CLP 257

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Cat.No. 5242 - CLP 257 | C14H14FN3O2S | CAS No. 1181081-71-9
Description: Selective KCC2 activator
Chemical Name: (5Z)-5-[(4-Fluoro-2-hydroxyphenyl)methylene]-2-(tetrahydro-1-(2H)-pyridazinyl)-4(5H)-thiazolone
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Selective KCC2 K+-Cl- cotransporter activator (EC50 = 616 nM). Exhibits selectivity for KCC2 over other KCC family members, NKCC1 and GABAA receptors, as well as 55 other receptors. Enhances Cl- transport and increases KCC2 plasma membrane expression in spinal slices with reduced KCC2 function. Alleviates hypersensitivity in rats with peripheral nerve injury.

Technical Data

M. Wt 307.34
Formula C14H14FN3O2S
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1181081-71-9
PubChem ID 44188931
InChI Key SKCADXVKQRCWTR-GHXNOFRVSA-N
Smiles OC1=C(/C=C2/C(N=C(N3CCCCN3)S2)=O)C=CC(F)=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
DMSO 30.73 100

Preparing Stock Solutions

The following data is based on the product molecular weight 307.34. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.25 mL 16.27 mL 32.54 mL
5 mM 0.65 mL 3.25 mL 6.51 mL
10 mM 0.33 mL 1.63 mL 3.25 mL
50 mM 0.07 mL 0.33 mL 0.65 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: CLP 257, supplier, CLP257, Selective, KCC2, K+-Cl-, cotransporters, activators, neuropathic, pain, K+/Cl-, Cotransporter, 2, Tocris Bioscience

Citations for CLP 257

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Literature in this Area

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.

Pathways for CLP 257

Protocols

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