Application

CLP257 has been used as a K⁺- Cl^- cotransporter 2 (KCC2) enhancer in human neuron culture.

Biochem/physiol Actions

In streptozotocin treated rats, by activating a K⁺- Cl^- cotransporter 2 (KCC2) in the arginine-vasopressin neuron, CLP257 mediates γ-aminobutyric acid (GABA)ergic excitation. It is however inactive with KCC1, KCC3 and KCC4.

CLP257 is a selective K⁺-Cl⁻ cotransporter KCC2 activator that restored impaired Cl⁻ transport in neurons with reduced KCC2 activity. Apparently, CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally.

Packaging

5, 25 mg in glass bottle