CLP257 (CLP-257) is a potent, selective K+-Cl- cotransporter KCC2 activator with EC50 of 616 nM.
CLP257 displays selectivity for KCC2 over other KCC family members, NKCC1 and GABAA receptors, and a panel of 55 other receptors.
CLP257 restores impaired Cl(-) transport in neurons, rescues KCC2 plasma membrane expression.
CLP257 renormalizes stimulus-evoked responses in spinal nociceptive pathways in a rat model of neuropathic pain.
