kcc2

(+)-KCC2 blocker 1 is a selective inhibitor of KCC2 with an IC50 of 0.4 μM.

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.

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.

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.

KCC2 Modulator-2 (example 53) is a regulator of KCC2 with an EC50 of 0.215 μM. It is used in the research of neurological diseases.

Compound 2, known as KCC2 potentiators-1, acts as an enhancer of the potassium chloride cotransporter-2 (KCC2). It holds potential for applications in studies related to neurological disorders.

KCC2 Modulator-3 (Example 54) is a KCC2 modulator with an EC50 of 0.253 μM. It is applicable in the study of neurological disorders such as epilepsy, neuropathic pain, and Rett syndrome.

KCC2 Modulator-1 (Example 52), possessing an EC50 value of 0.146 μM, acts as a modulator of KCC2 and is utilized in the study of diseases mediated by KCC2 [1].

Carbonic anhydrase inhibitor32 (compound 5B) is an orally active, selective inhibitor of hCA (carbonic anhydrase) II/VII, with Ki values of 6.3 nM for hCA II, 10.1 nM for hCA VII, and 681 nM for hCA I. It shows potential for neuroprotection and anticonvulsant effects by reducing mTOR activation and increasing hippocampal KCC2 levels.

VU0463271 quarterhydrate is a potent KCC2 antagonist with an IC50 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.