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IKr Channel Blocker
Sematilide hydrochloride is a selective blocker of the IKr channel, primarily involved in cardiac repolarization. It exhibits a concentration-dependent inhibition of the delayed rectifier K+ current, with an IC50 value of 25 μM. As a class III antiarrhythmic agent, sematilide is utilized in research to study heart rhythm disorders and the underlying mechanisms of arrhythmias. -
Antihypertensive Agent
Tripamide is an orally active sulfonamide-derived diuretic that primarily functions as an antihypertensive agent. It inhibits renal reabsorption of sodium and chloride, promoting diuresis and reducing blood pressure. This compound is utilized in research to investigate mechanisms of hypertension and fluid balance, making it relevant for cardiovascular studies and the development of novel antihypertensive therapies. -
TMEM175 Modulator
TMEM175 Modulator 1 is a selective modulator of the lysosomal potassium ion channel TMEM175. This compound exhibits significant activity in regulating ion transport, making it a valuable tool for investigating neurodegenerative diseases such as Parkinson's disease, dementia, and Alzheimer's disease. Additionally, it may be useful in studying L-DOPA-induced dyskinesia, providing insights into the underlying mechanisms of these conditions. -
Kv7 Channel Opener
IDOR-1104-0086 is an orally active Kv7 channel opener, demonstrating an EC50 of 210 nM and the ability to cross the blood-brain barrier. This compound exhibits strong selectivity against the hERG channel, with an IC20 of 25 μM. IDOR-1104-0086 has shown efficacy in rodent models of epilepsy and possesses a favorable tolerability profile, making it a valuable tool for research in epilepsy and related neurological disorders. -
TREK-1 Inhibitor
TKIM is a selective inhibitor of the TREK-1 channel, exhibiting an IC50 of 2.96 μM. By binding to the pocket of the intermediate (IM) state of TREK-1, TKIM modulates ion channel activity. This compound is valuable for investigations into the physiological roles of TREK-1 in neurobiology and cardiovascular research, as well as potential therapeutic applications in pain and mood disorders. -
Kv3.1 Channels Modulator
Kv3.1 modulator 2 is a selective modulator of Kv3.1 ion channels, exhibiting an EC50 value of 68 nM. This compound enhances the activity of Kv3.1 channels, which are crucial for neuronal action potential firing and synaptic transmission. It serves as a valuable tool for research exploring excitability in neuronal systems and the role of Kv3.1 channels in neurological conditions. -
Potassium Channel Chemical
PBFI-AM is a potassium channel-sensitive fluorescent indicator that selectively binds to intracellular potassium ions (K+). This compound is primarily utilized to measure and analyze intracellular K+ concentrations within various cell types. It serves as a valuable reagent in studies involving ion channels, cellular signaling, and physiological responses to changes in potassium levels. -
Potassium Channel Activator
SKA-111 is a selective activator of the potassium channel KCa 3.1, promoting membrane hyperpolarization in porcine endothelial cells. This compound enhances Bradykinin induced coronary dilations in isolated rat heart models. SKA-111 is valuable for cardiovascular disease research, particularly in studies exploring potassium channel modulation and endothelial function.
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hERG Channel Blocker
L-706000 free base is a potent hERG channel blocker, exhibiting an IC50 of 32 nM. This compound functions as a class III antiarrhythmic agent and is valuable for studying malignant ventricular tachyarrhythmias. Its ability to selectively inhibit hERG channels makes it an important tool for cardiovascular research and drug development focusing on arrhythmia mechanisms. -
KV1.3 Inhibitor
KV1.3-IN-1 is a selective inhibitor of the KV1.3 potassium channel, exhibiting IC50 values of 230 nM in Ltk cells and 26.12 nM in PHA-activated T-lymphocytes. This compound disrupts intracellular Ca2+ signaling, leading to notable inhibition of T-cell activation, proliferation, and colony formation. KV1.3-IN-1 is an essential tool for research on T-cell biology and the modulation of immune responses. -
TASK-1 channels blocker, IKur blocker
A1899 is a selective blocker of the two-pore potassium channel TASK-1, exhibiting IC50 values of 35.1 nM in oocytes and 7 nM in CHO cells. Additionally, A1899 functions as an IKur blocker, making it a valuable tool in the study of cardiac electrophysiology and related cardiovascular diseases. Its potency and specificity allow for detailed investigation into the physiological roles of potassium channels in cellular and cardiovascular research. -
IKCa Blocker
TRAM-39 is a selective inhibitor of intermediate conductance Ca2+-activated K+ (IKCa) channels, specifically targeting the KCa3.1 channel with an IC50 value of 60 nM. This compound is valuable for investigating various neurological conditions, including ataxia, epilepsy, memory disorders, schizophrenia, and Parkinson’s disease. Its ability to modulate IKCa channels makes it a useful tool for studying calcium signaling pathways and their implications in related pathologies. -
TREK Inhibitor
ONO-TR-772 is a selective TREK inhibitor with an IC50 value of 15 nM. This compound has been shown to enhance recognition memory in the MK-801-stimulated novel object recognition (NOR) mouse model. ONO-TR-772 is valuable in research pertaining to cognitive impairment and related neurological diseases. -
Antiarrhythmic Agent
(-)-Sotalol is an antiarrhythmic agent that primarily inhibits the hERG potassium channel, demonstrating a Kd of 0.60 μM. This compound is utilized in research focused on cardiac arrhythmias, providing insights into mechanisms of cardiac rhythm regulation. Its efficacy as a hERG inhibitor makes it a valuable tool for investigating arrhythmogenic conditions and potential therapeutic interventions. -
KV7 Activator/NaV Inhibitor
E0199 is a potent dual-target KV7 activator and NaV inhibitor, specifically enhancing KV7.2/7.3 (EC50 = 12.78 nM), KV7.2 (EC50 = 0.50 μM), and KV7.5 (EC50 = 27.14 nM) channels while inhibiting NaV1.7 (IC50 = 0.52 μM), NaV1.8 (IC50 = 0.24 μM), and NaV1.9 (IC50 = 0.16 μM) channels. This compound demonstrates significant analgesic properties in a chronic constriction injury mouse model, effectively managing neuropathic pain without adversely impacting cardiac and skeletal muscle ion channels. E0199 serves as a valuable tool for research in neuropathic pain mechanisms and therapeutic strategies. -
hERG K+ Channel Activator
AZSMO-23 is a potent activator of the hERG K+ channel, demonstrating effective modulation of wild-type hERG pre-pulse and tail currents with EC50 values of 28.6 µM and 11.2 µM, respectively. This compound is particularly relevant for studies investigating long QT syndrome, offering insights into cardiac repolarization and related disorders. Researchers can utilize AZSMO-23 to explore the therapeutic potential and underlying mechanisms of hERG channel dysfunction. -
Potassium Channel Inhibitor
VU625 is a selective inhibitor of the inward rectifier potassium channel 1 (AeKir) in the Aedes aegypti mosquito, exhibiting an IC50 of 96.8 nM in HEK293 cells. This compound demonstrates potential for development as a novel insecticide, targeting critical pathways in mosquito physiology. Its specificity for AeKir makes it a valuable tool for research aimed at controlling mosquito populations and studying potassium channel function. -
KV1.3 Inhibitor
cis-KV1.3-IN-1 is a selective inhibitor of the KV1.3 potassium channel, specifically designed to target this ion channel in cellular systems. At a concentration of 10 μM, cis-KV1.3-IN-1 demonstrates a 25.53% inhibition of KV1.3 activity in Xenopus oocytes expressing human hKV1.3. This compound is valuable for research into immunological responses and therapies, particularly in relation to autoimmune diseases where KV1.3 channels play a critical role. -
Stable Isotope
Gliclazide-d4 is a deuterated analog of Gliclazide, a recognized inhibitor of ATP-sensitive potassium channels in pancreatic beta cells. It exhibits biological activity as an antidiabetic agent with an IC50 of 184 nM, effectively regulating insulin secretion. Gliclazide-d4 is suitable for pharmacokinetic studies, metabolic research, and tracer studies in glucose homeostasis investigations. -
Potassium Channel Inhibitor
Charybdotoxin is a 37-amino acid peptide that selectively inhibits potassium channels. Its primary mechanism involves blocking voltage-gated K+ channels, leading to altered neuronal excitability and muscle contraction. This compound is useful in research applications focused on neurophysiology, cardiac function, and ion channel studies, providing insights into the role of potassium channels in physiological and pathological processes. -
Potassium Channel Opener
Foslevcromakalim is an ATP-sensitive potassium channel opener that induces vasodilation by promoting potassium efflux. This compound has demonstrated significant ocular hypotensive effects, making it a valuable tool for research on intraocular pressure regulation and related ocular conditions. Its primary applications include studies on glaucoma and other disorders where modulation of potassium channels plays a critical role in therapeutic strategies. -
ROMK Inhibitor
MK-8153 is a highly selective and orally active inhibitor of the renal outer medullary potassium channel (ROMK), demonstrating an IC50 of 5 nM for ROMK electrophysiology. This compound's potent inhibitory action makes it suitable for research applications related to diuresis and atriuresis. Its specificity towards ROMK provides a valuable tool for studying renal function and potassium homeostasis in various biological contexts. -
Potassium Channel Inhibitor
Guanfu base G is a potassium channel inhibitor derived from Aconitum coreanum. It effectively inhibits the HERG channel current, exhibiting an IC50 value of 17.9 μM. This compound is primarily utilized in research applications focused on cardiac arrhythmias and the modulation of ion channel activity. -
Potassium Channel Inhibitor
Allocryptopine is a potassium channel inhibitor, specifically targeting the human ether-a-go-go related gene (hERG) current. Derived from the plant Macleaya cordata, Allocryptopine exhibits antiarrhythmic properties that may be beneficial in cardiovascular research. Its ability to effectively block hERG channels positions it as a valuable reagent for studies investigating cardiac ion channel modulation and related disorders. -
Potassium Channel Blocker
5Me3F4AP is a potent potassium channel blocker, exhibiting an IC50 range of 220 μM to 693 μM depending on pH conditions from 6.4 to 9.1. This compound is notable for its ability to cross the blood-brain barrier, suggesting its potential utility in neurological research and imaging applications, such as positron emission tomography (PET). Researchers may find 5Me3F4AP valuable in studies aimed at understanding potassium channel functions and their role in various physiological and pathological processes. -
KCa2 Channel Inhibitor
AP14145 hydrochloride is a selective negative allosteric modulator of KCa2 channels, exhibiting an IC50 of 1.1 μM for both KCa2.2 (SK2) and KCa2.3 (SK3) channels. Its inhibitory action is significantly influenced by specific amino acids S508 and A533 within the channel structure. In preclinical models, AP14145 hydrochloride has been shown to prolong the atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic properties in a Vernakalant-resistant porcine model of atrial fibrillation, making it a valuable tool for studying cardiac electrophysiology and arrhythmia mechanisms. -
hERG Channel Activator
A-935142 is a potent activator of the human ether-a-go-go-related gene (hERG, Kv 11.1) channel. This compound modulates hERG current through a multifaceted mechanism, promoting activation, diminishing inactivation, and decelerating deactivation. A-935142 is crucial for studies investigating cardiac repolarization processes and the pharmacological modulation of ion channels associated with arrhythmias. -
Ventilatory Stimulant
Doxapram hydrochloride is a ventilatory stimulant that primarily functions as an inhibitor of TASK (Tandem Pore) potassium channels. It specifically inhibits TASK-1 and TASK-3 channels, exhibiting EC50 values of 410 nM and 37 nM, respectively, and also affects TASK-1/TASK-3 heterodimer channels with an EC50 of 9 μM. This compound is valuable for research applications focused on respiratory stimulation, particularly in the study of apnea in preterm infants. -
TASK-1 Inhibitor
TASK-1-IN-1 is a potent and selective inhibitor of the TASK-1 potassium channel, exhibiting an IC50 of 148 nM. It demonstrates reduced inhibition of the TASK-3 channel with an IC50 of 1750 nM and minimal impact on other K+ channels. This compound is primarily used in cancer research, exhibiting potential anticancer properties through modulation of potassium ion currents. -
TRPV4-KCa2.3 Interaction Enhancer
JNc-440 is a TRPV4-KCa2.3 interaction enhancer with significant potential as an antihypertensive agent. This compound promotes the interaction between the transient receptor potential vanilloid 4 (TRPV4) and the calcium-activated potassium channel 3 (KCa2.3) in endothelial cells, resulting in enhanced vasodilation. Furthermore, JNc-440 demonstrates effective antihypertensive properties in murine models, making it a valuable tool for cardiovascular research. -
Kv1.5 Inhibitor
MK-0448 is a selective inhibitor of the voltage-gated potassium channel Kv1.5. It demonstrates significant biological activity by modulating ion channel activity, which is vital in the study of cardiac electrophysiology. This compound is primarily utilized in research examining atrial fibrillation and other related cardiac arrhythmias. -
KV2.1/KV2.2 Channels Blocker
Guangxitoxin 1E selectively targets and inhibits KV2.1 and KV2.2 channels with an IC50 of 1-3 nM, making it a potent blocker of these potassium channels. These channels are involved in the generation of delayed-rectifier potassium currents in various neuronal types. Guangxitoxin 1E is primarily used in research applications focused on elucidating the physiological roles of KV2 channels and assessing their contributions to neuronal excitability and signaling pathways. -
Potassium Channel Activator
Carabersat is a potent activator of potassium channels, playing a critical role in regulating neuronal excitability. This compound has demonstrated significant anticonvulsant properties, making it valuable in the study of seizure disorders. Its ability to modulate ion channel activity aids in exploring therapeutic interventions for epilepsy and related neurological conditions. -
Potassium Channel Inhibitor
Phrixotoxin-1 is a selective peptide inhibitor targeting the Kv4 potassium channel. Derived from the venom of the theraphosid spider Phrixotrichus auratus, it exhibits potent biological activity in the modulation of potassium ion flow. This reagent is valuable for research applications involving neuronal excitability and cardiac function, providing insight into the roles of Kv4 channels in various physiological and pathological processes. -
Kv11.1 Inhibitor
LUF7346 is a potent inhibitor of the Kv11.1 (hERG) channel, acting as a negative allosteric modulator with an IC50 value of 35.6 ± 3.2 nM. This compound can be utilized in research focused on cardiac ion channel function, arrhythmias, and drug-induced QT interval prolongation. Its specificity makes it a valuable tool for investigating hERG channel-related therapeutic interventions and understanding associated physiological effects. -
Potassium Channel Inhibitor
Spinoxin is a 34-residue peptide neurotoxin derived from the venom of the scorpion Heterometrus spinifer and is classified as a Kv1.3 potassium channel inhibitor. With an IC50 of 63 nM, Spinoxin exhibits strong potency in inhibiting Kv1.3, making it a valuable tool in research related to autoimmune disorders and cancer therapies. Its unique structure, stabilized by four disulfide bridges, enhances its relevance in exploring the role of potassium channels in various biological processes. -
Potassium Channel Inhibitor
4-trans-Hydroxy-glibenclamide is a potent inhibitor of the SUR1/Kir6.2 potassium channels. As an active metabolite of the sulfonylurea inhibitor glyburide, it effectively disrupts glyburide binding to rat brain synaptosomes, exhibiting IC50 values of 0.95 nM and 100 nM at high and low affinity sites, respectively. This compound is valuable for research applications focused on investigating the physiological and pharmacological roles of potassium channels in cellular processes and metabolic disorders. -
Potassium Channel Blocker
Chlorahololide C is a lindenane sesquiterpenoid dimer that acts as a potent and selective blocker of potassium channels, exhibiting an IC50 value of 3.6 μM. This compound is derived from Chloranthus holostegius and is valuable for research into potassium channel function and related signaling pathways. Its selective inhibition makes it a useful tool for investigating the role of potassium channels in physiological and pathological processes. -
Maxi-K Channels Activator
Dehydrosoyasaponin I is a potent activator of maxi-K channels, functioning as a calcium-activated potassium channel modulator. This triterpene glycoside has a reversible action, making it a valuable tool for studying ionic transport and cellular excitability. Its unique properties make Dehydrosoyasaponin I useful in various research applications, particularly in cardiovascular and neuromuscular studies. -
Stable Isotope
(Rac)-Ropivacaine-d7 is a deuterium-labeled analogue of (Rac)-Ropivacaine, a local anesthetic that primarily acts by blocking voltage-gated sodium channels. This stable isotope is valuable in pharmacokinetic studies and metabolic research, enabling researchers to investigate the drug's distribution, metabolism, and elimination in biological systems. The incorporation of deuterium enhances the sensitivity and specificity of analytical methods such as mass spectrometry. -
Maxi Calcium-activated Potassium Channel Blocker
1,12-Dodecanediamine (1,12-DD) is a reversible blocker of Maxi calcium-activated potassium channels. It effectively diminishes single-channel current amplitude, mean channel open time, and overall channel open probability. This compound is valuable for studies involving cellular electrical signal transduction mechanisms, allowing researchers to explore the role of these channels in various physiological and pathological processes. -
Kv7.4 Agonist
Bimokalner is a selective agonist of the voltage-gated potassium channel Kv7.4. It is known to enhance Kv7.4 channel activity, leading to hyperpolarization of neuronal membranes and potential modulation of neuronal excitability. This compound is valuable in research focused on neurophysiology, cardiovascular function, and the pharmacological modulation of ion channels. -
Kv1.5 Potassium Channel Inhibitor
DDO-02005 is a potent inhibitor of the Kv1.5 potassium channel, exhibiting an IC50 value of 0.72 μM. This compound demonstrates notable anti-atrial fibrillation effects in a CaCl2-ACh-induced AF rat model and showcases effective anti-arrhythmic activity against aconitine-induced arrhythmias. DDO-02005 serves as a valuable tool for research into cardiac electrophysiology and potential therapeutic strategies for arrhythmia management. -
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. -
HCN2 Inhibitor
HCN2 modulator-8 is a selective inhibitor of the HCN2 channel, classified as a pyrazolopyridine derivative. It exhibits significant activity in modulating hyperalgesic and sensory signaling pathways, making it valuable for research into pain management, tinnitus, and various central nervous system disorders, including psychiatric and mood disorders. -
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.

