis. Purinergic Signal 7 e1002149 PMID: 21931544

Haam et al (2012) GABA is excitatory in adult vasopressinergic neuroendocrine cells. J Neurosci 32 572 PMID: 22238092

Ferando et al (2016) Diminished KCC2 confounds synapse specificity of LTP during senescence. Nat Neurosci 19 1197 PMID: 27500406

Lavertu et al (2014) Enhancing K-Cl co-transport restores normal spinothalamic sensory coding in a neuropathic pain model. Brain 137 724 PMID: 24369380


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

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GABA Receptors

GABA Receptors Scientific Review

Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.