VU 0463271

Name: VU 0463271
Brand: Tocris Bioscience
SKU: 4719

Tocris Bioscience, part of Bio-Techne | Catalog # 4719

Citations (34)

COA / SDS

Potent and selective KCC2 inhibitor

Key Product Details

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)
Molecular Weight:	382.5

View Full Technical Details for VU 0463271

Technical Data
Citations

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
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.

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

Solubility for VU 0463271

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	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.

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	0.10 mL	0.52 mL	1.05 mL

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References for VU 0463271

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

Sivakumaran Selective inhibition of KCC2 leads to hyperexcitability and epileptiform discharges in hippocampal slices and in vivo. J.Neurosci. 2015 PMID: 26019342
Delpire 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. 2012 PMID: 22727639