VU 0240551

Pricing Availability   Qty
Description: KCC2 inhibitor
Chemical Name: N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide
Purity: ≥99% (HPLC)
Citations (8)
Literature (1)

Biological Activity for VU 0240551

VU 0240551 is an 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 for VU 0240551

M. Wt 342.43
Formula C16H14N4OS2
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 893990-34-6
PubChem ID 7211972
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 for VU 0240551

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 34.24 100
ethanol 8.56 25

Preparing Stock Solutions for VU 0240551

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.

Select a batch to recalculate based on the batch molecular weight:
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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References for VU 0240551

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

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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

8 Citations for VU 0240551

Citations are publications that use Tocris products. Selected citations for VU 0240551 include:

Gagnon et al (2013) Chloride extrusion enhancers as novel therapeutics for neurological diseases. Nat Med 19 1524 PMID: 24097188

Doyon et al (2011) Efficacy of synaptic inhibition depends on multiple, dynamically interacting mechanisms implicated in chloride homeostasis. Purinergic Signal 7 e1002149 PMID: 21931544

Alfredo et al (2020) Enhancing neuronal chloride extrusion rescues α2/α3 GABAA-mediated analgesia in neuropathic pain. Nat Commun 11 869 PMID: 32054836

Marie-Pascale et al (2021) Enhancing KCC2 activity decreases hyperreflexia and spasticity after chronic spinal cord injury. Exp Neurol 338 113605 PMID: 33453210

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

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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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.