Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Potassium Channel Activator
SG-209 is a potassium channel activator derived from Nicorandil, known for its ability to induce smooth muscle relaxation. This compound facilitates vasodilation through its action on potassium channels, contributing to enhanced tracheal smooth muscle relaxation. Research applications of SG-209 include studies on respiratory physiology and vascular function, particularly in animal models where it has been shown to increase tracheal blood flow. -
KCNE2/KCNQ1 Potassium Channel Blocker
IKs124 is a potent inhibitor of the KCNE2/KCNQ1 potassium channel, exhibiting an IC50 value of 8 nM. This compound is valuable for investigating the role of potassium channels in various biological processes, particularly in the context of peptic ulcer studies. Its selective blockade of these channels makes it an essential tool for research into gastrointestinal disorders and related therapies. -
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. -
Potassium Channel Activator
KR-30450 is a potent potassium channel activator with a specific action as a K+ ATP opener. It demonstrates significant cardioprotective effects, outperforming Lemakalim in enhancing reperfusion cardiac function. Additionally, KR-30450 effectively reduces reperfusion contracture and the release of lactate dehydrogenase, making it valuable for research in cardiac protection and ischemia-reperfusion injury studies. -
hSK1 Bloker
UCL-1848 TFA is a potent blocker of the human small conductance calcium-activated potassium channel (hSK1), exhibiting an IC50 value of 1.1 nM. This compound is valuable for studies focused on the modulation of hSK1 activity and its role in cellular signaling pathways. Research applications include investigations into excitability in neurons and cardiac tissues, as well as potential therapeutic implications in various neurological and cardiovascular disorders. -
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. -
Potassium Channel
Lombazole is an antimicrobial agent that primarily targets potassium channels and inhibits lipid synthesis in bacterial membranes. It exhibits selective antibacterial activity by disrupting the de novo synthesis of cell enclosure in Staphylococcus aureus without significantly affecting potassium permeability. Additionally, Lombazole interferes with the sterol C-14 demethylation process in Candida albicans, highlighting its potential applications in studying membrane dynamics and lipid biosynthesis in infectious pathogens. This compound is valuable for researchers investigating membrane integrity and antimicrobial resistance mechanisms. -
Potassium Channel Blocker
Besipirdine hydrochloride is a potassium channel blocker that exerts both cholinergic and adrenergic effects. Its cholinergic activity is characterized by stimulation of phosphatidylinositol turnover and a reduction in potassium currents, while its adrenergic activity promotes norepinephrine release through the inhibition of presynaptic α2-adrenergic receptors and the blocking of norepinephrine reuptake. This compound is applicable in research related to Alzheimer's disease, providing insights into potential therapeutic pathways. -
Chemical Modulator Of KCNQ Channel
ztz240 is a chemical modulator targeting the voltage-gated potassium channel Kv7 (KCNQ), specifically KCNQ2 and KCNQ3 with an EC50 of 6.1 μM, and KCNQ4 with an EC50 of 12.2 μM. This compound exhibits significant biological activity relevant to analgesia and anti-epileptic research. Its modulation of KCNQ channels makes it a valuable tool for studying the underlying mechanisms of pain and seizure disorders. -
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
(S)-PF 03716556 is a potassium channel inhibitor that functions as a K+-competitive acid blocker, exhibiting gastric acid pump inhibitory activity. This compound is utilized in research to study disease states influenced by gastric acid secretion, providing insights into potential therapeutic approaches for acid-related conditions. -
Potassium Channel KV1.5 Blocker
Mephetyl tetrazole is a potent potassium channel KV1.5 blocker with an IC50 of 330 nM. This compound is useful in cancer research, providing insights into the role of KV1.5 in tumor cell proliferation and survival. Its inhibition of KV1.5 channels may help elucidate the biochemical pathways that are altered in various cancer types, facilitating the development of targeted therapeutic strategies. -
Antiarrhythmic Agent
Nifekalant is a class III antiarrhythmic agent that functions as a blocker of IKr potassium channels, exhibiting an IC50 value of 10 μM. This compound is primarily utilized in research focused on refractory ventricular tachyarrhythmias, providing valuable insights into cardiac rhythm management. Its ability to modulate potassium channel activity makes it an essential tool for studying arrhythmic conditions and potential therapeutic interventions. -
Potassium Channel Activator
Phe-Met-Arg-Phe, amide is a potent potassium channel activator that reliably elicits K+ current activation in peptidergic caudodorsal neurons, with an effective dose (ED50) of 23 nM. This compound is critical for studies involving ion channel modulation and neuronal signaling, making it an essential tool in neurobiology research and pharmacological investigations. -
Potassium Channel Activator
KRN4884 is a potassium channel activator that stimulates KATP channels in the presence of intracellular ATP at a concentration of 1 mM. It enhances channel activity in a concentration-dependent manner, with an EC50 value of 0.55 μM. This compound is useful for researchers investigating the physiological roles of KATP channels and their implications in cellular signaling and metabolic regulation. -
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. -
Potassium Channel Activator
Potassium Channel Activator 1 is a selective potassium channel activator that facilitates the opening of potassium channels, contributing to membrane potential regulation. This compound exhibits significant biological activity that may influence cellular excitability and neurotransmitter release. It is primarily utilized in research focused on dopaminergic system disorders, providing insights into potential therapeutic strategies for neurological and psychiatric conditions. -
Potassium Channel
U89232 is a selective opener of the ATP-sensitive potassium (KATP) channels. This compound primarily acts on cardiac tissues, promoting vasodilation and potentially offering protective effects against ischemic conditions. It is valuable for research into cardiovascular pharmacology and the modulation of KATP channels in various therapeutic contexts. -
Potassium-Competitive Acid Blocker
Vonoprazan Fumarate is a potent potassium-competitive acid blocker (P-CAB) that exerts its effect by inhibiting H+,K+-ATPase activity, demonstrating an IC50 of 19 nM at pH 6.5 in porcine gastric microsomes. This compound exhibits significant antisecretory activity, making it valuable for investigating acid-related disorders. Research applications include studies related to gastroesophageal reflux disease and peptic ulcer disease, where it may provide insights into therapeutic mechanisms. -
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. -
Antiarrhythmic Agent
Encainide is an antiarrhythmic agent classified as a class IC antiarrhythmic. It functions by blocking voltage-dependent potassium channels, thus modulating cardiac excitability. This compound shows promise in research focused on life-threatening ventricular arrhythmias, symptomatic ventricular arrhythmias, and supraventricular arrhythmias. Its role in these conditions makes it valuable for studies aimed at understanding and treating various cardiac arrhythmias. -
Histamine H1 Receptor Antagonist
Terfenadine N-oxide is a histamine H1 receptor antagonist with an IC50 value of 2.73 μM, also exhibiting inhibition of the hERG potassium channel with an IC50 of 0.698 μM. This compound is valuable for investigating histamine-related allergic diseases and the role of hERG channels in arrhythmias. Its dual activity makes it a useful tool for research in pharmacology and toxicology related to allergic responses and cardiac rhythm disturbances. -
Antispasmodic Agent
Terodiline is an antispasmodic agent that primarily targets the hERG potassium channel, exhibiting an IC50 of 375 nM. It possesses both anticholinergic and calcium antagonist properties, making it effective in reducing abnormal bladder contractions associated with detrusor instability. Terodiline is suitable for research applications focused on urinary incontinence. -
Stable Isotope
Bupivacaine-d9 hydrochloride is a deuterium-labeled analog of Bupivacaine hydrochloride, primarily known for its role as an NMDA receptor inhibitor. This compound effectively blocks sodium, L-calcium, and potassium channels, demonstrating potent inhibition of SCN5A channels with an IC50 value of 69.5 μM. Bupivacaine-d9 hydrochloride is valuable for research focused on chronic pain modulation and neuronal signaling studies. -
TRPV4-KCa2.3 Protein Complex Enhancer
TRPV4-KCa2.3 modulator 1 is a modulator that enhances the TRPV4-KCa2.3 protein complex, exhibiting significant antihypertensive activity. This compound promotes hyperpolarization and vasodilation in endothelial cells. Its ability to influence vascular responses makes it a valuable tool for investigating hypertension and related cardiovascular disorders in research settings. -
σ Receptor Agonist
threo-Ifenprodil hemitartrate is a sigma (σ) receptor agonist, exhibiting Kis of 59.1 nM and 2 nM for σ1 and σ2 receptors, respectively. This compound also acts as a NR2B subunit-selective NMDA receptor antagonist, with an IC50 of 0.22 μM, and demonstrates inhibition of the hERG potassium channel with an IC50 of 88 nM, indicating potential antiarrhythmic activity. threo-Ifenprodil hemitartrate serves as a valuable tool in neuropharmacology and cardiovascular research. -
KATP Opener
Iptakalim hydrochloride is a selective ATP-sensitive potassium channel (KATP) opener that exhibits significant lipophilicity. In addition to its primary mechanism, it also acts as an antagonist of α4β2-containing nicotinic acetylcholine receptors (nAChRs). This dual activity positions Iptakalim hydrochloride as a valuable tool for research in cardiovascular physiology and neuropharmacology, providing insights into potassium channel regulation and cholinergic signaling. -
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. -
GABAA Receptor Antagonist
Bicuculline (methochloride) is a selective antagonist of the GABAA receptor, exhibiting an IC50 value of 3 μM. This compound is known to induce clonic-tonic convulsions in mammals and is also capable of blocking Ca2+-activated potassium channels. Bicuculline (methochloride) is utilized in research focused on epilepsy and related psychiatric disorders, providing valuable insights into neuronal excitability and inhibitory transmission. -
Potassium Channel Opener
Flupirtine is a non-opioid analgesic that acts primarily as a potassium channel opener, specifically targeting Kv7 channels. This compound exhibits notable neuroprotective properties by stabilizing blood-brain barrier integrity, reducing oxidative stress, and counteracting focal cerebral ischemia. Flupirtine is utilized in research related to pain management, Alzheimer's disease, multiple sclerosis, and neuroprotection due to its ability to lessen neuronal excitotoxicity and maintain resting membrane potential without exhibiting antipyretic or antiphlogistic effects. -
Starting CompoundsFor The Synthesis of KV7.2/3 Openers
2,6-Dichloro-3-nitropyridine is a key starting compound in the synthesis of sulfide analogs of Flupirtine, which function as KV7.2/3 channel openers. This compound exhibits potential biological activity relevant to pain research, making it a valuable reagent for studies focused on the modulation of neuronal excitability and analgesic mechanisms. Its utility in the development of KV7.2/3 activators positions it as an important tool in therapeutic research. -
Biochemical Assay Reagents
6-FAM-AEEAc-Stichodactyla helianthus Neurotoxin (ShK) is a fluorescent-labeled polypeptide that primarily targets voltage-gated potassium channels. This reagent exhibits potent inhibitory activity on ion channel function, making it valuable for biochemical assays focused on channel pharmacology and neurobiology. Its applications extend to studies investigating ion channel modulation and neurotoxin interactions in cellular models. -
Biochemical Reagent
Glycopyramide is a sulfonylurea compound that primarily targets and inhibits the ATP-sensitive potassium channels in pancreatic beta cells. This inhibition promotes insulin secretion, making it relevant in the study of diabetes and glucose metabolism. It can be utilized in biochemical research to explore mechanisms of insulin release and the regulation of blood glucose levels. -
Endogenous Metabolite
ISQ-1 hydrochloride is an isoquinolinone compound that functions as an inhibitor of the IKur potassium channel. It demonstrates potential to influence cardiac electrophysiology by modulating arrhythmic activity in atrial tissues. This reagent is primarily utilized in research focused on cardiac rhythm disorders and electrophysiological studies of heart functions. -
Anti-malarial Agent
Quinine hydrochloride dihydrate is an anti-malarial agent primarily known for its inhibitory action on potassium channels. It effectively inhibits wild-type mouse Slo3 (KCa5.1) channel currents in response to voltage pulses, exhibiting an IC50 value of 169 μM. This compound is essential for research into malaria treatment and the study of ion channel modulation in various biological contexts. -
K+ Channel Blocker
Dendrotoxin-I (DTX-I) is a potent inhibitor of voltage-gated potassium channels, specifically targeting the KV1.1, KV1.2, and KV1.6 subunits with IC50 values ranging from 0.13 to 50 nM. This neurotoxin exhibits significant biological activity that can influence neuronal excitability and synaptic transmission. Dendrotoxin-I is primarily utilized in research applications related to cancer and neurobiology, providing insights into ion channel function and their roles in disease mechanisms. -
hERG Channel Blocker
Tannic acid is identified as a novel hERG channel blocker, exhibiting an IC50 of 3.4 μM. This compound has significant implications in cardiovascular research, particularly in studying drug-induced long QT syndrome and cardiac arrhythmias. Its capacity to modulate ion channel activity makes it a valuable tool in pharmacological studies focused on cardiac safety and ion channel function. -
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. -
Vasodilator
SCA-40 is a potent vasodilator targeting bronchial smooth muscle. It induces biphasic relaxation in bronchi exhibiting spontaneous tension, with its relaxation effects remaining unaffected by various potassium channel blockers. This compound is suitable for research applications focused on bronchial conditions and related pathophysiological studies.
