Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Nav1.8 Modulator
Nav1.8 modulator 1 is a selective modulator targeting the Nav1.8 sodium channel, which plays a crucial role in the transmission of pain signals. This compound exhibits potent modulation properties, making it a valuable tool for pain research. Its ability to influence neuronal excitability can aid in the exploration of pain pathways and the development of novel analgesic therapies. -
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. -
Antiarrhythmic Agent
(-)-(S)-Cibenzoline is an antiarrhythmic agent that primarily targets sodium channels. This S(+)-enantiomer of Cibenzoline demonstrates significant efficacy in the modulation of cardiac rhythm. It is commonly utilized in research focused on the treatment of arrhythmias and the investigation of cardiac electrophysiology. -
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. -
Potassium Channel Blocker
L-735821 is a potassium channel blocker specifically targeting the KCNQ1 channel. It exhibits potent antagonistic activity with an EC50 of 0.08 μM, effectively influencing current-voltage relationships of IKs and IKr in rabbit ventricular myocytes. Additionally, L-735821 completely inhibits IKs in isolated human ventricular myocytes at a concentration of 100 nmol/L, demonstrating its efficacy in modulating cardiac ion currents. This compound is well-suited for research focused on cardiac electrophysiology and the role of potassium channels in cardiac function. -
Antiarrhythmic Agent
Tedisamil is an antiarrhythmic agent primarily targeting the transient outward potassium current (I(to)) in the atrium, leading to a significant reduction in heart rate. This compound also inhibits various potassium currents, including IK and K(ATP), as well as PKA-activated chloride channels, ultimately prolonging the cardiac action potential and QT interval. Tedisamil demonstrates effective antiarrhythmic properties against ventricular arrhythmias and atrial flutter in preclinical animal models, making it a valuable tool for cardiovascular research. -
K+ Channel Opener
P-1060 is a potassium channel opener that enhances potassium ion conductance across cellular membranes. It shows significant biological activity in promoting vasodilation and reducing vascular resistance, making it a valuable tool in cardiovascular research. P-1060 is utilized to investigate the mechanisms underlying cardiovascular diseases and to explore potential therapeutic strategies targeting ion channel dysfunction. -
Kv Channel Blocker
RuBi-4AP is a caged Kv channel blocker that incorporates a photolabile protecting group, enabling controlled activation with light. This unique characteristic allows for precise manipulation of its effects on neuronal excitability and synaptic transmission. RuBi-4AP is valuable for investigating signal propagation and understanding the dynamics of electrical signaling in neuronal networks. -
Stable Isotope
Ropivacaine-d7 hydrochloride is a deuterium-labeled derivative of Ropivacaine, primarily functioning as a potent sodium channel blocker. It inhibits sodium ion influx in nerve fibers, leading to reversible blockade of impulse conduction. Additionally, Ropivacaine acts as an inhibitor of the TREK-1 potassium channel, demonstrating an IC50 of 402.7 μM in COS-7 cell membranes. This reagent is valuable for research in neuropathic pain management and the study of ion channel dynamics. -
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. -
KV4.2/KV4.3 Channels Blocker
Phrixotoxin 2 is a selective blocker of KV4.2 and KV4.3 channels, known for its potent inhibitory effects. This compound is valuable in studying the physiological roles of these ion channels in neuronal excitability and cardiac function. Phrixotoxin 2 is instrumental in research applications related to neurobiology, cardiology, and studies involving ion channel modulation. -
Potassium Channel Activator
KR-31378 is a potassium channel activator that exhibits neuroprotective properties. Its pharmacokinetic profile demonstrates dose-dependent behavior, characterized by reduced clearance and effective oral absorption in rat models. This compound is important for studying neuroprotection mechanisms and evaluating the therapeutic potential of potassium channel modulation in neurological disorders. -
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. -
Antiarrhythmic Agent
Disopyramide hydrochloride is a class IA antiarrhythmic agent primarily targeting cardiac sodium channels. It effectively treats both ventricular and atrial arrhythmias by blocking fast inward sodium currents and prolonging the duration of cardiac action potentials. Additionally, disopyramide inhibits HERG-encoded potassium channels and demonstrates significant negative inotropic effects. This compound is valuable for research investigating cardiac electrophysiology and the mechanisms underlying arrhythmogenic conditions. -
Antiarrhythmic Agent
AZD7009 is a novel antiarrhythmic agent targeting hKv1.5 and hKv4.3/hKChIP2.2 potassium channels. It effectively inhibits these currents with IC50 values of 27.0 µM and 23.7 µM, respectively. This compound is useful in research focused on cardiac rhythm disorders and the mechanistic understanding of arrhythmogenesis. -
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. -
Kv1.1 Channel Blocker
Dendrotoxin K is a selective blocker of the Kv1.1 potassium channel, influencing neuronal excitability. It modulates glutamate release in CA3 neurons in a time-dependent manner by altering the presynaptic spike waveform, making it a valuable tool for studying synaptic transmission and neuronal signaling. This compound is useful for investigations into neuronal circuit dynamics and pathophysiological conditions involving ion channel function. -
Kv7.2 Potassium Channel Activator
E0714 is a selective activator of the Kv7.2 potassium channel, exhibiting EC50 values of 1.90 μM for homotetrameric Kv7.2 channels and 0.021 μM for heterotetrameric Kv7.2/7.3 channels. This compound effectively crosses the blood-brain barrier and demonstrates anticonvulsant properties. E0714 is suitable for research applications focused on epilepsy and related neurological disorders. -
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. -
Kv7.2/Kv7.3 Activator
Kv7.2/Kv7.3 activator-1 is a selective activator of Kv7.2 and Kv7.3 ion channels, demonstrating potent activity with an EC50 value of less than 1 µM. This compound is instrumental for investigating the role of these channels in neurological disorders and may provide valuable insights into therapeutic strategies for related diseases. Researchers may utilize Kv7.2/Kv7.3 activator-1 to better understand the modulation of neuronal excitability and synaptic transmission. -
Inward Rectifier K+ Channel Blocker
Tertiapin (reduced) is an inward rectifier K+ channel blocker that effectively inhibits potassium channel activity. Its unique structure, derived from the melittin synthesis, features critical disulfide bonds, enabling selective blockage of calcium-activated large conductance potassium channels. This reagent is valuable for research applications related to various neurological and inflammatory diseases, including rheumatoid arthritis and multiple sclerosis. -
Potassium Channel Activator
BRL 55834 is a potent activator of potassium channels. This compound demonstrates significant bronchodilator activity while having a minimal impact on reducing arterial blood pressure. Due to its unique properties, BRL 55834 is a promising candidate for research applications related to respiratory therapies and the modulation of vascular tone. -
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.
