Catalog No.
Product Name
Application
Product Information
Citations
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TREK Activator
CAT335 is a selective and irreversible activator of the TREK-1 channel. This compound enhances TREK-1 activity, making it useful for investigating the underlying mechanisms of pain sensation, the regulation of sleep, and the modulation of intraocular pressure. Its specific action on TREK-1 allows for targeted research applications in neurobiology and ocular physiology. -
TREK-1 Inhibitor
TWIK-1/TREK-1-IN-3 is a potent inhibitor of the TREK-1 potassium channel, a member of the two-pore domain potassium (K2p) channel family. This compound selectively targets the TREK-1 homodimer and the TWIK-1/TREK-1 heterodimer with IC50 values of 9.74 μM and 16.5 μM, respectively. Its inhibition of TREK-1 is associated with notable antidepressant-like effects, making it a valuable tool for research in depression and related disorders. -
Antihypertensive Agent
Celikalim is an antihypertensive agent that primarily acts by opening potassium channels in vascular smooth muscle, resulting in a reduction in blood pressure. In addition to its vasodilatory effects, Celikalim exhibits the ability to inhibit white thrombus formation. This compound serves as a potent potassium channel opener in canine models and is valuable for research related to thrombosis. -
hERG Channel Activator
PD-307243 is a specific activator of the human Ether-à-go-go-Related Gene (hERG) potassium channel. It is primarily utilized in studies related to cardiac arrhythmias, aiding in the examination of hERG channel function and its implications in heart rhythm disorders. This compound serves as a valuable tool for investigating the pharmacological modulation of ion channels in cardiovascular research. -
KCa2.1 Inhibitor
B-TPMF is a selective inhibitor of the KCa2.1 channel, demonstrating an IC50 value of 30 nM. This compound engages in a competitive functional interaction with CM-TPMF. B-TPMF is utilized in research applications exploring calcium-activated potassium channels, contributing to the understanding of various physiological processes and potential therapeutic targets. -
Daul TREK-1/TREK-2 Inhibitor
ONO-9517601 is a potent and selective dual inhibitor of TREK-1 and TREK-2 channels, with IC50 values of 0.067 μM and 0.23 μM, respectively. This compound effectively penetrates the central nervous system and demonstrates strong efficacy in the MK-801-induced novel object recognition task in rats. ONO-9517601 is suitable for research on neurological and cognitive disorders, providing insights into the mechanisms of these conditions. -
Delayed Rectifier Potassium Current Blocker
WAY-125971 is a potent blocker of the delayed rectifier potassium current (IK), functioning as a propylamine analogue. This compound exhibits a high degree of specificity in its action, making it a valuable tool for investigating the mechanisms underlying arrhythmias. Its utility in electrophysiological studies aids in understanding cardiac ion channel dynamics and potential therapeutic targets for heart rhythm disorders. -
Daul TREK-1/TREK-2 Inhibitor
ONO-7927846 is a selective dual inhibitor of TREK-1 and TREK-2 channels, exhibiting potent activity with IC50 values of 0.11 μM for TREK-1 and 0.29 μM for TREK-2. This compound demonstrates significant efficacy in preclinical models, particularly in the MK-801-induced novel object recognition paradigm, highlighting its potential in research on neurological and cognitive disorders. ONO-7927846 is suitable for investigating the therapeutic implications of modulating these potassium channels in various CNS-related conditions. -
KV11.1 Channel Activator
VU0405601 is a potent activator of the KV11.1 ion channel, which plays a crucial role in cardiac repolarization. This compound has demonstrated the ability to protect cardiac tissue from dofetilide-induced ventricular tachycardia, making it valuable for research into arrhythmias and cardiac safety. Its mechanism of action positions it as a significant tool for studying cardiac electrophysiology and developing therapeutic strategies for related heart conditions. -
K+ Channel Opener
ZM226600 is an ATP-sensitive potassium channel opener with an EC50 of 500 nM. This compound effectively inhibits spontaneous activity in bladder tissues, making it a valuable tool for studying bladder function and disorders. Its ability to modulate potassium channels can offer insights into various physiological processes and potential therapeutic approaches in urology research. -
KCa2 Channel Modulator
KCa2 Channel Modulator 2 is a potent positive modulator of the KCa2 channel subtypes, specifically targeting KCa2.2a and KCa2.3. This compound demonstrates comparable efficacy with EC50 values of 0.64 μM for rat KCa2.2a and 0.60 μM for human KCa2.3 channels. Its selective modulation makes it suitable for investigations into the physiological roles of KCa2 channels and their potential implications in therapeutic applications related to calcium signaling and excitability in various tissues. -
Kv7.2/Kv7.3 Activator
Kv7.2/Kv7.3 activator-4 is a selective activator of the Kv7.2 and Kv7.3 potassium channels. It enhances neuronal excitability, making it a valuable tool in research related to epilepsy and neuropathic pain, as well as other neurological disorders. This compound aids in the investigation of Kv7 channel modulation, contributing to understanding their roles in various pathophysiological conditions. -
Antiarrhythmic Agent
L-702958 is a potent blocker of the human ether-à-go-go-related gene (hERG) potassium channel with an IC50 of 14.3 nM. This compound exhibits significant antiarrhythmic activity, making it valuable for research into the mechanisms underlying arrhythmias and potential therapeutic applications. L-702958 is essential for studies focused on cardiac electrophysiology and ion channel modulation. -
hERG Inhibitor
hERG-IN-2 is a potent inhibitor of the human Ether-à-go-go-Related Gene (hERG) potassium channel, demonstrating an IC50 of less than 2 μM. This compound is valuable for investigating the role of hERG channel activity in cancer research, making it a useful tool for studying tumor cell proliferation and apoptosis. Researchers can utilize hERG-IN-2 to explore therapeutic strategies targeting hERG-related pathways in oncology. -
Insulinotropic Agent/K+ Channel Blocker
BTS-67582 is an orally active nonsulfonylurea insulinotropic agent that functions as a potassium channel blocker, specifically targeting the K+ ATP channel in pancreatic islet cells through a distinct binding site compared to sulfonylureas. This compound exhibits significant antidiabetic activity, making it valuable for research applications aimed at understanding insulin secretion and glucose homeostasis. Its unique mechanism offers insights into alternative strategies for diabetes treatment. -
Potassium Channel Inhibitor
Noxiustoxin is a potent inhibitor of voltage-dependent potassium channels, specifically Kv1.3, with an IC50 of 360 nM, as well as calcium-activated potassium channels. Derived from the venom of the Mexican scorpion Centruroides noxius, this peptide is significant in the study of neuroinflammatory diseases. Noxiustoxin serves as a valuable tool for researchers investigating ion channel functions and their roles in various physiological and pathological processes. -
Kv4.2 Inhibitor
Heteropodatoxin-2 is a peptide consisting of 30 amino acids that acts as a selective inhibitor of the Kv4.2 potassium channel. This compound effectively blocks Kv4.2 currents expressed in Xenopus laevis oocytes in a voltage-dependent manner, exhibiting reduced inhibition at depolarized potentials. Heteropodatoxin-2 is valuable for studying ion channel physiology and the role of Kv4.2 in cardiac and neuronal signaling pathways. -
TREK-1/TREK-2 Channel activator
C3001a is a selective activator of the TREK-1 and TREK-2 potassium channels, exhibiting EC50 values of 12.81 μM and 11.31 μM, respectively. This compound specifically interacts with the cryptic binding site formed by P1 and TM4 in TREK-1, with no impact on other two-pore domain K+ channels. C3001a is applicable in research exploring pain mechanisms and pancreatitis. -
Antidepressant
TWIK-1/TREK-1-IN-2 is a specific inhibitor of the TWIK-1 and TREK-1 potassium channels. It demonstrates inhibitory activity against TREK-1 homodimers and TWIK-1/TREK-1 heterodimers with IC50 values of 10.13 μM and 15.5 μM, respectively. This compound has potential applications in antidepressant research, particularly in studies focusing on the modulation of mood and anxiety disorders. -
Potassium Conduction Blocker
GEA 857 is a potent potassium conduction blocker that selectively inhibits calcium-dependent potassium channels. By blocking these channels, GEA 857 enhances the effects of muscarinic receptor agonists, potentially prolonging muscarinic cholinergic responses. This compound is particularly useful in the investigation of neurodegenerative diseases, providing insights into cholinergic signaling pathways and their therapeutic modulation. -
Potassium Channel Activator
Phe-Met-Arg-Phe, amide acetate is a potent potassium channel activator, exhibiting a dose-dependent activation of K+ current in peptidergic caudodorsal neurons, with an ED50 of 23 nM. This compound facilitates research into neuronal signaling pathways and the modulation of excitability in neurons. Its specific mechanism of action makes it valuable for studying potassium channel dynamics and their implications in neurophysiological processes. -
Potassium Channel Inhibitor
CK-1649 chloride is a selective potassium channel inhibitor recognized for its class III antiarrhythmic properties. By inhibiting potassium channel activity, this compound plays a crucial role in the modulation of cardiac action potentials and is relevant in researching arrhythmia mechanisms and potential therapeutic interventions in cardiac conditions. Its application in pharmacological studies makes it a valuable tool for investigating ion channel dynamics. -
Potassium Channel Inhibitor
HsTX1 is a potent inhibitor of potassium channels, specifically Kv1.3, with an IC50 of 12 pM. This 34-residue peptide, derived from the scorpion Heterometrus spinnifer, is stabilized by four disulfide bonds. HsTX1 plays a critical role in modulating immune responses by inhibiting TEM cell activation and reducing inflammation in autoimmune conditions, making it a valuable tool for research in these areas. -
Potassium Channel
Lanceotoxin A is a potent inhibitor of potassium channels, exerting significant effects on cell membrane potential regulation. Research indicates that lanceotoxin A correlates negatively with extracellular metabolites in patients post-metabolic surgery, suggesting its involvement in metabolic processes. Additionally, this compound may influence intestinal microbial composition and its relationship to insulin resistance, highlighting its potential role in addressing metabolic syndrome and diabetes. -
Potassium Channel
VU714 oxalate is a selective inhibitor of the Kir7.1 potassium channel, impacting channel activity by enhancing the blockade induced by other structurally distinct inhibitors. This compound modulates the pharmacological profile of Kir channels through interactions with critical amino acid residues, making it a valuable tool for investigating Kir channel functions. It is applicable in research focused on cardiovascular, renal, and neurological areas where potassium channels play crucial roles. -
Antiarrhythmic Agent
WAY-123398 is a class III antiarrhythmic agent known for its selective inhibition of the delayed rectifier potassium current. This compound demonstrates significant potential in modulating cardiac electrophysiology and is primarily utilized in research focusing on arrhythmia mechanisms and treatment strategies. Its ability to target specific potassium channels makes it valuable in the study of cardiac dysfunction and the development of novel antiarrhythmic therapies. -
Potassium Channel Blocker
BRL-32872 is a potent blocker of the human ether-a-go-go-related gene (hERG) potassium channels, exhibiting an IC50 of 241 nM in isolated cardiomyocytes and 19.8 nM in HEK293 cells. This compound is of particular interest for the study of cardiac arrhythmias, including both atrial and ventricular rhythm disorders. Its ability to inhibit hERG channels makes it a valuable tool for investigating the mechanisms underlying cardiac electrical activity and potential therapeutic interventions. -
TREK-1 Agonist
BML264, a TREK-1 agonist, functions primarily through the activation of the TREK-1 potassium channel. This compound is valuable for investigating various pathologies linked to TASK1 dysfunction, providing insights into related ion channel activity and neuronal signaling. Its application in research can enhance the understanding of conditions such as pain, mood disorders, and neuroprotection. -
Potassium Channel Inhibitor
BDS-I is a potent potassium channel inhibitor specifically targeting the Kv3.4 subtype. This marine-derived toxin, extracted from Anemonia sulcata, effectively inhibits the Aβ1-42-induced enhancement of Kv3.4 activity, caspase-3 activation, and abnormal nuclear morphology in NGF-differentiated PC-12 cells. BDS-I demonstrates protective effects against Aβ peptide-induced cell death, making it a valuable tool for research into neurodegenerative diseases and cellular apoptosis pathways. -
Atrial-specific Potassium Channel Blocker
Inakalant is an atrial-specific potassium channel blocker that exhibits antiarrhythmic activity. By selectively inhibiting potassium channels in cardiac myocytes, Inakalant prolongs action potential duration (APD) and enhances the effective refractory period in both atrial and ventricular tissues. This mechanism is crucial for terminating and preventing arrhythmias, particularly atrial fibrillation (AF). Inakalant is useful for research in arrhythmia management and cardiac electrophysiology. -
Kv1.3 Inhibitor
UK-78282 hydrochloride is a selective inhibitor of the potassium channel Kv1.3, exhibiting an IC50 of 200 nM. This compound effectively suppresses the activation of human T-lymphocytes in vitro, making it a valuable tool for immunology research. UK-78282 hydrochloride binds to residues on the inner surface of the Kv1.3 channel, overlapping with the binding site of verapamil, thereby enhancing the understanding of ion channel modulation in immune responses. -
Potassium Channel Agonist
BMS-182264 is a highly selective agonist of ATP-sensitive potassium channels. It promotes potassium efflux and membrane hyperpolarization, leading to smooth muscle relaxation and vasodilation. This compound is valuable for studying cardiovascular conditions, including hypertension and myocardial ischemia, offering insights into potential therapeutic interventions. -
hERG Inhibitor
ERG-IN-5 is a potent hERG potassium channel inhibitor, demonstrating an IC50 value of 1.5 μM. This compound exhibits significant cytotoxicity towards MTAPdel HCT116 cells, with a CC50 of 28 nM. ERG-IN-5 is valuable for research applications focused on colon cancer, facilitating the exploration of mechanisms related to potassium channel modulation and cancer cell viability. -
Potassium Channel Blocker
Kaliotoxin (1-37) is a calcium-dependent potassium channel blocker derived from the venom of the scorpion Androctonus mauretanicus. This peptide demonstrates potent inhibition of potassium channels, making it a valuable tool for research into neuronal excitability and muscle contraction mechanisms. It is widely utilized in studies exploring ion channel function, neurophysiology, and potential therapeutic applications in cardiac and neurological disorders. -
Potassium Channel
SKF 95601 is a modulator of small conductive Ca2+-activated K+ channels, exhibiting anti-atrial fibrillation (AF) activity. This compound may inhibit atrial fibrillation by influencing the relationship between intracellular Ca2+ concentration and membrane potential. Due to its substantial expression in multiple species, particularly in human atria, SKF 95601 serves as a significant target for research into atrial fibrillation therapeutics. -
Potassium Channel
CM-TPMF is a modulator of the K(Ca)2.1 potassium channel, exhibiting selective activation and inhibition based on its stereochemical structure. This compound serves as both an activator and inhibitor of K(Ca)2.1 channels, making it valuable for investigating their physiological and pathophysiological roles in various biological contexts. CM-TPMF is an essential reagent for research aimed at understanding potassium channel dynamics and their implications in cellular signaling pathways. -
HERG Channel Inhibitor
GPV574 is a potent inhibitor of the HERG potassium channels, with an IC50 value of 5.04 μM. This compound is a derivative of the antiarrhythmic agent propafenone and is employed in research investigating cardiac electrophysiology and drug-induced arrhythmias. Its ability to modulate ion channel activity makes it a valuable tool in the study of heart rhythm disorders. -
Potassium Channel Inhibitor
Stromatoxin 1 is a selective inhibitor of potassium channels, specifically targeting K(V)2.1, K(V)2.2, and K(V)4.2 subunits. This peptide, derived from tarantulas, has been shown to effectively modulate smooth muscle contractions in the urinary bladder by inhibiting the activity of K(V)2.1 and K(V)2.2 channels, while having no effect on K(V)4.2. It serves as a valuable tool for research into bladder physiology and the electrophysiological properties of potassium channels. -
TREK-2 Activator
11-Deoxyprostaglandin F2α is a selective activator of TREK-2 channels, exhibiting an EC50 of 0.294 μM. This compound has been shown to modulate potassium ion conductance, making it valuable in studies of ion channel physiology and neurobiology. Additionally, 11-Deoxyprostaglandin F2α serves as an inhibitor of the K2P channel TREK-1, thereby providing insights into the functional differences between TREK channel subtypes. -
hERG Channels Blocker
E-4031 free base is a selective blocker of the hERG potassium channels, primarily involved in cardiac action potential repolarization. This compound is essential for studying the mechanisms of class III anti-arrhythmic agents and their effects on cardiac rhythm and arrhythmia. Its specificity for hERG channels makes it a valuable tool for investigating the pharmacological profiles of various therapeutic candidates in cardiological research. -
Potassium Channel Agonist
RWJ 29009 is a selective agonist of ATP-sensitive potassium channels. It activates these channels in vascular smooth muscle cells, facilitating potassium efflux and membrane hyperpolarization, resulting in coronary and peripheral vasodilation. This reagent is valuable for investigating cardiovascular diseases, including acute myocardial ischemia and hypertension. -
Kv7.2 Modulator
Kv7.2 Modulator 1 is a selective modulator of Kv7.2 ion channels, primarily involved in regulating neuronal excitability. It exhibits potential antiepileptic activity, making it a valuable tool for epilepsy research. This compound can be utilized to investigate the mechanistic pathways of seizure disorders and assess therapeutic strategies targeting Kv7.2 channels. -
Kv1.3 Blocker
ShK-Dap22 is a highly selective Kv1.3 channel blocker, exhibiting potent immunosuppressive properties with IC50 values of 23 pM for mKv1.3, 1.8 nM for mKv1.1, 10.5 nM for hKv1.6, 37 nM for mKv1.4, and 39 nM for rKv1.2. This polypeptide is primarily utilized in research focused on autoimmune diseases and T cell modulation, enhancing the understanding of Kv1.3's role in immune responses. Its high specificity for Kv1.3 makes it a valuable tool for investigating immune cell function and potential therapeutic pathways. -
Antiarrhythmic Agent
Tedisamil dihydrochloride is an antiarrhythmic agent primarily targeting the transient outward potassium current (I(to)) in cardiac tissue. This compound significantly slows heart rate by inhibiting multiple potassium channels, including IK, K(ATP), and PKA-activated chloride channels, which prolongs the cardiac action potential and QT interval. Tedisamil dihydrochloride is effective in demonstrating antiarrhythmic effects against ventricular arrhythmias and atrial flutter in various animal models, making it a valuable tool for cardiovascular research. -
Maxi-K Channel Modulator
Maxi-K modulator 1 is a modulator of the Maxi-K channel, a large conductance calcium-activated potassium channel. This compound exerts a significant stimulatory effect on Maxi-K channel activity, promoting potassium efflux. Maxi-K modulator 1 is particularly useful in research related to fragile X syndrome and other neurological disorders involving channelopathies. -
Kv1.3 Blocker
Nalanthalide is a selective blocker of the voltage-gated potassium channel Kv1.3, exhibiting an IC50 of 3.9 µM. It demonstrates potential as an immunosuppressant, making it valuable in the study of inflammatory immune diseases. This compound is particularly relevant for research involving neuroinflammation and related pathologies. -
hERG Channel Inhibitor
5-O-Desmethyl donepezil is a metabolite of Donepezil that functions as an inhibitor of the hERG potassium channel with an IC50 of 1.5 μM. This compound is particularly relevant for studies examining cardiac ion channel activity and drug interactions affecting cardiac repolarization. Its potential applications include assessing safety profiles for drug candidates in pharmacological research. -
Potassium Channel Blocker
AM 92016 is a potent potassium channel blocker that modulates ion flow, thereby increasing the duration of action potentials in isolated ventricular cells from guinea pigs and rabbits. This compound has been shown to exhibit proarrhythmic activity in guinea pigs and pigs, making it a valuable tool for studying cardiac electrophysiology and potential arrhythmogenic effects. It is suitable for research applications focused on cardiac function and the behavior of ion channels in the heart. -
Kv1.5. Potassium Channel Inhibitor
RH01617 is a selective inhibitor of the Kv1.5 potassium channel, known to modulate cardiac repolarization. This compound exhibits potential for research applications related to atrial fibrillation and other cardiovascular disorders. Additionally, RH01617 also functions as an MMP-13 inhibitor, suggesting a broader scope of biological activity in tissue remodeling processes. -
Potassium Channel Activator
Dihydroisopimaric acid is a potent activator of large conductance calcium-activated potassium (BK) channels, specifically targeting the BKαβ1 subunit. This compound has been demonstrated to effectively enhance the opening of BK channels under whole-cell voltage clamp conditions. Its key biological activity makes it a valuable tool for investigating the role of potassium channels in various physiological processes and in the study of cardiovascular and neurological disorders.
