Potassium Channels

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  1. Antimalarial

    Quinine is a primary alkaloid of various species of Cinchona, optical isomer of Quinidine and an anti-malarial, skeletal, muscle relaxant.
  2. sodium-potassium pump inhibitor

    Digoxin is a sodium-potassium pump inhibitor.
  3. Ion channel blocker

    Vernakalant Hcl is an investigational mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg and may be more atrial-selective than available agents; in treatment of antiarrhythmic.
  4. Kir7.1 potassium channels blocker

    ML418 is a selective, sub-micromolar pore blocker of Kir7.1 potassium channels. The inward rectifier potassium (Kir) channel Kir7.1 (KCNJ13) is a key regulator of melanocortin signaling in the brain, electrolyte homeostasis in the eye, and uterine muscle contractility during pregnancy.
  5. Kv1.3 blocker

    PAP-1 is a selective inhibitor of Kv1.3, voltage-gated potassium channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity.
  6. Potassium Channel Blocker

    TRAM-34 is a highly selective blocker of intermediate conductance Ca2+-activated K+ channels (KCa3.1) (Kd = 20 nM). Exhibits 200-1500-fold selectivity over KV, BKCa, KCa2, Na+, CRAC and Cl- channels. Suppresses the reactivation of lymphocytes by mitogenic stimuli.
  7. HIF-1α inhibitor

    Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.
  8. Kir6.2/SUR inhibitor

    Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus.
  9. K+ channel and CFTR Cl- channel blocker

  10. Hydralazine hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM.
  11. Minoxidil (U-10858) is a selective ATP dependent K+ (Kir6) channel activator.
  12. Nateglinide(Starlix) is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.
  13. Kir6 (KATP) channel opener

    Nicorandil (SG-75) is potassium channel activator.
  14. Potassium Channel inhibitor

    Repaglinide is a potent short-acting insulin secretagogue that acts by closing ATP-sensitive potassium (KATP) channels in the plasma membrane of the pancreatic beta cell.
  15. iron mobilizer

    Guanosine 5'-diphosphate disodium salt 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.
  16. KCa1.1 channels activator

    NS 11021 is a potent and specific Ca2-activated big-conductance K?? Channels (KCa1.1 channels) activator.
  17. TASK1(KCNK3) inhibitor

    ML365 is a novel selective small molecule inhibitor of TASK1(KCNK3) with IC50 of 4 nM(thallium influx fluorescent assay) and 16 nM(automated electrophysiology assay).
  18. KCNQ1 potassium channel activator

    ML277(CID53347902) is a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator with EC50 of 270 nM.
  19. non-narcotic antitussive

    Tipepidine hydrochloride, a non-narcotic antitussive, exerts an antidepressant-like effect.
  20. OPRM1/OPRD1 agonist

    ML335 (CYM 51010, CID-23723457) is an agonist for OPRM1(μ-opioid receptor)-OPRD1(δ-opioid receptor) heterodimerization with EC50 of 403 nM demonstrating selectivity over the individual OPRM1 and OPRD1 receptors and the serotonin HT5A receptor with EC50 of 14.9 μM, 1.1 μM, and >40 μM, respectively.
  21. Eleclazine, also known as GS-6615, is a selective late sodium current inhibitor. Eleclazine is potentially useful for treatment of coronary vasodilators, antiarrhythmics and vasodilators.
  22. KCNQ2/Q3 potassium channel activator

    ICA-069673 is a KCNQ2/Q3 potassium channel activator with an IC50 of 0.69 μM.
  23. SMN2 splicing modulator

    Branaplam (LMI070) is a highly potent, selective and orally active small molecule SMN2 splicing modulator.
  24. KCC2 inhibitor

    VU 0240551 is a small molecule inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells).
  25. Potassium Channel inhibitor

    Azimilide(NE-10064) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
  26. IKs blocker

    JNJ 303 is a potent IKs blocker with an IC50 value of 64 nM.
  27. HERG activator

    RPR-260243 is a novel activator of HERG; modifies HERG currents inhibited by dofetilide (IC50 = 58 nM); little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes.
  28. ROMK inhibitor

    MK-7145 is a ROMK inhibitor, with an IC50 of 0.045 μM.
  29. mitoKATP channels

    BMS-191095 is an activators of mitochondrial ATP-sensitive potassium (mitoKATP) channels.
  30. KATP activator

    Levcromakalim ((-)-Cromakalim) is an ATP-sensitive K+ channel (KATP) activator.
  31. Amiodarone is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM.

  32. hERG potassium channel inhibitor

    Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.
  33. potassium channel inhibitor

    VU591 is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM.
  34. potassium currents blocker

    Gliclazide is used as an antidiabetic. It is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. 

  35. BeKm-1 is a HERG (human ether-a-go-go-related gene) blocking compound. BeKm-1 can be used for the research of heart disease.
  36. ROMK inhibitor

    VU590 is a potent and moderately selective ROMK (Kir1.1) inhibitor, with an IC50 of 290 nM. VU590 also inhibits Kir7.1, with an IC50 of 8 μM. VU590 is not a good probe of ROMK function in the kidney.
  37. KCNQ2/3 potassium channels activator

    QO-40 is an activator of KCNQ2/3 potassium channels.
  38. Ca2+-activated K+ channel activator

    NS19504 is a Ca2+-activated K+ channel (BK channel, KCa1.1 channel) activator (EC50=11.0 μM) with relaxing effect on bladder smooth muscle spontaneous phasic contractions.

  39. potassium current activator

    NS5806, a potent potassium current activator, increases KV4.3/KChIP2 peak current amplitudes with an EC50 of 5.3 μM. NS5806 slows KV4.3 and KV4.2 current dacay in channel complexes containing KChIP2.
  40. Potassium Channel inhibitor

    Acecainide, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide. Acecainide is a Class III antiarrhythmic agent. It can be given either intravenously or orally, and is eliminated primarily by renal excretion.
  41. Serotonergic Receptor Antagonist

    Hymenidin is a natural antagonist of serotonergic receptors, exhibiting significant inhibitory effects on voltage-gated potassium channels. This compound demonstrates the ability to induce apoptosis in cancer cells, making it a valuable tool for research in cancer biology and therapeutics targeting serotonergic signaling pathways. Its dual action on ion channels and receptor antagonism positions Hymenidin as a noteworthy reagent for exploring complex cellular mechanisms in neurobiology and oncology.
  42. K+ Channels Activator

    1-EBIO is an activator of Ca2+-sensitive K+ channels, playing a crucial role in the modulation of membrane potential and cellular excitability. This compound is utilized in research to investigate the physiological functions and pathophysiological roles of K+ channels, contributing to a deeper understanding of cellular signaling processes and potential therapeutic targets in various diseases.
  43. Anti-microbial Agent/Kir3.2 Blocker

    3,6-Diaminoacridine hemisulfate is an acridine compound that functions primarily as a broad-spectrum antimicrobial agent and a Kir3.2 potassium channel blocker. Its mechanism involves insertion into bacterial DNA, thereby disrupting replication and transcription, which ultimately leads to bacterial lysis. Additionally, this compound is utilized in research to investigate the neurological phenotype associated with Down syndrome. Due to its ability to penetrate the stratum corneum and accumulate in the cell nucleus, prolonged exposure warrants caution due to potential oncogenic effects.
  44. Stable Isotope

    Terfenadine-d3 is the deuterated form of Terfenadine, which primarily targets the hERG potassium channel as a potent open-channel blocker with an IC50 of 204 nM. As an H1 histamine receptor antagonist, Terfenadine-d3 demonstrates significant biological activity by inducing apoptosis in melanoma cells through the modulation of calcium homeostasis. Its mechanism includes the generation of reactive oxygen species (ROS) and the subsequent activation of caspases -4, -2, and -9, making it valuable for research in cancer biology and apoptosis pathways.
  45. KCNQ2 activator

    Ebio1 is a selective activator of the voltage-gated potassium channel KCNQ2. It enhances KCNQ2 activity by stabilizing an extended channel gate conformation, resulting in increased conductance at a saturation voltage of +50 mV.
  46. HDAC inhibitor

    HL23 is a histone deacetylase (HDAC) inhibitor with demonstrated efficacy against hepatocellular carcinoma (HCC). It enhances acetylation at the TXNIP promoter, leading to upregulation of TXNIP expression and modulation of potassium channel activity, ultimately inducing TXNIP-dependent potassium deprivation. HL23 effectively suppresses HCC progression and metastasis, and exhibits a synergistic antitumor effect when combined with Sorafenib, outperforming the combination of Sorafenib and Vorinostat in preclinical models.
  47. TNFα/IL-2 Inhibitor

    Immuno modulator-1 is a potent inhibitor of TNFα and IL-2, displaying IC50 values of 4.7 nM and 26 nM, respectively, in human peripheral blood mononuclear cells (hPBMC). This compound is valuable for investigating immune response modulation and inflammatory pathways. Additionally, Immuno modulator-1 demonstrates a hERG potassium channel blocking effect, exhibiting a 20% inhibitory percentage at a concentration of 3 μM, making it relevant for studies involving cardiac safety profiles.
  48. Potassium Channel Inhibitor

    Endoxifen Z-isomer hydrochloride is a selective potassium channel inhibitor that acts as a potent metabolite of Tamoxifen, exhibiting over 100-fold increased potency compared to its parent compound. This compound effectively inhibits PKCβ1 kinase activity, leading to decreased phosphorylation of AKT at Ser473 and its substrates, which ultimately promotes apoptosis. Endoxifen Z-isomer hydrochloride demonstrates significant anticancer effects, particularly against hormone-resistant metastatic breast cancer, making it a valuable reagent for cancer research applications.
  49. Stable Isotope

    Trimebutine-d5 fumarate is a deuterium-labeled derivative of Trimebutine fumarate, functioning primarily as a multi-target inhibitor and opioid receptor agonist. This compound exhibits key biological activities, including the inhibition of L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa), which regulate calcium influx and potassium efflux. Additionally, Trimebutine-d5 fumarate targets Toll-like receptors, modulating inflammatory signaling pathways, and promotes apoptosis in tumor cells via the AKT/ERK pathway. Its applications are particularly relevant in the study of gastrointestinal disorders, including irritable bowel syndrome (IBS), due to its ability to inhibit excessive smooth muscle contraction.
  50. Progranulin secretion Activator

    Progranulin modulator-1 is a selective activator of progranulin (PGRN) secretion. It significantly increases PGRN levels in BV-2 cells and exhibits low cytotoxicity with an EC50 value of 83 nM for PGRN. Additionally, Progranulin modulator-1 inhibits the hERG potassium channel with an IC50 of 3100 nM, making it a valuable tool for research on neuroinflammation and associated neurodegenerative disorders.

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