Catalog No.
Product Name
Application
Product Information
Citations
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Potassium Channel Agonist
SR 47063 is an ATP-sensitive potassium channel (KATP) agonist that selectively activates KATP channels in vascular smooth muscle cells, exhibiting an IC50 of 8.1 nM in human saphenous vein and 3.86 nM in rat aorta. By promoting potassium efflux and inducing cellular hyperpolarization, SR 47063 facilitates vasorelaxation. This compound is valuable for research into hypertension and associated cardiovascular disorders. -
Antiarrhythmic Agent
Dofetilide N-oxide is a metabolite of the class III antiarrhythmic agent Dofetilide, primarily targeting potassium channels. Its mechanism involves the inhibition of potassium ion movement, which plays a crucial role in the regulation of cardiac action potentials. This compound is utilized in research to study cardiac arrhythmias and the therapeutic potential of potassium channel blockers in managing cardiovascular diseases. -
TREK-1 Inhibitor
TWIK-1/TREK-1-IN-1 is an inhibitor of the TREK-1 potassium channel, a member of the two-pore domain potassium channel family. By targeting both TREK-1 homodimers and TWIK-1/TREK-1 heterodimers, it exhibits IC50 values of 9.36 μM and 14.6 μM, respectively. This compound is significant for research into antidepressant mechanisms, demonstrating potential antidepressant-like effects that warrant further investigation in neuropharmacology. -
Potassium Channel Inhibitor
L-691121 is a potent potassium channel inhibitor that demonstrates antiarrhythmic efficacy by blocking potassium channels, leading to a prolonged cardiac action potential. This compound is orally bioavailable and has been shown to induce embryotoxicity, with fetal mortality noted at a dosage of 0.8 mg/kg/day. Its biological activity makes L-691121 a valuable tool in the study of cardiac function and developmental toxicity. -
Nav1.8 Inhibitor
Nav1.8-IN-7 is a selective inhibitor of the Nav1.8 ion channel, demonstrating over 50% inhibition at a concentration of 100 nM. This compound selectively targets Nav1.8 while exhibiting an IC50 for hERG of 15.6 μM. Nav1.8-IN-7 is particularly relevant for research in pain mechanisms and the development of analgesic therapies. -
Potassium Channel Blocker
Chlorahololide D is a selective potassium channel blocker with an IC50 value of 2.7 μM. Derived from the whole plant of Chloranthus holostegius, this natural product exhibits significant biological activity in modulating potassium ion flow. It is valuable for research applications investigating ion channel physiology and the pharmacological modulation of excitability in various cell types. -
Potassium Channel
NS4591 is a modulator of calcium-activated potassium channels, specifically enhancing the activity of small conductance (SK) and intermediate conductance (IK) potassium channels. It significantly increases IK-mediated currents at approximately 45 nM and SK3-mediated currents at about 530 nM in whole-cell patch-clamp studies. NS4591 has been shown to inhibit action potentials induced by suprathreshold depolarizing pulses in acutely isolated bladder primary afferent neurons and reduces carbamylcholine-induced detrusor contraction in the rat bladder, indicating its sensitivity to apamin. This reagent is useful for studying the physiological roles of potassium channels in bladder function and neuronal excitability. -
Kv1.5 Potassium Channel Inhibitor
DDO-02001 is a moderately potent inhibitor of the Kv1.5 potassium channel, exhibiting an IC50 value of 17.7 μM. This compound is utilized in research focused on understanding anti-arrhythmic mechanisms and the modulation of cardiac excitability. Its selective inhibition of Kv1.5 channels positions DDO-02001 as a valuable tool in the study of cardiac arrhythmias and related therapeutic interventions. -
Potassium Channel Inhibitor
Meglitinide is an ATP-sensitive potassium (KATP) channel inhibitor that selectively targets the SUR1, SUR2A, and SUR2B subunits. It exhibits IC50 values of 0.26 μM, 0.53 μM, and 1.6 μM for these channels, respectively, and demonstrates strong binding affinity with Kd values of 7 μM for SUR1 and SUR2A, and 8 μM for SUR2B. Meglitinide effectively closes KATP channels by binding to a shared site across all SUR subtypes, maintaining its efficacy even with the SUR1 S1237Y mutation. This compound is valuable for research applications centered on type 2 diabetes and the modulation of insulin secretion. -
Potassium Channel
ZD0947 is an ATP-sensitive potassium channel activator that primarily targets smooth muscle KATP channels (SUR2B/Kir6.1 and SUR2B/Kir6.2). It is known to partially antagonize pancreatic KATP channels (SUR1/Kir6.2) and cardiac KATP channels (SUR2A/Kir6.2). This compound shows potential for research applications in inhibiting overactive bladder (OAB) and exploring potassium channel functions in various physiological and pathological processes. -
Peptidyl Inhibitor
Kaliotoxin is a peptidyl inhibitor that targets neuronal BK-Type channels. It specifically inhibits voltage-gated (Kv) channels and calcium-activated potassium channels, making it a valuable tool for studying the regulation of membrane potential and neuronal excitability. This compound is particularly useful in research exploring the mechanisms underlying neuronal signaling and potential therapeutic interventions in neurological disorders. -
Kv7.2/Kv7.3 Modulator
Kv7.2/Kv7.3 modulator-1 is an effective modulator of the Kv7.2 and Kv7.3 potassium channels, exhibiting a pEC50 of 7.96 for channel opening activity. This reagent plays a critical role in studying neurological conditions, including epilepsy, depression, brain injury, and pain mechanisms. Its ability to selectively influence these ion channels offers valuable insights into potential therapeutic strategies in the treatment of various neuropsychological disorders. -
Kv7 Potassium Activator
Kv7 activator-2 is a selective activator of Kv7 potassium channels. It enhances neuronal excitability and has demonstrated potential in the study of neurological disorders, especially epilepsy. This compound serves as a valuable tool for investigating the modulation of neuronal signaling and the therapeutic strategies targeting Kv7 channels in various neurological conditions. -
ROMK Inhibitor
ROMK-IN-32 is a selective inhibitor of the renal outer medullary potassium channel (ROMK), exhibiting an IC50 value of 35 nM. In addition to its primary activity, ROMK-IN-32 demonstrates inhibition of the hERG channel with an IC50 of 22 μM. This compound is valuable for research applications investigating potassium ion channel regulation, renal physiology, and potential implications in cardiac safety assessments. -
KCNQ2 Activator
QO-83 is a potent activator of the KCNQ2 (Kv7.2) voltage-gated potassium channel, exhibiting an EC50 of 0.56 μM. It binds to a specific hydrophobic pocket within the KCNQ2-CaM complex in its closed conformation, resulting in a negative shift in the voltage-dependent activation curve. This mechanism enhances the voltage sensitivity of KCNQ2 channels. QO-83 is a valuable tool for research into the mechanisms underlying epilepsy and related ion channel disorders. -
Potassium Channel Blocker
δ-Dendrotoxin is a potent potassium channel blocker derived from the venom of the black mamba snake. This compound is utilized in research focused on neurological diseases, aiding in the understanding of ion channel function and its implications in neuronal excitability. Its ability to modulate potassium channels makes it a valuable tool for investigating potential therapeutic targets in various neurological disorders. -
Potassium Channel Blocker
WAY-123223 is an orally active blocker of potassium channels, specifically targeting cardiac ion currents. This compound prolongs transmembrane action potential duration and the cardiac refractory period in canine Purkinje fibers, enhancing the ventricular fibrillation threshold and facilitating the restoration of sinus rhythm from ventricular fibrillation. WAY-123223 is valuable for researching cardiovascular diseases, particularly in the study of arrhythmias and their treatment. -
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. -
HCN2 Inhibitor
HCN2 modulator-5 is a selective inhibitor of the HCN2 ion channel. This compound effectively reduces HCN2 channel activity, making it a valuable tool for investigating mechanisms underlying pain, inflammatory conditions, neuropathic pain, and tinnitus. Additionally, HCN2 modulator-5 can contribute to research focused on central nervous system and psychiatric disorders, including mood disorders. -
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.
