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Catalog No.
Product Name
Application
Product Information
Citations
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Kv1.3 Inhibitor
Dalazatide is a potent inhibitor of the Kv1.3 potassium channel, specifically designed for research applications in autoimmune diseases. This peptide has shown efficacy in the modulation of immune responses, making it a valuable tool for studying conditions such as multiple sclerosis, lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes, and inflammatory bowel disease. Its role in Kv1.3 inhibition provides insights into the pathophysiology of these diseases and potential therapeutic avenues. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
TREK-1 Inhibitor
TKIM is a selective inhibitor of the TREK-1 channel, exhibiting an IC50 of 2.96 μM. By binding to the pocket of the intermediate (IM) state of TREK-1, TKIM modulates ion channel activity. This compound is valuable for investigations into the physiological roles of TREK-1 in neurobiology and cardiovascular research, as well as potential therapeutic applications in pain and mood disorders. -
KV1.3 Inhibitor
KV1.3-IN-1 is a selective inhibitor of the KV1.3 potassium channel, exhibiting IC50 values of 230 nM in Ltk cells and 26.12 nM in PHA-activated T-lymphocytes. This compound disrupts intracellular Ca2+ signaling, leading to notable inhibition of T-cell activation, proliferation, and colony formation. KV1.3-IN-1 is an essential tool for research on T-cell biology and the modulation of immune responses. -
TREK Inhibitor
ONO-TR-772 is a selective TREK inhibitor with an IC50 value of 15 nM. This compound has been shown to enhance recognition memory in the MK-801-stimulated novel object recognition (NOR) mouse model. ONO-TR-772 is valuable in research pertaining to cognitive impairment and related neurological diseases. -
Potassium Channel Inhibitor
VU625 is a selective inhibitor of the inward rectifier potassium channel 1 (AeKir) in the Aedes aegypti mosquito, exhibiting an IC50 of 96.8 nM in HEK293 cells. This compound demonstrates potential for development as a novel insecticide, targeting critical pathways in mosquito physiology. Its specificity for AeKir makes it a valuable tool for research aimed at controlling mosquito populations and studying potassium channel function. -
KV1.3 Inhibitor
cis-KV1.3-IN-1 is a selective inhibitor of the KV1.3 potassium channel, specifically designed to target this ion channel in cellular systems. At a concentration of 10 μM, cis-KV1.3-IN-1 demonstrates a 25.53% inhibition of KV1.3 activity in Xenopus oocytes expressing human hKV1.3. This compound is valuable for research into immunological responses and therapies, particularly in relation to autoimmune diseases where KV1.3 channels play a critical role. -
Potassium Channel Inhibitor
Charybdotoxin is a 37-amino acid peptide that selectively inhibits potassium channels. Its primary mechanism involves blocking voltage-gated K+ channels, leading to altered neuronal excitability and muscle contraction. This compound is useful in research applications focused on neurophysiology, cardiac function, and ion channel studies, providing insights into the role of potassium channels in physiological and pathological processes. -
ROMK Inhibitor
MK-8153 is a highly selective and orally active inhibitor of the renal outer medullary potassium channel (ROMK), demonstrating an IC50 of 5 nM for ROMK electrophysiology. This compound's potent inhibitory action makes it suitable for research applications related to diuresis and atriuresis. Its specificity towards ROMK provides a valuable tool for studying renal function and potassium homeostasis in various biological contexts. -
Potassium Channel Inhibitor
Guanfu base G is a potassium channel inhibitor derived from Aconitum coreanum. It effectively inhibits the HERG channel current, exhibiting an IC50 value of 17.9 μM. This compound is primarily utilized in research applications focused on cardiac arrhythmias and the modulation of ion channel activity. -
Potassium Channel Inhibitor
Allocryptopine is a potassium channel inhibitor, specifically targeting the human ether-a-go-go related gene (hERG) current. Derived from the plant Macleaya cordata, Allocryptopine exhibits antiarrhythmic properties that may be beneficial in cardiovascular research. Its ability to effectively block hERG channels positions it as a valuable reagent for studies investigating cardiac ion channel modulation and related disorders. -
KCa2 Channel Inhibitor
AP14145 hydrochloride is a selective negative allosteric modulator of KCa2 channels, exhibiting an IC50 of 1.1 μM for both KCa2.2 (SK2) and KCa2.3 (SK3) channels. Its inhibitory action is significantly influenced by specific amino acids S508 and A533 within the channel structure. In preclinical models, AP14145 hydrochloride has been shown to prolong the atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic properties in a Vernakalant-resistant porcine model of atrial fibrillation, making it a valuable tool for studying cardiac electrophysiology and arrhythmia mechanisms. -
TASK-1 Inhibitor
TASK-1-IN-1 is a potent and selective inhibitor of the TASK-1 potassium channel, exhibiting an IC50 of 148 nM. It demonstrates reduced inhibition of the TASK-3 channel with an IC50 of 1750 nM and minimal impact on other K+ channels. This compound is primarily used in cancer research, exhibiting potential anticancer properties through modulation of potassium ion currents. -
Kv1.5 Inhibitor
MK-0448 is a selective inhibitor of the voltage-gated potassium channel Kv1.5. It demonstrates significant biological activity by modulating ion channel activity, which is vital in the study of cardiac electrophysiology. This compound is primarily utilized in research examining atrial fibrillation and other related cardiac arrhythmias. -
Potassium Channel Inhibitor
Phrixotoxin-1 is a selective peptide inhibitor targeting the Kv4 potassium channel. Derived from the venom of the theraphosid spider Phrixotrichus auratus, it exhibits potent biological activity in the modulation of potassium ion flow. This reagent is valuable for research applications involving neuronal excitability and cardiac function, providing insight into the roles of Kv4 channels in various physiological and pathological processes. -
Kv11.1 Inhibitor
LUF7346 is a potent inhibitor of the Kv11.1 (hERG) channel, acting as a negative allosteric modulator with an IC50 value of 35.6 ± 3.2 nM. This compound can be utilized in research focused on cardiac ion channel function, arrhythmias, and drug-induced QT interval prolongation. Its specificity makes it a valuable tool for investigating hERG channel-related therapeutic interventions and understanding associated physiological effects. -
Potassium Channel Inhibitor
Spinoxin is a 34-residue peptide neurotoxin derived from the venom of the scorpion Heterometrus spinifer and is classified as a Kv1.3 potassium channel inhibitor. With an IC50 of 63 nM, Spinoxin exhibits strong potency in inhibiting Kv1.3, making it a valuable tool in research related to autoimmune disorders and cancer therapies. Its unique structure, stabilized by four disulfide bridges, enhances its relevance in exploring the role of potassium channels in various biological processes. -
Potassium Channel Inhibitor
4-trans-Hydroxy-glibenclamide is a potent inhibitor of the SUR1/Kir6.2 potassium channels. As an active metabolite of the sulfonylurea inhibitor glyburide, it effectively disrupts glyburide binding to rat brain synaptosomes, exhibiting IC50 values of 0.95 nM and 100 nM at high and low affinity sites, respectively. This compound is valuable for research applications focused on investigating the physiological and pharmacological roles of potassium channels in cellular processes and metabolic disorders. -
Kv1.5 Potassium Channel Inhibitor
DDO-02005 is a potent inhibitor of the Kv1.5 potassium channel, exhibiting an IC50 value of 0.72 μM. This compound demonstrates notable anti-atrial fibrillation effects in a CaCl2-ACh-induced AF rat model and showcases effective anti-arrhythmic activity against aconitine-induced arrhythmias. DDO-02005 serves as a valuable tool for research into cardiac electrophysiology and potential therapeutic strategies for arrhythmia management. -
Kv1.5 Potassium Channel Inhibitor
DDO-02005 free base is a potent inhibitor of the Kv1.5 potassium channel, exhibiting an IC50 value of 0.72 μM. This compound demonstrates significant anti-atrial fibrillation effects in the CaCl2-ACh induced atrial fibrillation rat model and displays effective anti-arrhythmic activity in the context of aconitine-induced arrhythmias. DDO-02005 free base is a valuable tool for researching cardiac arrhythmias and potential therapeutic interventions. -
Kv1.3 Potassium Channel Inhibitor
KV1.3-IN-2 is a potent inhibitor of the Kv1.3 potassium channel, selectively inhibiting its activity while sparing hERG channel function. This compound has demonstrated significant potential in the investigation of immune-related diseases, including psoriasis, rheumatoid arthritis, and systemic lupus erythematosus, making it a valuable tool for research in these areas. -
ROMK Inhibitor
ROMK-IN-2 is a highly effective inhibitor of the renal outer medullary potassium (ROMK) channel. This compound exhibits potent biological activity, making it suitable for research focused on renal physiology and electrolyte homeostasis. ROMK-IN-2 is utilized in studies investigating potassium channel modulation and its implications in renal pathophysiology. -
Potassium Channel Inhibitor
UK-66914 is a selective potassium channel inhibitor that targets the delayed rectifier potassium current (I_K). This compound is designed to prolong action potential duration (APD) and enhance the cardiac refractory period, which may aid in terminating reentry mechanisms in arrhythmias. Its mechanism of action allows for therapeutic effects without the adverse side effects typically associated with antiarrhythmic agents that modulate sodium and calcium currents, making it valuable for cardiac research applications. -
Potassium Channel Inhibitor
Tityustoxin-Kα is a potent inhibitor of voltage-gated potassium channels. It exhibits a dose-dependent blockade of the sustained outward current in cultured hippocampal neurons, making it a valuable tool for researching neuronal excitability and synaptic transmission. Its application extends to studies on channel physiology and the mechanisms underlying neurotoxicity. -
Potassium Channel Inhibitor
AP14145 is a selective inhibitor of small conductance calcium-activated potassium channels, specifically targeting KCa2.2 and KCa channels with an IC50 of 1.1 μM. This compound has demonstrated the ability to prolong the atrial effective refractory period (AERP) in rat models and facilitate the conversion of atrial fibrillation to sinus rhythm in porcine models of left ventricular dysfunction. Its antiarrhythmic properties make AP14145 a valuable tool in cardiac electrophysiology research and the study of arrhythmias. -
ROMK or Kir1.1 Inhibitor
PF-06807656 is a highly selective inhibitor of the renal outer medullary potassium channel (ROMK or Kir1.1), exhibiting an IC50 of 61 nM against human ROMK in patch-clamp assays. This compound demonstrates significant selectivity for inhibiting rat ROMK and remains effective against N171D pore mutations. PF-06807656 serves as a valuable tool in cardiovascular disease research, enabling the exploration of potassium channel modulation in renal function and related pathophysiological conditions. -
TREK-1 Inhibitor
TREK inhibitor-3 is a selective inhibitor of the TREK-1 channel, exhibiting an IC50 of 0.81 μM and demonstrating blood-brain barrier permeability. This compound exhibits neuroprotective properties, significantly reducing the apoptosis of cortical neurons in models of oxygen-glucose deprivation and reoxygenation, as well as improving outcomes in mouse models of ischemic stroke, specifically middle cerebral artery occlusion and reperfusion. TREK inhibitor-3 serves as a valuable tool for investigating ischemic stroke and related neuroprotective mechanisms. -
Potassium Channel Inhibitor
UK-78282 is a selective inhibitor of the Kv1.3 voltage-gated potassium channel, exhibiting an IC50 of 200 nM. In addition to its primary target, UK-78282 also inhibits the Kv1.4 potassium channel. This compound demonstrates significant effects on human T cell activation, making it a valuable tool for studying immune responses and potential therapeutic applications in autoimmune diseases. -
Potassium Channel Inhibitor
L-3373 is a voltage-dependent potassium channel inhibitor that effectively reduces the refractory period and the dispersion of monophasic action potential duration. Its significant action in minimizing susceptibility to ventricular fibrillation has been demonstrated in a feline model of left ventricular hypertrophy. This compound serves as a valuable tool for research into cardiac electrophysiology and the mechanisms underlying arrhythmias. -
KCNT1 Inhibitor
KCNT1-IN-3 is a selective inhibitor of the potassium channel KCNT1, exhibiting an IC50 of 30 nM against wild-type human KCNT1. This compound is valuable for investigating the role of KCNT1 in epilepsy and related neurological conditions. Its potency allows for detailed studies into the modulation of ion channel activity and its implications in neuronal excitability. -
ROMK Inhibitor
VU590 dihydrochloride is a potent inhibitor of the renal outer medullary potassium channel (ROMK, Kir1.1) with an IC50 of 290 nM. It also exhibits inhibitory activity against Kir7.1, with an IC50 of 8 μM. This compound is valuable for research applications investigating potassium channel physiology and associated renal functions, although it may not be ideal for probing ROMK function specifically in kidney tissue. -
K+ Channel Inhibitor
Maurotoxin is a 34-residue peptide that acts as a potent inhibitor of potassium channels, specifically targeting Shaker potassium channels (ShB). With an IC50 value of 2 nM, Maurotoxin effectively attenuates K+ currents, making it a valuable tool for studying ion channel physiology and pharmacology. Its unique structure, characterized by four disulfide bridges, facilitates research into the mechanistic aspects of channel inhibition and potential therapeutic applications in neurobiology. -
Potassium Channel Inhibitor
Kv1.5-IN-1 is a selective inhibitor of the Kv1.5 potassium channel, exhibiting an IC50 value of 0.51 μM in humanKv1.5 channels. The introduction of a methoxy group at the R5 position maintains its inhibitory potency while demonstrating enhanced selectivity—approximately 2,600-fold over compound Ik and 300-fold over compound IId. This high selectivity profile suggests a favorable safety margin, promoting further pharmacodynamic and pharmacokinetic studies. Kv1.5-IN-1 is promising for research into therapies targeting diseases associated with dysfunctional Kv1.5 channel activity. -
Potassium Channel Inhibitor
Pandinotoxin Kα is a potent inhibitor of A-type potassium channels, derived from the venom of the Emperor scorpion (Pandinus imperator). This compound demonstrates significant biological activity by modulating ion channel function, making it a valuable tool for research in neurobiology and cardiovascular studies. Its inhibition of potassium channels has implications for understanding neuronal excitability and therapeutic interventions for channelopathies. -
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. -
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.
