Potassium Channel Modulator

DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB voltage-dependently activates potassium channels TREK1 and TRAAK, and inhibits TRESK, TASK1 and TASK3 (IC₅₀s: 0.14, 0.95, 50.72 μM, respectively). DCPIB is also a selective blocker of swelling-induced chloride current (I_Cl,swell), with an IC₅₀ of 4.1 μM. DCPIB is a useful tool for investigating structure-function studies of K2P channels.

AUT1 is a recombinant human Kv3 channel modulator. AUT1 modulates Kv3.1b and Kv3.2a channels in human recombinant with pEC₅₀ values of 5.33 and 5.31 μM, respectively. AUT1 can be used for the research of disorders associated with dysfunction of inhibitory feedback in corticolimbic circuits, such as schizophrenia.

NPBA, a potassium K2P channel TASK-3 (KCNK9) agonist, is a tandem pore domain weak inward rectifying K⁺ channel (TWIK2) channel blocker. NPBA suppresses NLRP3 inflammasome activation in macrophages.

Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (K_i=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.

ICA 110381 is an orally active Kv7.2/Kv7.3 (KCNQ2/3) potassium channel activator with anticonvulsive properties. ICA 110381 is a KCNQ2/Q3 activator (EC₅₀=0.38 μM) as well as KCNQ1 antagonist (IC₅₀=15 μM).

Brevetoxin B (Brevetoxin-2) is a red tide toxin. Brevetoxin B affects sodium, potassium and calcium currents in nerve terminals. Brevetoxin B also modulates the metabolic activity of Jurkat cells, reduces cell viability and induces apoptosis. Brevetoxin B can be used in research on synaptic transmission and tumors.

TMEM175 modulator 1 (compound 47) is a TMEM175 modulator.TMEM175 modulator 1 modulates activity of the lysosomal potassium ion channel TMEM175.TMEM175 modulator 1 can be used for the research of parkinson’s disease, dementia, alzheimer’s disease, l-dopa induced dyskinesia.

LUF7244 is a selective allosteric modulator of K_v11.1 channels. LUF7244 inhibits early afterdepolarizations. LUF7244 can be used for anti-arrhythmia research.

Kv3.1 modulator 2 (compound 4) is a Kv3.1 channels modulator with an EC₅₀ value of 68 nM.

Icariside E4 is an antinociceptive agent, and can be isolated from Tabebuia roseo-alba. Icariside E4 has peripheral analgesic activity by ATP-sensitive K⁺ channel-dependent mechanisms. Icariside E4 also has anti-oxidant, anti-Alzheimer and anti-inflammatory effects.

KCC2 Modulator-2 (example 53) is a KCC2 modulator with an EC₅₀ of 0.215 μM. KCC2 Modulator-2 can be used in the study of neurological disorders.

Nav1.8 modulator 1 (compound 1) is a potent Nav1.8 modulator. Nav1.8 modulator 1 has the potential for pain research.

KCC2 Modulator-1 (example 52) is a KCC2 modulator. KCC2 Modulator-1 is used for the research of neurological disorders.

Kv3 modulator 2 (formula (I)) is a potent Kv3 channels modulator extracted from patent WO2018109484A1, compound formula (I) , has analgesic activity and is used in the prophylaxis or treatment of related disorders.

Kv3 modulator 4 is a Kv3.1 (pEC₅₀=5.45) and Kv3.2 modulator extracted from patent WO2018020263A1, Cyclobutyl structure.

Cariporide is a Na+/H+ Exchanger 1 (NHE-1) inhibitor. Cariporide inhibits the expression of monocyte endothelial cell adhesion and intercellular adhesion molecule-1 (ICAM-1) mediated by high glucose (HG) by inhibiting the activation of NHE-1.

Kv3 modulator 3 (Compound 4) is a selective modulator of Kv3.1 and/or Kv3.2 and/or Kv3.3 channels extracted from patent WO2017098254A1, compound 4, has analgesic activity for use in the prophylaxis o or treatment of pain.

RA-2 is a negative-gating modulator of KCa2/3 channels with an IC₅₀ of 17 nM. RA-2 inhibits bradykinin-induced endothelium-derived hyperpolarization (EDH)-type relaxation in U46619-precontracted rings. RA-2 can help to define the physiologic and pathomechanistic roles of KCa2/3 in the vasculature, central nervous system, and during inflammation.

Kv7.2/Kv7.3 modulator-3 (example 40 peak-1) is a selective K_v7.2/K_v7.3 modulator with an EC₅₀ of 0.099 μM.

AU-1421 is a potassium ion (K⁺) site-directed regulator that specifically acts on various cation transport ATPases. AU-1421 can distinguish between two different K⁺-sensitive phosphorylation intermediate (E2P) states: for non-K⁺ transport type ATPases (such as the sarcoplasmic reticulum Ca²⁺-ATPase), after binding to AU-1421, it mimics the agonistic effect of K⁺, significantly accelerating the hydrolysis (dephosphorylation) of E2P. For K⁺ transport type ATPases (such as the gastric mucosa H⁺/K⁺-ATPase and the renal Na⁺/K⁺-ATPase), after binding to AU-1421, it inhibits the hydrolysis of E2P, stabilizing the phosphorylated intermediate, thereby blocking the ion transport cycle. AU-1421 can be used to study the mechanism of the potassium ion pump.