Catalog No.
Product Name
Application
Product Information
Citations
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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. -
BKCa-channel Blocker
GAL-021 sulfate is a potent BKCa-channel blocker that selectively inhibits KCa1.1 channels in GH3 cells. This compound serves as a novel modulator of breathing control, derived from selective modifications of the almitrine pharmacophore. Research indicates that GAL-021 sulfate effectively enhances minute ventilation in both rat and non-human primate models, making it relevant for studies in respiratory physiology and pharmacology. -
P-CAB Agent
P-CAB Agent 2 Hydrochloride is a potent potassium-competitive acid blocker targeting the H+/K+-ATPase enzyme, demonstrating an IC50 value of less than 100 nM. This reagent effectively inhibits gastric acid secretion and exhibits selective blocking of the hERG potassium channel with an IC50 of 18.69 µM. P-CAB Agent 2 Hydrochloride has been shown to have a favorable safety profile, as it demonstrates no acute toxicity while effectively suppressing histamine-induced gastric acid production. It is a valuable tool for research applications focused on gastrointestinal pharmacology. -
Potassium Channel Blocker
Amifampridine phosphate is a potent voltage-gated potassium (Kv) channel blocker with oral bioavailability. It effectively reverses the effects of botulinum toxin type A (BoNT/A) intoxication and enhances neurotransmitter release at neuromuscular junctions (NMJs). This compound is valuable for research applications related to Lambert-Eaton myasthenic syndrome (LEMS) and other neuromuscular disorders. -
KCa2/3 Channel Modulator
RA-2 is a negative-gating modulator of KCa2/3 channels, exhibiting an IC50 of 17 nM. This compound effectively inhibits bradykinin-induced endothelium-derived hyperpolarization (EDH)-type relaxation in U46619-precontracted vascular rings. RA-2 serves as a valuable tool for investigating the physiological and pathophysiological roles of KCa2/3 channels in the vasculature, central nervous system, and inflammatory processes. -
Kv7.2/Kv7.3/TSPO Activator
Kv7.2/Kv7.3 activator-3 is a potent activator targeting the Kv7.2 and Kv7.3 potassium channels, as well as the translocator protein (TSPO). It demonstrates biological activities by activating Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC50 values of 0.37, 2.06, and 0.75 μM, respectively, and showing binding affinity to TSPO with Ki values of 0.07 μM and 4.60 μM in rat and human cells, respectively. This compound has been shown to prevent motor neuron degeneration associated with ALS/FTD, stimulate axonal growth in dorsal root ganglia, and exhibit anti-epileptic effects. Additionally, it alleviates pain hypersensitivity in diabetic neuropathy and promotes neuronal survival after cervical injury in preclinical models. -
Potassium Channel Agonist
ZD-6169 is a selective agonist of ATP-sensitive potassium channels (KATP). By activating KATP channels, ZD-6169 effectively reduces cell membrane excitability and contractility in bladder smooth muscle. This compound shows potential in the research of conditions such as overactive bladder, making it a valuable tool for studying bladder function and related disorders. -
Potassium Channel Opener
NIP-121 is a potassium channel opener that facilitates vasodilation, leading to a reduction in mean pulmonary artery pressure and total pulmonary resistance. Its unique mechanism makes it a valuable reagent for researching pulmonary arterial hypertension, providing insights into potential therapeutic strategies for this condition. -
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 Opener
YM 934 is a potassium channel opener that modulates ion flow to enhance cellular excitability. It has demonstrated inhibitory effects on neurogenic plasma leakage and can attenuate airway neurogenic inflammation. This compound is applicable in research focusing on respiratory diseases and neurogenic mechanisms involved in inflammation and leakage pathways. -
Potassium Channel Agonist
Emakalim is an ATP-dependent potassium channel agonist. It exhibits significant biological activity by promoting the opening of potassium channels, which can lead to cellular hyperpolarization. Research applications of Emakalim include investigating its effects on gliomas, triple-negative breast cancer, non-small cell lung cancer, and colorectal cancer, providing insights into potential therapeutic strategies for these malignancies. -
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. -
Kv7.2 Activator
Kv7.2 activator-1 is a selective activator of the Kv7.2 ion channel with an EC50 of 178 nM. This compound exhibits a prolonged half-life of 120 minutes in human liver microsomes, making it suitable for in-depth pharmacological studies. Its role in modulating ion channel activity positions Kv7.2 activator-1 as a valuable tool for research in neuropharmacology and related fields. -
Kv7 Channel Activator
Kv7 activator-1 is a potent activator of Kv7 channels, influencing neuronal excitability. It has demonstrated key biological activities relevant to the modulation of synaptic transmission, making it a valuable tool in research focused on depression disorders, neurodegenerative diseases, and pain management. This compound can facilitate investigations into the therapeutic potential of Kv7 channel modulation in various neurological conditions. -
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. -
Stable Isotope
Acetohexamide-d11 is a deuterium-labeled derivative of Acetohexamide, a first-generation sulfonylurea compound. This reagent primarily targets ATP-sensitive potassium channels in pancreatic β cells, promoting insulin secretion vital for studies on type 2 diabetes. Researchers can utilize Acetohexamide-d11 to trace metabolic pathways and evaluate pharmacokinetics in diabetes research applications. -
Potassium Channel Opener
KI 1769 is a potassium channel opener that facilitates vasodilation. This compound has been shown to prolong micturition intervals and decrease urethral resistance to fluid infusion. KI 1769 serves as a valuable tool for investigating cardiovascular diseases and related physiological processes. -
Antiarrhythmic Agent
L-702958 hydrochloride is a potent blocker of the human Ether-à-go-go-Related Gene (hERG) channel, with an IC50 of 14.3 nM. This compound functions as an antiarrhythmic agent and is primarily utilized in research focused on the mechanisms underlying arrhythmias. Its ability to inhibit hERG potassium channels makes it a valuable tool for studying cardiac electrophysiology and associated pathologies. -
Potassium Currents Blocker
Ethyl tosylcarbamate is a chemical intermediate utilized in the synthesis of Gliclazide, a potent blocker of ATP-sensitive potassium currents in pancreatic beta-cells. With an IC50 of 184 nM, Gliclazide plays a crucial role in regulating insulin secretion. This compound is valuable for research focused on diabetes and potassium ion channel functions. -
Kv7 Channel Activator
PF-05020182 is an orally active Kv7 channel activator that specifically targets human Kv7.2/7.3, Kv7.4, and Kv7.3/7.5 channels, with EC50 values of 334, 625, and 588 nM, respectively. This compound demonstrates significant anticonvulsant activity in rat models of corneal electric shock-induced tonic seizures. Additionally, PF-05020182 is capable of crossing the blood-brain barrier, making it a valuable tool for neurological research applications. -
Kv Channel Blocker
OSK-1 is a potent blocker of voltage-gated potassium (Kv) channels, specifically exhibiting IC50 values of 0.6 nM, 5.4 nM, and 0.014 nM for Kv1.1, Kv1.2, and Kv1.3, respectively. Additionally, OSK-1 demonstrates moderate activity against the Ca2+-activated KCa3.1 channel, with an IC50 of 225 nM. As a member of the α-KTx3 toxin family, OSK-1 serves as an immunosuppressive agent and is valuable in research exploring potassium channel modulation and its effects on cellular signaling pathways. -
Kv7.2/Kv7.3 Modulator
Kv7.2/Kv7.3 modulator-3 is a selective modulator of the Kv7.2 and Kv7.3 potassium channels, exhibiting an EC50 of 0.099 μM. This compound is valuable for research into neuronal excitability and modulation of action potentials. Its precise action on these ion channels supports studies in areas such as epilepsy and other neurological disorders, facilitating a better understanding of their physiological roles and potential therapeutic targets. -
Aprikalim Enantiomer
Rel-Aprikalim is the relative configuration of Aprikalim, a potassium channel opener (KCO) that specifically activates ATP-sensitive K+ (KATP) channels. It has demonstrated biological activity in guinea pig ventricular myocytes, making it a valuable tool for research into cardiac function and potassium channel modulation. This compound can be utilized in studies exploring the physiological roles of KATP channels and their implications in cardiac pathophysiology. -
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. -
P-CAB Agent
P-CAB Agent 2 is a potent potassium-competitive acid blocker that targets and inhibits H+/K+-ATPase activity, demonstrating an IC50 of less than 100 nM. It is effective in reducing gastric acid secretion and shows no acute toxicity. Additionally, P-CAB Agent 2 inhibits the hERG potassium channel with an IC50 of 18.69 µM, making it relevant for studies in gastric physiology and potential therapeutic applications for acid-related disorders. -
Potassium Channel Opener
AL 0671 is a potassium channel opener that promotes the relaxation of vascular smooth muscle through the opening of potassium channels. It effectively inhibits nonenzymatic glycation of proteins and reduces LDL oxidation. This compound is valuable for research applications related to cardiovascular and metabolic diseases, including hypertensive diabetes, providing insights into potential therapeutic strategies. -
Kv7.2/Kv7.3 Agonist
Kv7.2/Kv7.3 agonist 1 is a potent orally active agonist targeting the KV7.2/7.3 channels (KCNQ2/3), exhibiting an EC50 value of 1.03 μM. This compound demonstrates significant analgesic effects in both the chronic constriction injury (CCI) model and the Streptozotocin-induced diabetic peripheral neuropathic pain (DPNP) model, with effective doses (ED50) of 12.02 mg/kg and 9.63 mg/kg, respectively. It serves as a valuable tool for research into pain management and neurological conditions associated with Kv7 channel modulation. -
KCa2 Channel Modulator
KCa2 Channel Modulator 1 is a potent subtype-selective positive modulator specifically targeting KCa2 channels. It enhances the activity of human KCa2.3 channels with an EC50 of 0.19 μM, and also exhibits activity on rat KCa2.2 channels with an EC50 of 0.99 μM. This compound is valuable for research applications focusing on calcium-activated potassium channels and their roles in various physiological processes. -
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. -
SK2 Channels Blocker
Lei-Dab7 is a highly selective blocker of SK2 (KCa2.2) channels, exhibiting a Kd value of 3.8 nM. This compound demonstrates minimal to no activity against KCa1, KCa3, Kv, and Kir2.1 channels, making it an excellent tool for investigating SK2 channel functions. Its specificity makes Lei-Dab7 valuable in research applications focused on calcium-activated potassium channels and related physiological pathways. -
Potassium Ion Regulator
AU-1421 is a potassium ion (K⁺) site-directed regulator that selectively interacts with various cation transport ATPases. This compound distinguishes between two K⁺-sensitive phosphorylation intermediate (E2P) states, accelerating hydrolysis in non-K⁺ transport ATPases such as sarcoplasmic reticulum Ca²⁺-ATPase, while inhibiting hydrolysis and stabilizing the phosphorylated state in K⁺ transport ATPases, including gastric mucosa H⁺/K⁺-ATPase and renal Na⁺/K⁺-ATPase. AU-1421 is valuable for investigating the mechanistic pathways of potassium ion pumps in cellular processes. -
Kv3 Channel Modulator
Kv3 modulator 5 is a selective modulator of the Kv3 channel, specifically enhancing Kv3.2 ion currents. This compound plays a significant role in the modulation of neuronal firing rates and has potential applications in the study of auditory processing and hearing disorders. Researchers can utilize Kv3 modulator 5 to investigate its effects on synaptic transmission and its therapeutic potential in auditory-related pathologies. -
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. -
Potassium Channel Opener
BMS-223131 is a potent maxi-K potassium channel opener, primarily targeting potassium channels to enhance K+ efflux and hyperpolarize cell membranes, leading to reduced Ca2+ influx. It demonstrates strong inhibitory activity on the CYP2C9 enzyme (IC50 = 1.7 μM) and modulates several other CYP enzymes, including CYP1A2, CYP2C19, CYP2D6, and CYP3A4. This compound is valuable in research focused on neurological diseases, particularly stroke, due to its ability to influence ion channel activity and cellular excitability. -
Potassium Channel Opener
TCV 295 is an orally active potassium channel opener that targets potassium channels to induce vasodilation. It has demonstrated efficacy in reducing blood pressure, systemic vascular resistance, and myocardial oxygen consumption. This compound is particularly useful for research applications focused on cardiovascular diseases, including hypertension. -
Potassium Channel Opener
JTV-506 is a potent ATP-sensitive potassium channel opener that primarily targets KATP channels. It effectively inhibits histamine-induced contractions in tracheal smooth muscle and reduces pulmonary vascular tone through direct action on vascular smooth muscle cells. JTV-506 serves as a valuable tool in pulmonary hypertension research, facilitating investigations into therapeutic strategies for managing this condition. -
Potassium channel opener
Rilmakalim is a potassium channel opener that primarily targets ATP-sensitive K+ channels. It enhances potassium efflux, leading to hyperpolarization of the cell membrane, which can result in vasodilation and decreased heart muscle contractility. Rilmakalim is widely utilized in research investigating cardiovascular physiology, diabetic complications, and neuroprotection, particularly in the context of cardiac and vascular health. -
Kv1.5 Blocker
KVI-020 is a potent and selective blocker of the atrial potassium channel Kv1.5, exhibiting an IC50 of 480 nM. This compound demonstrates a weaker inhibition of hERG channels, with an IC50 of 15,100 nM. KVI-020 serves as an effective antiarrhythmic agent and is valuable for research focused on atrial fibrillation (AF) and related cardiac dysrhythmias. -
Potassium Channel Activator
Aprikalim is a potassium channel activator that primarily targets ATP-sensitive K+ (KATP) channels. It has been shown to enhance KATP channel activity in guinea pig ventricular myocytes, particularly in Mg-NDP solutions, where it reduces ATP sensitivity and increases the K1 value from 56 μM to 180 μM. This property highlights the potential of Aprikalim in modulating cardiac excitability and suggests its relevance in exploring therapeutic strategies for cardiac conditions. Its effects on KATP channel functionality may also provide insights into the enzymatic activity of channel proteins under various experimental conditions. -
Kv1.5 Blocker
AVE-0118 is a nonselective blocker of the voltage-gated potassium channel Kv1.5, exhibiting an IC50 of 1.1 μM. This compound functions as a multichannel inhibitor with micromolar activity against Kv1.5 and several other ion channels, while demonstrating inactivity towards IKs, IKATP, and L-type calcium channels. AVE-0118 is useful in research related to cardiac action potentials and can aid in the study of ion channel pharmacology. -
Kv7.2 Modulator
Kv7.2 modulator 2 is a selective modulator of the Kv7.2 potassium ion channel, primarily involved in neuronal excitability. This compound has demonstrated potential in the modulation of excitatory neurotransmission, making it valuable for research related to epilepsy and other neurological disorders. Its role in enhancing potassium ion flow may provide insights into therapeutic strategies for seizure management and neuronal stabilization. -
Antiarrhythmic Agent
Ipazilide fumarate is an antiarrhythmic agent that primarily targets potassium channels. It effectively reduces K+-depolarized tone and prolongs ventricular refractoriness, making it beneficial in the management of arrhythmias. Additionally, Ipazilide fumarate exhibits antiectopic activity, providing important insights into cardiac electrophysiology and potential therapeutic applications in treating arrhythmia-related disorders. -
Potassium Channel Control
Dehydroindapamide targets potassium channels and is an indole derivative of Indapamide. This compound serves as an important tool for quantitatively assessing the turnover rate of Indapamide by the CYP3A4 enzyme, exhibiting a turnover rate approximately ten times higher than that of Indoline. Its enhanced affinity for CYP3A4 makes it a valuable reagent for research applications involving cardiac and vascular function regulation. -
Kv1.3 Blocker
Vm24-toxin (Vaejovis mexicanus peptide 24) selectively targets the Kv1.3 potassium channel, exhibiting a dissociation constant (Kd) of approximately 3 pM in lymphocytes. With over 1500-fold selectivity for Kv1.3 compared to other potassium channels, this 36-residue peptide adopts a unique cystine-stabilized α/β fold comprised of a single-turn α-helix and a three-stranded antiparallel β-sheet. Vm24-toxin effectively reduces the CD4+ effector memory T cell response following T cell receptor (TCR) stimulation, making it a valuable tool for immunological research and studies exploring T cell signaling pathways. -
Potassium Channel Modulator
SDZ PCO 400 is a potassium channel modulator that targets and regulates potassium channels, leading to relaxation of airway smooth muscle. It has demonstrated efficacy in reversing airway obstruction induced by intravenous bronchospasmodics. This compound is of interest in research applications related to respiratory physiology and the treatment of airway hyperresponsiveness. -
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. -
Sodium/Potassium Channel Blocker
α-Dendrotoxin is a peptide neurotoxin derived from the venom of the African green mamba (Dendroaspis angusticeps) that serves as a sodium/potassium channel blocker. It selectively inhibits KV1.1, KV1.2, KV1.6, and ASIC channels, leading to increased neuronal excitability by lowering the threshold for action potentials and enhancing their frequency. This compound is valuable for neurotoxicology research and the investigation of neuronal signaling pathways.
