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Submit ReviewCLP 257
Description: Selective KCC2 activator
Chemical Name: (5Z)-5-[(4-Fluoro-2-hydroxyphenyl)methylene]-2-(tetrahydro-1-(2H)-pyridazinyl)-4(5H)-thiazolone
Purity: ≥98% (HPLC)
Biological Activity for CLP 257
CLP 257 is a 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 for CLP 257
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CLP 257
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 30.73 | 100 |
Preparing Stock Solutions for CLP 257
The following data is based on the product molecular weight 307.34. 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 |
|---|---|---|---|
| 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 for CLP 257
References for CLP 257
References are publications that support the biological activity of the product.
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, CLP 257 supplier, CLP257, Selective, KCC2, K+-Cl-, cotransporters, activators, neuropathic, pain, K+/Cl-, Cotransporter, 2, 5242, Tocris Bioscience
1 Citation for CLP 257
Citations are publications that use Tocris products. Selected citations for CLP 257 include:
Ferando et al (2016) Diminished KCC2 confounds synapse specificity of LTP during senescence. Nat Neurosci 19 1197 PMID: 27500406
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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
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.