Catalog No.
Product Name
Application
Product Information
Citations
-
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. -
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
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. -
Potassium Channel Agonist
SR 47063 is an ATP-sensitive potassium channel (KATP) agonist that selectively activates KATP channels in vascular smooth muscle cells, exhibiting an IC50 of 8.1 nM in human saphenous vein and 3.86 nM in rat aorta. By promoting potassium efflux and inducing cellular hyperpolarization, SR 47063 facilitates vasorelaxation. This compound is valuable for research into hypertension and associated cardiovascular disorders. -
Antiarrhythmic Agent
Dofetilide N-oxide is a metabolite of the class III antiarrhythmic agent Dofetilide, primarily targeting potassium channels. Its mechanism involves the inhibition of potassium ion movement, which plays a crucial role in the regulation of cardiac action potentials. This compound is utilized in research to study cardiac arrhythmias and the therapeutic potential of potassium channel blockers in managing cardiovascular diseases. -
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. -
Potassium Channel Blocker
Chlorahololide D is a selective potassium channel blocker with an IC50 value of 2.7 μM. Derived from the whole plant of Chloranthus holostegius, this natural product exhibits significant biological activity in modulating potassium ion flow. It is valuable for research applications investigating ion channel physiology and the pharmacological modulation of excitability in various cell types. -
Potassium Channel
NS4591 is a modulator of calcium-activated potassium channels, specifically enhancing the activity of small conductance (SK) and intermediate conductance (IK) potassium channels. It significantly increases IK-mediated currents at approximately 45 nM and SK3-mediated currents at about 530 nM in whole-cell patch-clamp studies. NS4591 has been shown to inhibit action potentials induced by suprathreshold depolarizing pulses in acutely isolated bladder primary afferent neurons and reduces carbamylcholine-induced detrusor contraction in the rat bladder, indicating its sensitivity to apamin. This reagent is useful for studying the physiological roles of potassium channels in bladder function and neuronal excitability. -
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. -
Potassium Channel
ZD0947 is an ATP-sensitive potassium channel activator that primarily targets smooth muscle KATP channels (SUR2B/Kir6.1 and SUR2B/Kir6.2). It is known to partially antagonize pancreatic KATP channels (SUR1/Kir6.2) and cardiac KATP channels (SUR2A/Kir6.2). This compound shows potential for research applications in inhibiting overactive bladder (OAB) and exploring potassium channel functions in various physiological and pathological processes. -
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. -
Kv7.2/Kv7.3 Modulator
Kv7.2/Kv7.3 modulator-1 is an effective modulator of the Kv7.2 and Kv7.3 potassium channels, exhibiting a pEC50 of 7.96 for channel opening activity. This reagent plays a critical role in studying neurological conditions, including epilepsy, depression, brain injury, and pain mechanisms. Its ability to selectively influence these ion channels offers valuable insights into potential therapeutic strategies in the treatment of various neuropsychological disorders. -
Kv7 Potassium Activator
Kv7 activator-2 is a selective activator of Kv7 potassium channels. It enhances neuronal excitability and has demonstrated potential in the study of neurological disorders, especially epilepsy. This compound serves as a valuable tool for investigating the modulation of neuronal signaling and the therapeutic strategies targeting Kv7 channels in various neurological conditions. -
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. -
KCNQ2 Activator
QO-83 is a potent activator of the KCNQ2 (Kv7.2) voltage-gated potassium channel, exhibiting an EC50 of 0.56 μM. It binds to a specific hydrophobic pocket within the KCNQ2-CaM complex in its closed conformation, resulting in a negative shift in the voltage-dependent activation curve. This mechanism enhances the voltage sensitivity of KCNQ2 channels. QO-83 is a valuable tool for research into the mechanisms underlying epilepsy and related ion channel disorders. -
Potassium Channel Blocker
δ-Dendrotoxin is a potent potassium channel blocker derived from the venom of the black mamba snake. This compound is utilized in research focused on neurological diseases, aiding in the understanding of ion channel function and its implications in neuronal excitability. Its ability to modulate potassium channels makes it a valuable tool for investigating potential therapeutic targets in various neurological disorders. -
Potassium Channel Blocker
WAY-123223 is an orally active blocker of potassium channels, specifically targeting cardiac ion currents. This compound prolongs transmembrane action potential duration and the cardiac refractory period in canine Purkinje fibers, enhancing the ventricular fibrillation threshold and facilitating the restoration of sinus rhythm from ventricular fibrillation. WAY-123223 is valuable for researching cardiovascular diseases, particularly in the study of arrhythmias and their treatment. -
TREK Activator
CAT335 is a selective and irreversible activator of the TREK-1 channel. This compound enhances TREK-1 activity, making it useful for investigating the underlying mechanisms of pain sensation, the regulation of sleep, and the modulation of intraocular pressure. Its specific action on TREK-1 allows for targeted research applications in neurobiology and ocular physiology. -
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. -
Antihypertensive Agent
Celikalim is an antihypertensive agent that primarily acts by opening potassium channels in vascular smooth muscle, resulting in a reduction in blood pressure. In addition to its vasodilatory effects, Celikalim exhibits the ability to inhibit white thrombus formation. This compound serves as a potent potassium channel opener in canine models and is valuable for research related to thrombosis. -
hERG Channel Activator
PD-307243 is a specific activator of the human Ether-à-go-go-Related Gene (hERG) potassium channel. It is primarily utilized in studies related to cardiac arrhythmias, aiding in the examination of hERG channel function and its implications in heart rhythm disorders. This compound serves as a valuable tool for investigating the pharmacological modulation of ion channels in cardiovascular research. -
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. -
Delayed Rectifier Potassium Current Blocker
WAY-125971 is a potent blocker of the delayed rectifier potassium current (IK), functioning as a propylamine analogue. This compound exhibits a high degree of specificity in its action, making it a valuable tool for investigating the mechanisms underlying arrhythmias. Its utility in electrophysiological studies aids in understanding cardiac ion channel dynamics and potential therapeutic targets for heart rhythm disorders. -
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. -
KV11.1 Channel Activator
VU0405601 is a potent activator of the KV11.1 ion channel, which plays a crucial role in cardiac repolarization. This compound has demonstrated the ability to protect cardiac tissue from dofetilide-induced ventricular tachycardia, making it valuable for research into arrhythmias and cardiac safety. Its mechanism of action positions it as a significant tool for studying cardiac electrophysiology and developing therapeutic strategies for related heart conditions. -
K+ Channel Opener
ZM226600 is an ATP-sensitive potassium channel opener with an EC50 of 500 nM. This compound effectively inhibits spontaneous activity in bladder tissues, making it a valuable tool for studying bladder function and disorders. Its ability to modulate potassium channels can offer insights into various physiological processes and potential therapeutic approaches in urology research. -
KCa2 Channel Modulator
KCa2 Channel Modulator 2 is a potent positive modulator of the KCa2 channel subtypes, specifically targeting KCa2.2a and KCa2.3. This compound demonstrates comparable efficacy with EC50 values of 0.64 μM for rat KCa2.2a and 0.60 μM for human KCa2.3 channels. Its selective modulation makes it suitable for investigations into the physiological roles of KCa2 channels and their potential implications in therapeutic applications related to calcium signaling and excitability in various tissues. -
Kv7.2/Kv7.3 Activator
Kv7.2/Kv7.3 activator-4 is a selective activator of the Kv7.2 and Kv7.3 potassium channels. It enhances neuronal excitability, making it a valuable tool in research related to epilepsy and neuropathic pain, as well as other neurological disorders. This compound aids in the investigation of Kv7 channel modulation, contributing to understanding their roles in various pathophysiological conditions. -
Antiarrhythmic Agent
L-702958 is a potent blocker of the human ether-à-go-go-related gene (hERG) potassium channel with an IC50 of 14.3 nM. This compound exhibits significant antiarrhythmic activity, making it valuable for research into the mechanisms underlying arrhythmias and potential therapeutic applications. L-702958 is essential for studies focused on cardiac electrophysiology and ion channel modulation. -
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. -
Insulinotropic Agent/K+ Channel Blocker
BTS-67582 is an orally active nonsulfonylurea insulinotropic agent that functions as a potassium channel blocker, specifically targeting the K+ ATP channel in pancreatic islet cells through a distinct binding site compared to sulfonylureas. This compound exhibits significant antidiabetic activity, making it valuable for research applications aimed at understanding insulin secretion and glucose homeostasis. Its unique mechanism offers insights into alternative strategies for diabetes treatment. -
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. -
TREK-1/TREK-2 Channel activator
C3001a is a selective activator of the TREK-1 and TREK-2 potassium channels, exhibiting EC50 values of 12.81 μM and 11.31 μM, respectively. This compound specifically interacts with the cryptic binding site formed by P1 and TM4 in TREK-1, with no impact on other two-pore domain K+ channels. C3001a is applicable in research exploring pain mechanisms and pancreatitis.
