VU 0463271

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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)
Citations (5)
Literature (1)

Biological Activity for VU 0463271

VU 0463271 is a 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 for VU 0463271

M. Wt 382.5
Formula C19H18N4OS2
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1391737-01-1
PubChem ID 70690453
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.

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

Solubility Data for VU 0463271

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 19.12 50

Preparing Stock Solutions for VU 0463271

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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets for VU 0463271

Certificate of Analysis / Product Datasheet
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References for VU 0463271

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

5 Citations for VU 0463271

Citations are publications that use Tocris products. Selected citations for VU 0463271 include:

Akiko et al (2021) CLP290 promotes the sedative effects of midazolam in neonatal rats in a KCC2-dependent manner: A laboratory study in rats. PLoS One 16 e0248113 PMID: 33711029

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

Israel et al (2022) SNAP23 regulates KCC2 membrane insertion and activity following mZnR/GPR39 activation in hippocampalneurons. iScience 25 103751 PMID: 35118363

Sourav et al (2020) A Cellular Mechanism of Learning-Induced Enhancement of Synaptic Inhibition: PKC-Dependent Upregulation of KCC2 Activation. Sci Rep 10 962 PMID: 31969605

Do you know of a great paper that uses VU 0463271 from Tocris? Please let us know.

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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* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

GABA Receptors Scientific Review

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.