Potassium Channel
KcsA
Potassium channels are the most widely distributed type of ion channel and are found in virtually all living organisms. They form potassium-selective pores that span cell membranes. Potassium channels are found in most cell types and control a wide variety of cell functions. Potassium channels function to conduct potassium ions down their electrochemical gradient, doing so both rapidly and selectively. Biologically, these channels act to set or reset the resting potential in many cells. In excitable cells, such asneurons, the delayed counterflow of potassium ions shapes the action potential. By contributing to the regulation of the action potential duration in cardiac muscle, malfunction of potassium channels may cause life-threatening arrhythmias. Potassium channels may also be involved in maintaining vascular tone.
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Potassium Channel Inhibitors
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Potassium Channel Agonists
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Potassium Channel Antagonists
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Potassium Channel Activators
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Potassium Channel Modulators
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Potassium Channel Chemical
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Potassium Channel Controls
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Potassium Channel Related Products (1121)
Related Products (1121)
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Antibodies (6)
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Related Compound Screening Libraries (1)
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Hypaconitine
0 ImagesHypaconitine inhibits the KCNH2 current with an IC50 of 8.1 nM, and exhibits cardiotoxicity. Hypaconitine inhibits TGF-β1-induced epithelial-mesenchymal transition (EMT) in A549 cell through the inhibition of NF-κB nuclear translocation. Hypaconitine acts as the neuromuscular blocker. Hypaconitine is orally active.
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Dalazatide
0 ImagesSynonyms: ShK-186Dalazatide (ShK-186) is a specific Kv1.3 potassium channel peptide inhibitor. Dalazatide can be used in the study of autoimmune diseases such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes and inflammatory bowel disease.
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Linopirdine
0 ImagesSynonyms: DuP 996Linopirdine (DuP 996) is an orally active, selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing agent, increases acetylcholine release in rat brain tissue.
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Talatisamine
0 ImagesTalatisamine is an orally active cyclophilin D activator isolated from the roots of Aconitum carmichaeli Debx. Talatisamine exerts biological functions by activating cyclophilin D, inhibiting Ca2+-dependent opening of the mitochondrial permeability transition pore (mPTP) (IC50=78 μM), and blocking delayed rectifier K+ channels (IC50=146 μM). Talatisamine possesses both antioxidant and membrane-stabilizing properties, effectively inhibits lipid peroxidation and protects mitochondrial membrane function. Talatisamine exhibits multiple activities including antiarrhythmic, hypotensive, anti-inflammatory, anticancer and neuroprotective effects. Talatisamine finds applications in the research of ischemic diseases, rheumatoid arthritis, inflammation-related diseases and Alzheimer's disease.
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ADL-5859 hydrochloride
0 ImagesADL-5859 hydrochloride (compound 20) is a selective and orally active δ opioid receptor (DOR) agonist with an Ki and an EC50 value of 0.84 and 20 nM, respectively. ADL-5859 hydrochloride also shows inhibitory activity to hERG channel with an IC50 value of 78 μM. ADL-5859 hydrochloride can be used for the research of pain.
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Dihydroberberine
0 ImagesDihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy.
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Norfluoxetine hydrochloride
0 ImagesNorfluoxetine hydrochloride is the active metabolite of the antidepressant Fluoxetine (HY-B0102); it is also a TREK-2 K2P potassium channel inhibitor. Norfluoxetine hydrochloride exhibits neuroimmunological activity, induces apoptosis in primary microglial cells, and inhibits the release of pro-inflammatory factors. Norfluoxetine hydrochloride inhibits high-threshold voltage-gated Ca2+ currents in neurons with an EC50 of 20.4 μM. Norfluoxetine hydrochloride can be used in research related to depression, ischemic stroke, and epilepsy.
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VU 0240551
0 ImagesVU 0240551 is a potent neuronal K-Cl cotransporter KCC2 inhibitor (IC50=560 nM) and is selective versus NKCC1. VU 0240551 also inhibits hERG and L-type Ca2+ channels. VU 0240551 attenuates GABA-induced hyperpolarization of P cells, produces a positive shift in the P cell GABA reversal potential and enhances P cell synaptic transmission.
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ASP2905
0 ImagesASP2905 is an orally active potassium channel Kv12.2 inhibitor encoded by the Kcnh3/BEC1 gene. ASP2905 can cross the blood-brain barrier and has antipsychotic activities.
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Tricarbonyldichlororuthenium(II) dimer
0 ImagesSynonyms: CORM-2Tricarbonyldichlororuthenium(II) dimer (CORM-2) is a CO-releasing molecule. Tricarbonyldichlororuthenium(II) dimer exhibits anti-inflammatory, antioxidant, and gastric mucosa-protective activities. Additionally, Tricarbonyldichlororuthenium(II) dimer has CO-independent functional effects on multiple potassium channels.
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5-Hydroxydecanoate sodium
0 Images5-Hydroxydecanoate sodium is a selective ATP-sensitive K+ (KATP) channel blocker (IC50 of ~30 μM). 5-Hydroxydecanoate sodium is a substrate for mitochondrial outer membrane acyl-CoA synthetase and has antioxidant activity.
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Mosapride citrate
0 ImagesSynonyms: TAK-370 citrate; AS-4370 citrateMosapride citrate is an orally active gastroenterokinetic compound. Mosapride citrate is a 5HT4 agonist. Mosapride citrate is a CYP inducer. Mosapride citrate has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride citrate can be used in the study of gastrointestinal diseases.
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Spadin
0 ImagesSpadin, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with IC50 value of 10 nM. Spadin enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin can be used for antidepressant research.
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Margatoxin
0 ImagesMargatoxin, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research.
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VU0529331
0 ImagesVU0529331 is a homomeric GIRK channel activator, with an EC50 value of 5.1 μM for human GIRK2 and an EC50 value of 22.3 μM for GIRK4. VU0529331 serves as a starting point for the development of non-GIRK1/X channel probes and also acts as a tool for studying homomeric GIRK channels. VU0529331 is applicable to research related to addiction, primary aldosteronism and delayed-onset obesity.
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VU0134992 hydrochloride
0 ImagesVU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC50 of 0.97 µM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 µM) at -120 mV.
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ICA-105574
0 ImagesICA-105574 is a potent and efficacious hERG channel activator. The primary mechanism by which ICA-105574 potentiates hERG channel activity is by removing hERG channel inactivation. ICA-105574 steeply potentiates current amplitudes more than 10-fold with an EC50 value of 0.5 +/- 0.1 μM and a Hill slope (n(H)) of 3.3 +/- 0.2. ICA-105574 can prevent arrhythmias induced by cardiac delayed repolarization. ICA-105574 shortens action potential duration in ventricular myocytes concentration-dependently.
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Ropivacaine hydrochloride
0 ImagesRopivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine is widely used for neuropathic pain management in vivo.
