(+)-KCC2 blocker 1 is a selective blocker of KCC2 (IC50 = 0.4 μM).

VU0463271 (N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide) is a potent and selective antagonist of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC50 of 61 nM and >100-fold selectivity versus the closely related Na-K-2Cl cotransporter 1 (NKCC1) and no activity in a larger panel of GPCRs, ion channels, and transporters.

VU0463271 quarterhydrate is a potent KCC2 antagonist, with an IC 50 of 61 nM [1].

ML-077, also known as VU0255011, is a highly selective, potent, saline soluble, best in class KCC2 antagonist for high fidelity in vitro studies on KCC2 function with IC(50)=537 nM. ML-077 is cell permeable and exhibits submicromolar potency

VU 0240551 is a selective antagonist of neuronal K-Cl cotransporter KCC2 inhibitor with an IC50 of 560 nM. VU 0240551 inhibits L-type calcium channels and hERG.

CLP257 is a selective K+-Cl− cotransporter KCC2 activator (EC50: 616 nM) and it is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 alleviates hypersensitivity in rats with neuropathic painc and it also modulates plasmalemmal KCC2 protein turnover post-translationally. CLP257 restores impaired Cl− transport in neurons with diminished KCC2 activity.

CLP290 is an activator of the neuron-specific K+-Cl cotransporter KCC2 and displays potential for the treatment of a wide range of neurological and psychiatric indications.