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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
KV1.3 Channel Inhibitor
ShK toxin is a potent inhibitor of the voltage-dependent potassium channel (Kv1.3), derived from the Caribbean sea anemone Stichodactylus helianthus. This toxin competitively interacts with dendrotoxin I and α-dendrotoxin at synaptosomal membranes, enhancing acetylcholine release. In addition to its neural effects, ShK toxin effectively suppresses K+ currents in cultured rat dorsal root ganglion neurons and demonstrates significant inhibition of T lymphocyte proliferation. It serves as a valuable tool in studies of neurophysiology and immunology. -
Kir2 Inhibitor
ML-133 is a selective inhibitor of the Kir2 family of potassium channels, exhibiting an IC50 of 1.8 μM at pH 7.4 and 290 nM at pH 8.5. This compound serves as a valuable tool for investigating the role of Kir2 channels in various physiological processes and pathophysiological conditions. Its ability to modulate potassium ion flow makes it applicable in studies related to cardiac function, neuronal signaling, and other cellular activities influenced by Kir2 channel activity. -
Kv 1.5 Inhibitor
BMS-394136 is a selective inhibitor of the Kv 1.5 potassium channel, exhibiting an IC50 of 0.05 μM. This compound effectively prolongs the atrial effective refractory period (AERP) and action potential duration (APD) in a dose-dependent manner while leaving the ventricular effective refractory period (VERP) unaffected. BMS-394136 is particularly useful for research focused on acute atrial ischemia and related cardiac electrophysiological studies. -
Ion Channel Inhibitor
Nerispirdine is an ion channel inhibitor that selectively targets voltage-gated potassium channels K(v)1.1 and K(v)1.2, exhibiting IC50 values of 3.6 µM and 3.7 µM, respectively, and also inhibits voltage-dependent sodium channels with an IC50 of 11.9 µM. As a derivative of 4-aminopyridine, Nerispirdine serves as a valuable tool in the investigation of neurological disorders, contributing to research focused on channelopathies and synaptic transmission. Its potential for modulating ion channel activity makes it a significant compound for studying electrophysiological processes. -
Kv1.5 Channel Inhibitor
MSD-D is a potent Kv1.5 channel inhibitor, exhibiting a frequency-dependent mechanism with an IC50 value of 0.5 μM. This compound is promising for research into atrial-selective class III antiarrhythmics, offering potential insights into cardiac arrhythmias and related therapies. -
hERG Inhibitor
6-O-Desmethyl donepezil is a potent hERG channel inhibitor, exhibiting an IC50 value of 1 μM. As a metabolite of Donepezil, it is instrumental in studying cardiac ion channel activity and the potential implications of drug interactions. This compound is valuable for research in cardiotoxicity and pharmacology, particularly in the context of drug development and assessment of cardiac safety profiles. -
bTREK-1 Potassium Channel Inhibitor
6-Bnz-cAMP (N6-Benzoyl-cAMP) is a potent inhibitor of the bTREK-1 potassium channel, functioning through a protein kinase A (PKA) independent mechanism. This compound is instrumental in investigating the roles of signal transduction proteins within the cAMP signaling pathway. Its use can aid in elucidating the physiological and pathophysiological processes mediated by bTREK-1 and cAMP-related signaling cascades. -
Potassium Channel Inhibitor
(BrMT)2 is a non-peptide potassium channel inhibitor that primarily targets Kv1.1 channels. It effectively slows the activation kinetics of these channels, making it a valuable tool for elucidating the physiological roles of potassium channels in various cellular processes. This compound is useful in research applications focusing on neurophysiology, cardiac function, and other studies involving ion channel modulation. -
Potassium Channel Inhibitor
CS476 is a potent inhibitor of potassium channels, exhibiting significant hypoglycemic activity. This compound may facilitate research into the modulation of glucose homeostasis and has potential applications in the study of diabetes-related pathways. Its ability to influence potassium channel activity makes it a valuable tool for investigating various cellular processes linked to metabolic regulation. -
Proton Pump/Potassium-competitive Acid Inhibitor
Abeprazan hydrochloride is a potassium-competitive acid inhibitor that selectively targets H+, K+-ATPase, providing a mechanism of action distinct from traditional proton pump inhibitors. By reversibly binding in a potassium-competitive manner, Abeprazan hydrochloride effectively reduces gastric acid secretion without requiring acid activation. This compound is being investigated for its therapeutic potential in treating various acid-related gastrointestinal disorders. -
Proton Pump/Potassium-competitive Acid Inhibitor
Abeprazan is a potassium-competitive acid inhibitor primarily targeting the H+, K+-ATPase enzyme. By reversibly binding to this enzyme through potassium-competitive ionic interactions, it effectively reduces gastric acid secretion without the need for acid activation. Abeprazan is being developed as a potential alternative to traditional proton pump inhibitors for the management of acid-related disorders, providing a novel approach to acid control in clinical applications. -
Potassium Channel Inhibitor
RY785 is a potent and selective inhibitor of voltage-gated potassium channels, specifically targeting KV2.2 with an IC50 of 0.05 μM. This compound exhibits notable analgesic activity, making it valuable for research into pain management and related therapeutic applications. Its specificity towards KV2 channels allows for exploration of their role in various physiological and pathological processes. -
P-gp Inhibitor/Potassium Channel Activator
GPV0057 is a selective and potent inhibitor of P-glycoprotein (P-gp) and a specific activator of the potassium channel Kir2.1. By competitively binding to the substrate-binding site of P-gp, GPV0057 inhibits ATP-dependent drug efflux, effectively reversing multidrug resistance in tumor cells. Additionally, it stabilizes the open state of Kir2.1, facilitating potassium ion influx. This compound holds potential for research in tumors characterized by high P-gp expression and in conditions such as heart failure and Andersen-Tawil Syndrome that involve Kir2.1 deficiency. -
NMDA Receptor Inhibitor
Bupivacaine is an NMDA receptor inhibitor that modulates neuronal excitability by blocking sodium, L-calcium, and potassium channels. It exhibits potent inhibition of SCN5A channels, with an IC50 of 69.5 μM. This compound is primarily utilized in research focused on chronic pain mechanisms and therapeutic interventions. -
NMDA Receptor Inhibitor
Bupivacaine-d9 is a deuterium-labeled analog of Bupivacaine, primarily targeting NMDA receptors. This compound exhibits inhibitory effects on sodium, L-calcium, and potassium channels, with a notable potency against SCN5A channels, characterized by an IC50 value of 69.5 μM. Bupivacaine-d9 is utilized in research related to chronic pain mechanisms and the modulation of excitatory neurotransmission, offering valuable insights into therapeutic applications in pain management. -
Potassium/Sodium Channel Inhibitor
Huwentoxin I is a peptide toxin that specifically inhibits voltage-gated sodium channels and N-type calcium channels. This compound has demonstrated significant inhibitory effects on sodium channels in both rat hippocampus and cockroach dorsal unpaired median (DUM) neurons, with IC50 values of 66.1 nM and 4.80 nM, respectively. Huwentoxin I is valuable for studies focused on neuronal excitability and channelopathy-related research applications. -
NMDA Receptor Inhibitor
Bupivacaine hydrochloride monohydrate is an NMDA receptor inhibitor that effectively modulates excitatory neurotransmission. It possesses the ability to block sodium, L-calcium, and potassium channels, with a notable potency in inhibiting SCN5A channels, exhibiting an IC50 value of 69.5 μM. This compound is primarily utilized in research focused on chronic pain mechanisms and the development of analgesic strategies. -
TASK-1 Inhibitor
Doxapram hydrochloride hydrate is a TASK-1 inhibitor that enhances respiratory function by stimulating the brain's respiratory centers and peripheral chemoreceptors. This compound effectively increases both the rate and depth of breathing, while demonstrating inhibitory effects on TASK-1, TASK-3, and their heterodimeric channels with EC50 values of 410 nM, 37 μM, and 9 μM, respectively. Additionally, it inhibits Ca²⁺-activated and Ca²⁺-independent potassium currents in type I cells of the carotid body, with IC50 values of approximately 13 μM and 20 μM, respectively. Doxapram hydrochloride hydrate serves as a useful reagent for research on respiratory depression conditions, including post-anesthesia recovery, chronic obstructive pulmonary disease, and apnea of prematurity. -
Potassium Channel Inhibitor
Cloperastine hydrochloride is a potassium channel inhibitor primarily targeting hERG K+ currents. It demonstrates concentration-dependent inhibition, with an IC50 value of 27 nM. This reagent is employed in research applications focused on cardiac ion channel function and drug interactions, providing valuable insights into cardiovascular safety and pharmacology. -
Potassium Channel Inhibitor
Cloperastine fendizoate is a potent inhibitor of the hERG potassium channels, exhibiting concentration-dependent inhibition with an IC50 value of 27 nM. This compound is primarily utilized in research applications focusing on cardiac ion channel function and related arrhythmia studies. Its effects on potassium currents make it valuable for investigating the electrophysiological properties of cardiac tissues and potential therapeutic interventions. -
Potassium Channel Inhibitor
Tetraethylammonium chloride is a non-selective inhibitor of potassium channels, effectively blocking their function. This compound is recognized as a substrate for organic cation transporter 1 (OCTN1), which may be relevant in transport-related studies. Additionally, tetraethylammonium chloride exhibits potential antitumor properties, making it a valuable tool in cancer research and investigations into ion channel dynamics. -
FTO Inhibitor
Meclofenamic acid is a highly selective inhibitor of the fat mass and obesity-associated (FTO) enzyme, which plays a crucial role in the regulation of m(6)A RNA methylation. By competing with FTO for binding to m(6)A-containing nucleic acids, it modulates RNA metabolism and influences cellular processes related to metabolism and obesity. Additionally, Meclofenamic acid exhibits non-selective blockade of gap junctions and inhibits the potassium channels hKv2.1 and hKv1.1, with IC50 values of 56.0 µM and 155.9 µM, respectively. This compound is valuable for research applications focused on obesity, metabolic regulation, and ion channel physiology.
