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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
HCN2 Inhibitor
HCN2 modulator-8 is a selective inhibitor of the HCN2 channel, classified as a pyrazolopyridine derivative. It exhibits significant activity in modulating hyperalgesic and sensory signaling pathways, making it valuable for research into pain management, tinnitus, and various central nervous system disorders, including psychiatric and mood disorders. -
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. -
SK channel/TRPM7 Inhibitor
NS8593 is a selective inhibitor of small conductance Ca2+-activated K+ channels (SK channels), specifically targeting the SK1-3 subtypes. It exhibits a reversible inhibition of SK3-mediated currents with Ca2+-dependent potency (Kd values of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca2+), while leaving intermediate and large conductance K channels unaffected. Additionally, NS8593 inhibits the TRPM7 channel with an IC50 of 1.6 mM. This compound is valuable for research into central nervous system-related diseases and the physiological roles of SK and TRPM7 channels. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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 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. -
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. -
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. -
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. -
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. -
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.
