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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.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|ethanol||3.83||10 with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 382.5. 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|
|0.5 mM||5.23 mL||26.14 mL||52.29 mL|
|2.5 mM||1.05 mL||5.23 mL||10.46 mL|
|5 mM||0.52 mL||2.61 mL||5.23 mL|
|25 mM||0.1 mL||0.52 mL||1.05 mL|
References are publications that support the biological activity of the product.
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
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
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Keywords: VU 0463271, VU 0463271 supplier, VU0463271, potent, selective, inhibitors, inhibits, neuronal, K-Cl, cotransporters, KCC2, K+/Cl-, Cotransporter, 2, 4719, Tocris Bioscience
2 Citations for VU 0463271
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
Alfonsa et al (2016) Cl- out is a novel cooperative optogenetic tool for extruding chloride from neurons Nature Communications 7 13495 PMID: 27853135
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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.