VU 0463271

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Cat.No. 4719 - VU 0463271 | CAS No. 1391737-01-1
Description: Potent and selective KCC2 inhibitor
Chemical Name: N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Reviews
Literature

Biological Activity

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
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1391737-01-1
PubChem ID 70690453
InChI Key DPONSKCACOZTGN-UHFFFAOYSA-N
Smiles O=C(N(C4CC4)C3=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
ethanol 3.83 10 with gentle warming
DMSO 19.12 50

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 solvent 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

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References

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:

Alfonsa et al (2016) Cl- out is a novel cooperative optogenetic tool for extruding chloride from neurons Nature Communications 7 13495 PMID: 27853135

Pál et al (2015) Appearance of fast astrocytic component in voltage-sensitive dye imaging of neural activity. Mol Syst Biol 8 35 PMID: 26043770


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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.