Potassium Channels

Items 101-150 of 501

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  1. KCC2 activator

    CLP290 is an orally available activator of the neuron-specific K+-Cl? cotransporter KCC2, displays potential for treatment of a wide range of neurological and psychiatric indications.
  2. KCC2 antagonist

    VU0463271 is a potent KCC2 antagonist, with an IC50 of 61 nM.
  3. hERG channel activator

    PD-118057 is a human ether-a-go-go-related gene (hERG) channel activator that does not cause hERG blockade.
  4. BKCa channel opener

    BMS-191011 (BMS-A) is an opener of the large-conductance, Ca2++-activated potassium (maxi-K) channel, effective in stroke models.
  5. sAHP channel blocker

    UCL 2077 is a selective slow-afterhyperpolarization (sAHP) channel blocker (IC50 = 500 nM in hippocampal neurons in culture), having minimal effects on Ca2+ channels, action potentials, input resistance and the medium after hyperpolarization.
  6. KV7 channel blocker

    DMP-543 (XR-543) is a KV7 channel blocker, also acts as a potent neurotransmitter release enhancer.
  7. ROMK inhibitor

    VU591 hydrochloride is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM.
  8. K+ channel opener

    Y-27152, a prodrug of the KATP (Kir6) channel opener Y-26763, is a long-acting K+ channel opener with less tachycardia: antihypertensive effects in hypertensive rats and dogs in conscious state.
  9. Kv7 (KCNQ) channels blocker

    XE 991 dihydrochloride, a Kv7 (KCNQ) channels blocker, potently inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channel, and M-current with IC50s of 0.75 ?M, 0.71 ?M, 0.6 μM, and 0.98 ?M, respectively.
  10. KATP channel activator

    P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation.
  11. Kv7.2/Kv7.4 channels activator

    ML213 is a selective activator of Kv7.2 and Kv7.4 channels, enhances Kv7.2 and Kv7.4 channels with EC50s of 230 and 510 nM, respectively.
  12. Cl- conductance/hKCa3.1 channel activator

    DCEBIO, a derivative of 1-EBIO, is an extremely potent activator of Cl?? secretion in T84 colonic cells.
  13. potassium channel blocker

    Almokalant is a class III antiarrhythmic drug, acts as a potassium channel blocker, and inhibits a specific component (Ikr) of the time-dependent delayed rectifier K+ current.
  14. KCa3.1 activator

    SKA-121 is a selective KCa3.1 activator. SKA-121 exhibits EC50s of 109 nM and 4.4 μM for KCa3.1 and KCa2.3, respectively.
  15. IKs blocker

    HMR 1556, a chromanol derivative, is a IKs blocker with IC50s of 10.5 nM and 34 nM in canine and guinea pig left ventricular myocytes, respectively.
  16. cyanoguanidine KATP opener

    Naminidil is a cyanoguanidine KATP opener.
  17. IK blocker

    AM-92016 hydrochloride is a specific blocker of rectifier potassium current (IK).
  18. intravenous BKCa-channel blocker

    GAL-021 a new intravenous BKCa-channel blocker.
  19. potassium channel blocker

    VU0134992 is a selective inward rectifier potassium (Kir) channel Kir4.1 blocker with an IC50 of 0.97 ?M.
  20. Kv3 potassium channel modulator

    AUT1 is a Kv3 potassium channel modulator with pEC50s of 5.33 and 5.31 for human recombinant Kv3.1b and Kv3.2a, respectively, exhibits 10-fold lower potency at human recombinant Kv3.3 channel (pEC50, 4.5).
  21. L-Palmitoylcarnitine is a fatty acid metabolite.
  22. Iron mobilizer

    Guanosine 5'-diphosphate is a nucleoside diphosphate. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulating the interleukin-6 (IL-6)/stat-3 pathway.
  23. Kv3.1/Kv3.2 modulator

    Kv3 modulator 4 is a Kv3.1 (pEC50=5.45) and Kv3.2 modulator extracted from patent WO2018020263A1, Cyclobutyl structure.
  24. Kv3.1/Kv3.2/Kv3.3 channels modulator

    Kv3 modulator 3 (Compound 4) is a selective modulator of Kv3.1 and/or Kv3.2 and/or Kv3.3 channels extracted from patent WO2017098254A1, compound 4, has analgesic activity for use in the prophylaxis o or treatment of pain.
  25. VRAC inhibitor

    DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC), voltage-dependently activates potassium channels TREK1 and TRAAK, inhibits TRESK, TASK1 and TASK3 (IC50s, 0.14, 0.95, 50.72 μM, respectively).
  26. Kv3 voltage-gated potassium channel modulator

    Kv3 modulator 1 is a Kv3 voltage-gated potassium channel modulator extracted from patent WO2018020263A1, Compound X. Kv3 modulator 1 can be used to treat inflammatory pain.
  27. 20-HETE is a potent vasoconstrictor produced in vascular smooth muscle (VSM) cells.
  28. Potassium channel blocker

    Cesium chloride is a potassium channel blocker; inhibits the pacemaker current (If) and the hyperpolarization-activated cationic current (Ih). Prevents activation of caspase-3 and neuronal apoptosis in serum- and potassium-deprived cerebellar granule neurons by inactivating GSK-3β.
  29. hERG1 potassium channel activator

    KB130015 is a novel activator of hERG1 potassium channels, blocking native and recombinant hERG1 channels at high voltages, but activating them at low voltages.
  30. KV7.2/7.3 activator

    ICA-110381 is a KV7.2/7.3 activator with EC50 of 0.38 uM.
  31. 5-HT3 receptor inhibitor

    Eucalyptol is a bicyclic monoterpene that has been found in Eucalyptus and other plants. It is an inhibitor of 5-HT3 receptor ,potassium channel, TNF-α and IL-1β.
  32. Nucleotide Analogue

    Uridine 5'-monophosphate disodium salt is a nucleotide analogue that activates mitochondrial ATP-dependent potassium channels, providing cardioprotective effects. This compound facilitates the synthesis of CDP-choline and induces apoptosis in intestinal epithelial cells, supporting gut development and reducing the incidence of diarrhea. It serves as a valuable tool for studies related to cardiac health and gastrointestinal function.
  33. Calcium Sensitiser

    OR-1896 is a potent calcium sensitizer and active metabolite of Levosimendan, primarily targeting phosphodiesterase (PDE) III isoforms. It exhibits significant vasodilatory effects and can activate ATP-sensitive potassium channels, enhancing calcium sensitivity. OR-1896 has been shown to reduce cardiomyocyte apoptosis, alleviate cardiac remodeling, and mitigate myocardial inflammation, making it valuable for research in cardiovascular disease therapies.
  34. Kv2.1 Inhibitor

    Kv2.1-IN-1 is a selective inhibitor of the Kv2.1 potassium channel, demonstrating a potent inhibitory activity with an IC50 of 0.07 μM. It exhibits over 130-fold selectivity against other potassium, sodium, and calcium channels. Kv2.1-IN-1 has been shown to reduce H2O2-induced apoptosis in HEK293 cells and provides significant neuroprotective effects in models of middle cerebral artery occlusion (MCAO) in rats. This compound is useful for research into ischemic stroke and related neurological conditions.
  35. Potassium Binder

    Patiromer is a selective, non-absorbable intestinal potassium binder that targets potassium ions through a reversible exchange with calcium ions. It effectively lowers serum potassium levels while promoting fecal potassium excretion and reducing serum aldosterone levels. Patiromer is utilized in research on hyperkalemia associated with conditions such as chronic kidney disease, diabetes, and heart failure, and is particularly beneficial in studies aimed at enhancing the efficacy of renin-angiotensin-aldosterone system inhibitor (RAASi) therapies.
  36. Antiarrhythmic Agent

    Quinidine gluconic acid is an antiarrhythmic agent primarily targeting potassium channels, exhibiting an IC50 of 19.9 μM. This compound is a potent, orally active inhibitor of cytochrome P450 enzymes and has been shown to induce apoptosis in certain cell types. Quinidine gluconic acid is utilized in research related to cardiac arrhythmias as well as malaria studies, providing valuable insights into these complex biological processes.
  37. SERT/NET Inhibitor

    Amitriptyline is a tricyclic antidepressant that primarily inhibits the serotonin transporter (SERT) and norepinephrine transporter (NET), enhancing synaptic levels of serotonin and norepinephrine. With a Ki value of 3.45 nM for SERT and 13.3 nM for NET, Amitriptyline demonstrates significant antidepressant activity. Additionally, it exhibits agonistic properties at α2A adrenergic and TrkA/TrkB receptors, contributing to its analgesic and neurotrophic effects. Furthermore, Amitriptyline interacts with various receptors, including muscarinic cholinergic and H1 receptors, which may lead to a variety of side effects, while its ability to block sodium channels and hERG potassium channels raises concerns regarding cardiotoxicity.
  38. Stable Isotope

    Hydrochlorothiazid-d2 is the deuterated form of Hydrochlorothiazide, a thiazide diuretic known for its role in inhibiting the transforming growth factor-beta (TGF-β)/Smad signaling pathway. This compound exhibits direct vascular relaxation by activating calcium-activated potassium channels, contributing to its antihypertensive properties. Hydrochlorothiazid-d2 is valuable in research applications involving the study of cardiovascular function, fibrosis reduction, and the overall effects of diuretics on systemic blood pressure regulation.
  39. Stable Isotope

    Hydrochlorothiazid-13C,d2 is a stable isotope-labeled form of Hydrochlorothiazide (HCTZ), a thiazide diuretic that functions by inhibiting the TGF-β/Smad signaling pathway. This compound exhibits direct vascular relaxant effects through the activation of calcium-activated potassium channels. Hydrochlorothiazide is primarily utilized in research to improve cardiac function, reduce fibrosis, and exhibit antihypertensive properties, making it a valuable tool for studies on cardiovascular health and hypertension management.
  40. Stable Isotope

    Hydrochlorothiazide-15N2,13C,d2 is a stable isotope-labeled derivative of hydrochlorothiazide, incorporating 15N and deuterium for enhanced tracking in metabolic studies. As a thiazide diuretic, hydrochlorothiazide inhibits the TGF-β/Smad signaling pathway, which plays a crucial role in cardiovascular remodeling. This compound exhibits direct vascular relaxation by activating calcium-activated potassium channels, thereby improving cardiac function, reducing fibrosis, and delivering antihypertensive effects. It is ideal for research applications focusing on cardiovascular health and the mechanisms of diuretic therapy.
  41. Autophagy Inducer

    Diazoxide is an ATP-sensitive potassium channel activator that induces autophagy through modulation of cellular ion balance. This compound demonstrates potential therapeutic effects in conditions related to hyperinsulinism. It is commonly utilized in research applications focusing on autophagy pathways and metabolic regulation.
  42. Kir2.1 Agonist

    Tetramisole hydrochloride is a selective inward rectifier potassium channel agonist that primarily targets the Kir2.1 subunit with an EC50 of approximately 30 μM. This compound plays a crucial role in promoting Kir2.1 channel functioning, hyperpolarizing the resting potential, and shortening action potential duration. Additionally, it exhibits effects on intracellular calcium regulation while influencing PKA signaling, contributing to its anti-arrhythmic and anti-myocardial remodeling properties. Tetramisole hydrochloride is valuable for investigations in cardiac electrophysiology, as well as studies focused on myocardial ischemia and heart failure.
  43. KATP Inhibitor

    Tolbutamide is an orally active KATP inhibitor that primarily targets ATP-sensitive potassium channels. It is known to inhibit cell proliferation and stimulate the exocytosis of glucagon, while also reducing fetal lethality in murine models. This compound is utilized in diabetes research to explore mechanisms of insulin secretion and glucose metabolism.
  44. 5-HT(1A/B/D) Receptor Antagonist

    GSK-588045 is a potent antagonist of the 5-HT(1A/B/D) receptors, demonstrating a high degree of selectivity for these targets while sparing human ether-a-go-go related gene (hERG) potassium channels. This specificity makes GSK-588045 a valuable tool in the study of neurological disorders, particularly in the context of depression and anxiety research applications. Its unique profile can aid in elucidating the role of serotonin receptors in various neuropsychiatric conditions.
  45. Stable Isotope

    Uridine 5'-monophosphate-13C9,15N2 dilithium is a stable isotope-labeled form of uridine 5'-monophosphate, incorporating both 13C and 15N isotopes. This compound acts as an orally active mitochondrial ATP-dependent potassium channel activator, demonstrating cardioprotective effects. Additionally, uridine 5'-monophosphate promotes the synthesis of CDP-choline and induces apoptosis in intestinal epithelial cells, making it valuable for research in gut development and in studies related to gastrointestinal health.
  46. CO Donor

    Tricarbonyldichlororuthenium(II) dimer serves as a carbon monoxide (CO) donor, facilitating various biological processes. This compound demonstrates notable anti-inflammatory and antioxidant properties, in addition to its protective effects on gastric mucosa. Furthermore, Tricarbonyldichlororuthenium(II) dimer exhibits CO-independent effects on several potassium channels, highlighting its significance in cellular physiology and potential therapeutic applications.
  47. Antiarrhythmic Agent

    Quinidine sulfate is an antiarrhythmic agent that primarily targets cardiac ion channels, particularly potassium channels. It exhibits potent K+ channel blocking activity with an IC50 of 19.9 μM and has been shown to induce apoptosis in various cell types. Additionally, quinidine sulfate is utilized in malaria research, making it valuable for studies related to both cardiovascular and infectious diseases.
  48. Antiarrhythmic Agent

    Quinidine polygalacturonate is an antiarrhythmic agent that primarily targets potassium channels, exhibiting an IC50 of 19.9 μM. It also functions as a selective inhibitor of cytochrome P450db and has the capability to induce apoptosis. This compound is particularly useful in research focused on cardiac arrhythmias and malaria studies, making it a valuable reagent for pharmacological investigations.
  49. Vasodilator

    KMUP-1 is a xanthine derivative that acts as a vasodilator through the inhibition of phosphodiesterase (PDE) and activation of soluble guanylyl cyclase (sGC). It stimulates the nitric oxide/sGC/cyclic GMP signaling pathway and facilitates the opening of potassium channels. Additionally, KMUP-1 has been shown to reduce ischemia-induced cardiomyocyte apoptosis. This compound is relevant for studies in cardiovascular health and anti-inflammatory research.
  50. Potassium Channel Inhibitor

    DPO-1 is a selective inhibitor of Kv1.5 and Kv1.3 potassium channels (EC50 = 3.1 μM) with notable immunomodulatory and anti-inflammatory properties. It effectively reduces Kv1.3 current density, diminishes Ca2+ influx in calcium-depleted Jurkat cells, and inhibits IL-2 secretion in activated Jurkat cells. Additionally, DPO-1 obstructs uric acid sodium (MSU)-induced NLRP3 inflammasome activation by interfering with Kv1.5-mediated K+ efflux. This reagent is valuable for research into immunological disorders and atrial fibrillation.

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