CLP 290

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Cat.No. 6758 - CLP 290 | C19H21FN4O3S | CAS No. 1181083-81-7
Description: K+/Cl- cotransporter 2 (KCC2) activator; orally bioavailable prodrug of CLP 257 (Cat. No.5242)
Chemical Name: (Z)-5-Fluoro-2-((4-oxo-2-(tetrahydropyridazin-1(2H)-yl)thiazol-5(4H)-ylidene)methyl)phenyl pyrrolidine-1-carboxylate
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (1)

Biological Activity

K+/Cl- Cotransporter 2 (KCC2) activator. Activates spinal inhibitory interneurons, restores physiological neuronal activity in the spinal cord and induces functional recovery in a mouse model of spinal cord injury. Also decreases blood vasopressin and glucose levels in mice with Streptozotocin (Cat. No. 1621) induced diabetes mellitus. Orally bioavailable prodrug of CLP 257 (Cat. No.5242).

Technical Data

M. Wt 404.46
Formula C19H21FN4O3S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1181083-81-7
PubChem ID 68637267
InChI Key DIXMMXNNKLCLOM-WJDWOHSUSA-N
Smiles FC1=CC(OC(N2CCCC2)=O)=C(C=C1)/C=C3SC(N4CCCCN4)=NC\3=O

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 20.22 50
ethanol 2.02 5

Preparing Stock Solutions

The following data is based on the product molecular weight 404.46. 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 4.94 mL 24.72 mL 49.45 mL
2.5 mM 0.99 mL 4.94 mL 9.89 mL
5 mM 0.49 mL 2.47 mL 4.94 mL
25 mM 0.1 mL 0.49 mL 0.99 mL

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References

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

Kim et al (2019) Long-term ionic plasticity of GABAergic signalling in the hypothalamus. J.Neuroendocrinol. 31 e12753 PMID: 31166034

Chen et al (2018) Reactivation of dormant relay pathways in injured spinal cord by KCC2 manipulations. Cell 174 521 PMID: 30033363


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Keywords: CLP 290, CLP 290 supplier, CLP290, CLP257, Selective, KCC2, K+/Cl-, cotransporters, activators, activates, neuropathic, pain, orally, bioavailable, Cotransporter, 2, 6758, Tocris Bioscience

Citations for CLP 290

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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* or download your copy today!

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


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.