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Submit ReviewVU 0240551
Description: KCC2 inhibitor
Chemical Name: N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide
Purity: ≥99% (HPLC)
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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 the degree 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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Product Datasheets
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
If you know of a relevant reference for VU 0240551, please let us know.
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Keywords: VU 0240551, VU 0240551 supplier, cotransporter, potassium, chloride, transport, KCC2, Neuronal, cotransport, SLC12A5, Na+/2Cl-/K+, NKCC1, NKCC2, inhibitors, inhibits, Ion, Pumps, K-Cl, VU0240551, epilepsy, K+/Cl-, Cotransporter, 2, 3888, Tocris Bioscience
5 Citations for VU 0240551
Citations are publications that use Tocris products. Selected citations for VU 0240551 include:
Lavertu et al (2014) Enhancing K-Cl co-transport restores normal spinothalamic sensory coding in a neuropathic pain model. Brain 137 724 PMID: 24369380
Ferando et al (2016) Diminished KCC2 confounds synapse specificity of LTP during senescence. Nat Neurosci 19 1197 PMID: 27500406
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
Do you know of a great paper that uses VU 0240551 from Tocris? Please let us know.
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Literature in this Area
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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.