Catalog No.
Product Name
Application
Product Information
Citations
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Kir4.1 Blocker
VU0134992 hydrochloride is a selective blocker of the Kir4.1 potassium channel, exhibiting an IC50 of 0.97 µM. This compound demonstrates a nine-fold selectivity for homomeric Kir4.1 channels compared to Kir4.1/5.1 concatemeric channels, with an IC50 of 9 µM at -120 mV. Its unique profile makes it a valuable tool for investigating the physiological roles of Kir4.1 channels in various biological processes and potential therapeutic applications. -
KATP Channel Opener
Tifenazoxide (NN414) is a potent, orally active opener of KATP channels, specifically targeting the SUR1/Kir6.2 subunits. This compound demonstrates antidiabetic properties by inhibiting glucose-stimulated insulin release both in vitro and in vivo, thereby contributing to enhanced glucose homeostasis. Tifenazoxide is valuable for research applications focused on diabetes and metabolic disorders. -
PKG Activator
Dibutyryl-cGMP sodium is a cell-permeable analogue of cyclic guanosine monophosphate (cGMP) that primarily activates cGMP-dependent protein kinase (PKG). This compound has been shown to inhibit the release of [3H]-arachidonic acid from γ-thrombin-stimulated human platelets, demonstrating its role in modulating platelet activity. Additionally, Dibutyryl-cGMP sodium induces peripheral antinociception through the activation of ATP-sensitive potassium channels, making it a valuable tool for research in pain modulation and cardiovascular physiology. -
TASK-3 Agonist/TWIK2 Blocker
NPBA is a potassium K2P channel TASK-3 (KCNK9) agonist and TWIK2 (KCNK1) channel blocker. This compound plays a crucial role in inhibiting NLRP3 inflammasome activation in macrophages, making it valuable for research into inflammatory pathways and potassium channel function. Its unique mechanism provides insights into potential therapeutic applications in inflammatory diseases. -
SK2/3 Positive Modulator
CyPPA is a positive modulator of human small conductance potassium channels hSK2 and hSK3, exhibiting EC50 values of 14 μM and 5.6 μM, respectively. This compound does not activate hSK1 or hIK channels, making it selective for its target. CyPPA is utilized in research to investigate the physiological roles and therapeutic potential of small conductance potassium channels in various biological processes. -
Sodium Current Inhibitor
Eleclazine hydrochloride is a selective inhibitor of the cardiac late sodium current, exhibiting an IC50 value of less than 1 μM, along with a weaker inhibitory effect on potassium current (IC50 approximately 14.2 μM). This compound demonstrates therapeutic potential by providing protection against autonomically induced atrial premature beats, repolarization alternans, heterogeneity, and atrial fibrillation in porcine models. Eleclazine hydrochloride is applicable in the study of cardiac arrhythmias and their underlying mechanisms. -
TREK1/2 Channels Opener
GI-530159 is a selective opener of TREK1 and TREK2 potassium channels, exhibiting an EC50 of 0.76 μM for TREK1. This compound demonstrates a significant ability to reduce excitability in rat dorsal root ganglion neurons, indicating potential analgesic effects. GI-530159 is valuable for research applications focused on pain modulation and the physiological roles of TREK channels in neuronal activity. -
Antiarrhythmic Agent
Flecainide hydrochloride is a potent antiarrhythmic agent that primarily targets sodium channels in cardiac tissues. By inhibiting the release of calcium ions mediated by the cardiac ryanodine receptor (RyR2), it effectively stabilizes cardiac membrane excitability. This compound is utilized in research studies focusing on cardiac arrhythmias, including catecholaminergic polymorphic ventricular tachycardia (CPVT) and other related cardiovascular diseases. -
Sodium Channel Inhibitor
Ropivacaine hydrochloride monohydrate is a potent sodium channel inhibitor that reversibly blocks sodium ion influx, thereby disrupting impulse conduction in nerve fibers. Additionally, it inhibits the K2P potassium channel TREK-1 with an IC50 of 402.7 μM in COS-7 cell membranes. This compound is widely utilized for regional anesthesia and in the management of neuropathic pain in vivo, making it a valuable reagent in pain research and therapeutic applications. -
Kv7 Potassium Channels Opener
ICA-105665 is a potent opener of neuronal Kv7.2/7.3 and Kv7.3/7.5 potassium channels. It effectively enhances potassium ion flow, making it relevant for research in neurological disorders, particularly in the context of seizure activity. Additionally, ICA-105665 inhibits liver mitochondrial function and bile salt export protein (BSEP) transport with an IC50 of 311 μM, positioning it as a valuable tool for studying both central nervous system and hepatic physiological processes. Its ability to penetrate the blood-brain barrier further supports its utility in investigating antiseizure mechanisms. -
K(v)7 Channels Modulator
QO 58 is a potent modulator of K(v)7 channels, specifically enhancing current amplitudes and shifting the voltage-dependent activation curve in a more negative direction. Additionally, it effectively slows the deactivation of K(v)7.2/K(v)7.3 currents. This compound is valuable for studying diseases linked to neuronal hyperexcitability, providing insights for potential therapeutic applications. -
Potassium Channel Modulator
Flindokalner is a potassium channel modulator that positively influences all neuronal Kv7 channel subtypes expressed in HEK293 cells, alongside acting as a positive modulator of large conductance calcium-activated potassium channels (BKca). It exhibits negative modulatory activity at Kv7.1 channels with a Ki of 3.7 μM and also negatively modulates GABAA receptors. In vivo studies demonstrate its anxiolytic efficacy, making it a valuable reagent for research in neuropharmacology and the study of ion channel function. -
Potassium Channel Opener
Cromakalim functions as a potassium channel opener, facilitating relaxation of smooth muscle tissue. It exhibits bronchodilator activity in asthma by inhibiting the spontaneous tone of human isolated bronchi in a concentration-dependent manner. Its effectiveness is comparable to that of isoprenaline or theophylline, making it a valuable tool for research in respiratory physiology and pharmacology. -
KCNQ2 Inhibitor
ML252 is a selective inhibitor of the KCNQ2 (Kv7.2) ion channel, exhibiting an IC50 of 69 nM for KCNQ2, along with lower inhibitory effects on KCNQ1, KCNQ2/Q3, and KCNQ4. This compound also demonstrates inhibition of key Cytochrome P450 enzymes, including CYP1A2, CYP2C9, CYP3A4, and CYP2D6, with IC50 values ranging from 3.9 nM to 19.9 nM. ML252 is notable for its ability to penetrate the blood-brain barrier, making it a valuable tool for investigating neuronal function and related disorders. -
TREK Activator
ONO-2920632 is an orally active TREK activator that effectively penetrates the central nervous system, exhibiting EC50 values of 0.3 µM for TREK-1 and 2.8 µM for TREK-2. This compound demonstrates significant selectivity for TREK channels over other K2P channels, showing more than 91-fold selectivity versus TASK1, TASK2, TASK3, TRAAK, and TWIK2, as well as 31-fold selectivity for TRESK. ONO-2920632 is recognized for its analgesic properties and is suitable for research applications in pain management, migraine, and various neurological disorders. -
Antiarrhythmic Agent
Nifekalant hydrochloride is a class III antiarrhythmic agent that primarily targets the IKr potassium channel, demonstrating an inhibitory concentration (IC50) of 10 µM. This compound is utilized in research to investigate refractory ventricular tachyarrhythmias, providing a valuable tool for studying cardiac rhythm management and potential therapeutic interventions. -
BK Channel Antagonist
Penitrem A is an indole diterpene alkaloid that selectively antagonizes large-conductance calcium-activated potassium (BK) channels. This compound exhibits notable antiproliferative and anti-invasive properties across various cancer types. Additionally, Penitrem A enhances the spontaneous release of neurotransmitters such as glutamate, gamma-aminobutyric acid (GABA), and aspartate from cerebrocortical synaptosomes, leading to tremorgenic effects in animal models. Its unique mechanism makes it a valuable tool for studying neuronal signaling and cancer research. -
hERG1/IKr/Ito Activator
NS3623 is an activator of the human ether-a-go-go-related gene (hERG1/KV11.1) potassium channels. It enhances the IKr and Ito currents, exhibiting significant antiarrhythmic properties. Notably, NS3623 operates through a dual mechanism, acting as an inhibitor of hERG1 channels as well, making it valuable for research in cardiac electrophysiology and arrhythmia treatment strategies. -
SK Channel Blocker
UCL 1684 dibromide is a potent, non-peptidic blocker of small conductance calcium-activated potassium (SK) channels, exhibiting nanomolar potency. This compound demonstrates significant atrial-selective inhibition of sodium current (INa), effectively preventing the onset of atrial fibrillation. In addition, UCL 1684 dibromide induces atrial-selective prolongation of the effective refractory period (ERP) by promoting postrepolarization refractoriness, making it a valuable tool for researching cardiac electrophysiology and arrhythmogenesis. -
KCC2 Blocker
KCC2 Blocker 1 is a selective inhibitor of the K+-Cl- cotransporter KCC2, exhibiting an IC50 value of 1 μM. This compound, classified as a benzyl prolinate, has been utilized in research to investigate the functional roles of KCC2 in cellular processes and neuronal signaling. Its ability to modulate ion transport mechanisms makes it a valuable tool for studying pathophysiological conditions associated with KCC2 dysregulation. -
Stable Isotope
Ropivacaine-d7 is a deuterium-labeled derivative of Ropivacaine, a potent sodium channel blocker. It works by reversibly inhibiting sodium ion influx, thereby blocking impulse conduction in nerve fibers. Additionally, Ropivacaine acts as an inhibitor of the K2P (two-pore domain potassium channel) TREK-1, exhibiting an IC50 of 402.7 μM in COS-7 cell membranes. This reagent is primarily used in studies focused on the management of neuropathic pain. -
Insulin Secretagogue
Repaglinide-d5 is a deuterium-labeled form of Repaglinide, an insulin secretagogue that stimulates insulin secretion from pancreatic beta cells. This compound is primarily utilized in the research of type 2 diabetes mellitus to better understand mechanisms of insulin regulation and glucose homeostasis. Its unique labeling facilitates pharmacokinetic studies and metabolic tracing in various biological assays. -
TASK-3 Blocker
PK-THPP is a selective blocker of the TASK-3 potassium ion channel (K2P9.1), exhibiting IC50 values of 35 nM for TASK-3 and 300 nM for TASK-1. This compound demonstrates minimal activity against other potassium channels, making it a valuable tool for investigating specific ion channel functions. PK-THPP is recognized for its efficacy as a breathing stimulant and is useful for research into various breathing disorders and related physiological studies. -
Kir6.2/SUR1 Activator
VU0071063 is a selective activator of the Kir6.2/SUR1 potassium channel complex, exhibiting an EC50 of 7.44 μM. This compound is primarily used to study the physiological roles of Kir6.2/SUR1 in pancreatic and neuronal tissues. VU0071063 promotes hyperpolarization of β-cell membrane potential, effectively inhibiting insulin secretion. The compound’s chemotype demonstrates a pronounced structure-activity relationship, making it a valuable tool for exploring insulin signaling and regulatory mechanisms in cellular physiology. -
KATP Channel Blocker
Clamikalant sodium is a selective ATP-sensitive potassium (KATP) channel blocker. This compound has demonstrated significant effects in cardiac research, particularly in the study of arrhythmias. Clamikalant sodium is useful for investigating the mechanisms of excitability and potential therapeutic targets in heart rhythm disorders. -
KCNT1 channel blocker
CPK20 is a potent and highly selective blocker of the KCNT1 ion channel. It is primarily utilized in research pertaining to epilepsy, offering valuable insights into the modulation of excitability associated with KCNT1 activity. This compound serves as an essential tool for investigating therapeutic approaches to channelopathies and related neurological disorders. -
Potassium Channel Inhibitor
Psora-4 is a potent and selective inhibitor of Kv1.3 (voltage-gated potassium channels) with an EC50 of 3 nM. This compound exhibits significant immunosuppressive activity, effectively inhibiting the proliferation of human and rat myelin-specific effector memory T cells in vitro. Its specificity for Kv1.3 makes it a valuable tool for studying autoimmune disorders and T cell-mediated responses in research applications. -
KCNQ2 Activator
HN37 is a potent activator of the KCNQ2 potassium channel, exhibiting an EC50 of 37 nM. This compound serves as a promising candidate in the development of antiepileptic therapies. Additionally, HN37 contains an alkyne group, allowing it to undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, enabling versatile applications in chemical biology and drug discovery. -
KATP Channel Inhibitor
Cibenzoline is a KATP channel inhibitor targeting the pore-forming subunit Kir6.2, exhibiting an IC50 of 22.2 μM. This compound also inhibits cardiac ion currents IKr and IKs, with IC50 values of 8.8 μM and 12.3 μM, respectively. Cibenzoline is primarily utilized in the investigation of cardiac diseases, and it has been shown to induce hypoglycemia, making it relevant for studies related to glucose metabolism and endocrine functions. -
K(ATP) Channel Antagonist
Mitiglinide calcium hydrate is an ATP-sensitive K+ (KATP) channel antagonist specifically targeting the Kir6.2/SUR1 complex in pancreatic beta cells. This compound functions as an insulinotropic agent, stimulating insulin secretion in response to glucose levels. Mitiglinide calcium hydrate is primarily utilized in research focused on type 2 diabetes and offers insights into the regulation of insulin release. -
SLO3 Inhibitor
VU0546110 is a selective inhibitor of the sperm-specific potassium channel SLO3, exhibiting an IC50 of 1.287 μM for SLO3 in HEK293 cells and a more modest IC50 of 59.80 μM for SLO1. This compound effectively blocks both heterologous SLO3 currents and endogenous K+ currents in human sperm, leading to the cessation of sperm hyperpolarization, acrosome reaction induction, and hyper-activated motility. VU0546110 is of particular interest in reproductive biology research due to its potential contraceptive applications. -
Potassium Channel Inhibitor
N-Acetylprocainamide is a potassium channel inhibitor that functions as a class III antiarrhythmic agent. By blocking K+ channels, it effectively modulates cardiac action potentials, making it relevant in the study of arrhythmias. This compound serves as a valuable tool in cardiac electrophysiology research and associated therapeutic investigations. -
Kir6.1/SUR2B KATP channel inhibitor
VU0542270 is a selective inhibitor of the vascular Kir6.1/SUR2B KATP channel, demonstrating an IC50 value of 100 nM. It exhibits minimal activity against other members of the Kir channel family, with an IC50 greater than 30 μM for nine variants. This compound is valuable for investigating the role of KATP channels in cardiovascular disease and exploring potential therapeutic strategies. -
KATP Channels Blocker
PNU 37883 hydrochloride is a selective blocker of ATP-sensitive potassium (KATP) channels, specifically targeting the Kir6 subunit. This compound exerts diuretic effects through its selective binding in renal tissue and vascular smooth muscle, while exhibiting minimal interaction with brain or pancreatic beta cells. PNU 37883 hydrochloride is useful for research applications related to cardiovascular physiology and renal function studies. -
BK Channels Activator
Isopropyl unoprostone is a potent activator of large conductance Ca2+-activated K+ (BK) channels. This analogue of a prostaglandin metabolite demonstrates significant biological activity by lowering intraocular pressure (IOP) through enhanced aqueous humor outflow, making it relevant for antiglaucoma research. Additionally, isopropyl unoprostone has been shown to improve retinal sensitivity and provide protective effects on central retinal sensitivity, highlighting its potential in ocular health studies. -
Antipsychotic Agent
Mesoridazine is an orally active phenothiazine antipsychotic agent that primarily targets the human ether-a-go-go related gene (hERG) channels. It functions as a potent and rapid open-channel blocker, inhibiting hERG currents with an IC50 of 550 nM in human embryonic kidney 293 cells. Mesoridazine is utilized in research focused on schizophrenia and various other psychiatric disorders, making it a valuable reagent for studies in psychopharmacology. -
K(ATP) Channel Blocker
Glisoxepide is a sulphonamide derivative that functions as a nonselective K(ATP) channel blocker. It exhibits significant antihyperglycemic activity, making it effective in the management of diabetes. Additionally, Glisoxepide plays a role in cardiovascular regulation, providing insights into potential therapeutic applications in metabolic and cardiovascular disorders. -
TREK-1 Inhibitor
PE 22-28 is a potent TREK-1 inhibitor with an IC50 value of 0.12 nM, demonstrating its efficacy in modulating TREK-1 activity. This 7-amino-acid peptide serves as a core sequence for generating analogs through chemical modifications or amino acid substitutions. PE 22-28 is relevant for research into depression, offering insights into the role of TREK-1 in mood regulation and potential therapeutic interventions. -
KCNQ2/3 Activator
RL648_81 is a selective activator of the KQT-like subfamily 2/3 (KCNQ2/3) channels, exhibiting an EC50 of 190 nM. This compound effectively induces a hyperpolarizing shift in V1/2 for KCNQ2/3, while showing no effect on KCNQ4 or KCNQ5 channels. RL648_81 holds promise for research involving neurological disorders linked to neuronal hyperexcitability. -
TASK-1 Inhibitor
AVE1231 is a selective inhibitor of the two-pore potassium channel TASK-1, effectively blocking carbamoylcholine chloride-activated IKACh with an IC50 of 8.4 μM. This compound plays a crucial role in the study of electrophysiological processes, making it valuable for research focused on cardiac arrhythmias and atrial fibrillation. Its ability to modulate potassium ion currents offers insights into the mechanisms underlying these cardiovascular conditions. -
Potassium Channel Activator
Isopimaric acid is a potent activator of large conductance calcium-activated potassium (BK) channels. This compound facilitates the opening of BK channels, leading to increased ion conductance and cellular hyperpolarization. Isopimaric acid is valuable in research applications exploring cardiovascular function, neuronal excitability, and muscle physiology. Its ability to modulate potassium channels makes it a useful tool for studying various physiological processes and drug discovery. -
IKur Current Blocker
BMS-919373 is a selective and potent inhibitor of the IKur potassium current. This compound has demonstrated significant biological activity in the modulation of cardiac action potentials and repolarization. BMS-919373 is primarily utilized in cardiovascular disease research, providing insights into arrhythmias and other related cardiac conditions. -
Kir4.1/5.1 Inhibitor
VU6036720 is a selective inhibitor of Kir4.1/5.1 channels, exhibiting potent in vitro activity with an IC50 of 0.24 μM. This compound is valuable for investigating the physiological roles of Kir4.1/5.1 in both brain and kidney tissues. Its specificity makes it an essential tool for studies focused on ion channel modulation in neurological and renal research. -
TRESK/TASK-1 Inhibitor
A2793 is a selective inhibitor of the TWIK-related acid-sensitive K+ channels, TASK-1 and TRESK. With an IC50 of 6.8 μM for mTRESK, this reagent demonstrates significant activity against TRESK while exhibiting only moderate effects on TREK-1 and TALK-1. A2793 is valuable for research applications focusing on ion channel regulation and neurological studies. -
TRESK Inhibitor
A2764 dihydrochloride is a potent and selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1), exhibiting moderate inhibitory effects on TREK-1 and TALK-1 channels. This compound demonstrates increased sensitivity to activated mTRESK channels, with an IC50 value of 6.8 μM. A2764 dihydrochloride effectively induces cell depolarization and enhances excitability in native cells, making it a valuable tool for investigating the role of TRESK channels in migraine pathophysiology and nociceptive signaling. -
TRAAK Inhibitor
RU-TRAAK-2 is a selective inhibitor of the TRAAK (TWIK-related arachidonic acid-stimulated K+ channel) that demonstrates complete reversibility in its inhibitory action. It shows no activity against other potassium channels, including Kv1.2, Slo1, and GIRK2, ensuring specificity in experimental applications. Additionally, RU-TRAAK-2 features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it a valuable tool in chemical biology for labeling and tagging biomolecules. This compound is primarily utilized in research focusing on ion channel regulation and signaling pathways. -
Stable Isotope
Nicorandil-d4 is the deuterium-labeled analog of Nicorandil, a potent activator of potassium channels, specifically targeting vascular nucleoside diphosphate-dependent K+ channels and cardiac ATP-sensitive K+ channels (KATP). This compound exhibits significant vasodilatory and cardioprotective effects, making it relevant for research in angina and ischemic heart diseases. Nicorandil-d4 serves as a valuable stable isotope for metabolism studies and pharmacokinetic investigations in cardiovascular research. -
GIRK Activator
VU0810464 is a potent and selective activator of G protein-gated inwardly rectifying potassium channels (GIRK, Kir3). It demonstrates nanomolar potency for neuronal GIRK channels (EC50=165 nM) and GIRK1/4 channels (EC50=720 nM), facilitating efficient modulation of neuronal excitability. The compound is particularly noteworthy for its enhanced brain penetration, making it a valuable tool for research focused on neuronal signaling and disorders involving GIRK channel dysfunction. -
Kv Channels Allosteric Modulator
LUF7244 is a selective allosteric modulator of Kv11.1 channels, acting by inhibiting early afterdepolarizations. This compound is valuable for anti-arrhythmia research, providing insights into the modulation of cardiac activity and potential therapeutic interventions for arrhythmias. Its specificity for Kv11.1 channels makes it an essential tool for studying ion channel regulation in cardiology. -
Potassium Channel activator
NS004 is a potent activator of large-conductance calcium-activated potassium (BK) channels, enhancing Iberiotoxin and Tetraethylammonium-sensitive whole-cell efflux currents. This compound significantly boosts the activity of individual BK channels in GH3 cells and rat brain channels integrated into planar lipid bilayers. The observed effects include increased channel mean open time, reduced intermittent time, and enhanced voltage and calcium sensitivity, making NS004 valuable for research on potassium channel modulation and related physiological processes.
