Membrane Transporters-Ion Channels

Items 1401-1450 of 2532

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  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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