Potassium Channels

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  1. Anti-malaria Agent

    Quinine hemisulfate hydrate, an alkaloid obtained from the bark of the cinchona tree, functions primarily as an anti-malaria agent. It acts as a potassium channel inhibitor, specifically targeting the Slo3 (KCa5.1) channel, and can effectively inhibit channel currents in wild-type mouse models. Its inhibitory activity is quantified with an IC50 value of 169 μM, making it a valuable compound for research into malaria treatment and the modulation of potassium channels.
  2. Stable Isotope

    Endoxifen-d5 (Z-isomer) is the stable isotope-labeled derivative of the Z-isomer of Endoxifen. This metabolite of Tamoxifen exhibits significant anti-estrogenic activity in breast cancer cells that express the estrogen receptor alpha (ERα), contributing to its therapeutic efficacy in estrogen-sensitive tumors. Additionally, Endoxifen (Z-isomer) demonstrates a concentration-dependent inhibition of the hERG potassium channel, with an IC50 value of 1.6 μM, making it a valuable tool for research into breast cancer treatment and associated cardiotoxic effects.
  3. Antimalarial Agent

    Halofantrine is an antimalarial agent that primarily targets Chloroquine-resistant strains of Plasmodium falciparum. This compound exhibits high lipophilicity and effectively blocks HERG potassium channels, contributing to its pharmacological profile. Halofantrine is utilized in research focused on malaria treatment and the mechanisms of drug resistance in parasitic infections.
  4. Parasite Inhibitor

    Ep vinyl quinidine, an epi-vinyl stereoisomer of Quinidine, serves as a targeted inhibitor of parasitic activity. This compound exhibits significant potential in malaria research, leveraging its capabilities as a selective cytochrome P450db inhibitor. Additionally, it functions as a potassium channel blocker with an IC50 of 19.9 μM, positioning it as a valuable tool for investigating anti-parasitic mechanisms and therapeutic interventions.
  5. Potassium-Competitive Acid Blocker

    Vonoprazan hydrochloride is a potassium-competitive acid blocker (P-CAB) that inhibits H+,K+-ATPase activity, exhibiting an IC50 of 19 nM at pH 6.5. Its potent antisecretory effects make it a valuable reagent in research related to acid-related conditions, including gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan hydrochloride is also utilized for studies focusing on the eradication of Helicobacter pylori, contributing to advancements in gastrointestinal therapeutics.
  6. Potassium Channel Activator

    Kaurenoic acid is a diterpene that acts as a potassium channel activator. It exhibits various biological activities, including antibacterial, anti-inflammatory, anticonvulsant, analgesic, and aortic vasodilating effects. This compound is primarily utilized in research related to neuroprotection, cardiovascular health, and the modulation of ion channel activity.
  7. TREK-1 Channel Blocker

    Spadin is a potent TREK-1 channel blocker with an IC50 value of 10 nM. This natural peptide, derived from a propeptide released into the bloodstream, enhances 5-HT neurotransmission in the dorsal raphe nucleus of mice, promoting hippocampal CREB activation and neurogenesis. Spadin is valuable for research applications targeting antidepressant mechanisms and neuroplasticity.
  8. Stable Isotope

    Chlorpromazine-d6 hydrochloride is a deuterated derivative of Chlorpromazine, primarily functioning as a dopamine receptor antagonist. This stable isotope is utilized in biochemical and pharmacological research to explore the interactions and mechanisms of action of antipsychotic agents. Its ability to inhibit serotonin receptors, potassium channels, and sodium channels makes it valuable for studying neuropharmacology and drug metabolism.
  9. Potassium Channel Inhibitor

    Naluzotan hydrochloride is a selective potassium channel inhibitor that primarily functions as an amidosulfonamide 5-HT1A agonist, exhibiting an IC50 of approximately 20 nM and a Ki value of 5.1 nM. This compound demonstrates notable activity in modulating neurotransmitter pathways, making it a valuable tool for research into anxiety and depression treatments. Additionally, naluzotan hydrochloride acts as a weak hERG K+ channel blocker with an IC50 of 3800 nM, highlighting its potential relevance in cardiac safety assessments.
  10. Anti-malarial Agent

    Quinine sulfate hydrate (2:1:4) is an orally active alkaloid used primarily as an anti-malarial agent. This compound functions as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel, with an IC50 of 169 μM observed in response to voltage pulses of +100 mV. It is valuable for research applications focused on malaria treatment and investigating ion channel physiology.
  11. Anti-malaria Agent

    Quinine hydrochloride is an alkaloid extracted from the bark of the cinchona tree, primarily functioning as an anti-malarial agent. It acts as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel and demonstrating inhibitory effects on channel currents evoked by voltage pulses to +100 mV, with an IC50 value of 169 μM. This compound is widely utilized in research applications related to malaria treatment and ion channel studies.
  12. Anti-malarial Agent

    Quinine hemisulfate is an orally active alkaloid derived from cinchona bark, primarily recognized for its anti-malarial properties. This compound acts as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel, with an IC50 value of 169 μM for channel currents induced by voltage pulses to +100 mV. Quinine hemisulfate serves as a valuable reagent for anti-malarial studies and relevant pharmacological investigations.
  13. Anti-malarial Agent

    Quinine dihydrochloride is an orally active alkaloid extracted from cinchona bark, primarily used as an anti-malarial agent. It functions as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel, with an IC50 of 169 μM. This compound is utilized in various research applications aimed at understanding malaria pathophysiology and exploring therapeutic strategies for its treatment.
  14. Stable Isotope

    Quinine-d3 is a deuterium-labeled derivative of quinine, primarily used as a stable isotope in chemical research. Quinine is an alkaloid isolated from the cinchona tree, known for its efficacy as an antimalarial agent and its role as a potassium channel inhibitor. It specifically inhibits wild-type mouse Slo3 (KCa5.1) channel currents induced by voltage pulses, exhibiting an IC50 of 169 μM. This reagent facilitates studies in pharmacology and biochemistry, enabling precise tracking and quantification in various applications.
  15. ASK1 Inhibitor

    ASK1-IN-10 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 value of less than 200 nM. In addition to its primary mechanism, ASK1-IN-10 exhibits inhibitory activity against hERG potassium channels. This compound serves as a valuable tool for investigating the role of ASK1 in inflammation-related research and its potential therapeutic implications.
  16. Potassium Channel Opener

    Bimakalim is an ATP-sensitive potassium channel opener that induces vasodilation by enhancing potassium ion efflux. This compound has been shown to reduce transmural myeloperoxidase (MPO) activity and mimics ischemic preconditioning effects, leading to decreased infarct size and modulation of adenosine release and neutrophil function. Bimakalim is valuable for research applications focused on cardiovascular physiology and ischemia-reperfusion injury studies.
  17. hERG Inhibitor

    GSK369796 is a selective inhibitor of the hERG potassium ion channel, demonstrating an IC50 value of 7.5 μM. This compound exhibits significant antimalarial activity, making it a valuable tool for research in both cardiac function and malaria therapeutics. Its potential implications in pharmacology and drug development provide a basis for further exploration in ion channel regulation and associated biological pathways.
  18. μ-opioid Receptor Activator, hERG (Kv11.1) Potassium Channel Inhibitor

    ERG-IN-6 is a potent μ-opioid receptor activator, exhibiting an EC50 of 0.12 nM, which makes it an effective tool for studies related to pain modulation. Additionally, ERG-IN-6 functions as a hERG (Kv11.1) potassium channel inhibitor with an IC50 of 0.681 μM. This compound is valuable for research applications investigating the interplay between opioid signaling and ion channel regulation.
  19. CB1/2 Agonist

    AB-FUBICA is a potent agonist for CB1 and CB2 receptors, serving as a valuable tool in cannabinoid research. It functions by activating G-protein coupled inwardly rectifying potassium channels (GIRK) through its binding to these receptors, demonstrating significant cannabinoid-like activity. With EC50 values of 21 nM for CB1 and 15 nM for CB2, AB-FUBICA is ideal for investigating pain management, neurodegenerative diseases, and inflammation-related pathways.
  20. Anxiolytic Agent

    Succinic acid sodium functions as an effective anxiolytic agent. It has demonstrated inhibitory effects on colonic epithelial cell proliferation in vivo and can down-regulate the expression of key genes such as KCNMB1 and TET1. This compound is particularly useful for research involving gestational hypertension and related physiological studies.
  21. Adrenergic Receptor Inhibitor

    Besipirdine is an adrenergic receptor inhibitor that exhibits non-receptor-dependent cholinomimetic properties. This compound is known to inhibit voltage-dependent sodium and potassium channels, contributing to its pharmacological profile. Besipirdine's biological activity makes it relevant for research applications focused on neuropharmacology and the modulation of synaptic transmission.
  22. FTO Inhibitor

    Meclofenamic acid sodium hydrate is a selective inhibitor of fat mass and obesity-associated enzyme (FTO). Its primary action involves competing with FTO for binding to m(6)A-containing nucleic acids, thereby influencing RNA metabolism. Additionally, it exhibits non-selective gap-junction blocking activity and inhibits potassium channels hKv2.1 and hKv1.1, with IC50 values of 56.0 μM and 155.9 μM, respectively. This compound is valuable in research focused on obesity, metabolic regulation, and the role of RNA modifications in cellular processes.
  23. CCR8 Antagonist

    AZ760 is a potent antagonist of the CCR8 receptor, which plays a significant role in immune response modulation. This compound demonstrates excellent potency and favorable lipophilicity, resulting in a high free fraction in blood. However, it is important to note that AZ760 exhibits unacceptable inhibition of the hERG potassium channel, which may have implications for cardiovascular safety in therapeutic applications.
  24. Bupivacaine metabolite

    Bupivacaine N-oxide hydrochloride is a metabolite of the local anesthetic Bupivacaine, which primarily acts as an NMDA receptor inhibitor. It also exhibits significant activity by blocking sodium, L-calcium, and potassium channels, particularly SCN5A channels with an IC50 of 69.5 μM. This compound is relevant for research into chronic pain mechanisms and provides insight into the pharmacological action of Bupivacaine and its derivatives.
  25. Drug Metabolite Control

    Nicorandil pyridine oxide is a metabolite of Nicorandil, which acts as an activator of the sulfonylurea receptor 2B (SUR2B) and the ATP-sensitive potassium channel Kir6.2. This compound serves as a crucial tool for drug metabolite control, offering insights into the pharmacokinetics and therapeutic mechanisms of Nicorandil. Its biological activity is important for researchers studying cardiovascular effects and the modulation of ion channels in various biological systems.
  26. EBP Inhibitor

    EBP-IN-1 is a selective inhibitor of emopamil binding protein (EBP) that effectively crosses the blood-brain barrier. This compound demonstrates an IC50 of 8.2 μM against human ERG potassium channels in CHO cells, leading to the inhibition of EBP's sterol isomerase activity and subsequent accumulation of Zymostenol. EBP-IN-1 has been shown to promote oligodendrocyte differentiation in human cortical organoids, making it a valuable tool for research into multiple sclerosis and related neurological disorders.
  27. σ Receptor Agonist

    threo-Ifenprodil hemitartrate is a sigma (σ) receptor agonist, exhibiting Kis of 59.1 nM and 2 nM for σ1 and σ2 receptors, respectively. This compound also acts as a NR2B subunit-selective NMDA receptor antagonist, with an IC50 of 0.22 μM, and demonstrates inhibition of the hERG potassium channel with an IC50 of 88 nM, indicating potential antiarrhythmic activity. threo-Ifenprodil hemitartrate serves as a valuable tool in neuropharmacology and cardiovascular research.
  28. KATP Opener

    Iptakalim hydrochloride is a selective ATP-sensitive potassium channel (KATP) opener that exhibits significant lipophilicity. In addition to its primary mechanism, it also acts as an antagonist of α4β2-containing nicotinic acetylcholine receptors (nAChRs). This dual activity positions Iptakalim hydrochloride as a valuable tool for research in cardiovascular physiology and neuropharmacology, providing insights into potassium channel regulation and cholinergic signaling.
  29. P-gp Inhibitor/Potassium Channel Activator

    GPV0057 is a selective and potent inhibitor of P-glycoprotein (P-gp) and a specific activator of the potassium channel Kir2.1. By competitively binding to the substrate-binding site of P-gp, GPV0057 inhibits ATP-dependent drug efflux, effectively reversing multidrug resistance in tumor cells. Additionally, it stabilizes the open state of Kir2.1, facilitating potassium ion influx. This compound holds potential for research in tumors characterized by high P-gp expression and in conditions such as heart failure and Andersen-Tawil Syndrome that involve Kir2.1 deficiency.
  30. GABAA Receptor Antagonist

    Bicuculline (methochloride) is a selective antagonist of the GABAA receptor, exhibiting an IC50 value of 3 μM. This compound is known to induce clonic-tonic convulsions in mammals and is also capable of blocking Ca2+-activated potassium channels. Bicuculline (methochloride) is utilized in research focused on epilepsy and related psychiatric disorders, providing valuable insights into neuronal excitability and inhibitory transmission.
  31. Potassium Channel Opener

    Flupirtine is a non-opioid analgesic that acts primarily as a potassium channel opener, specifically targeting Kv7 channels. This compound exhibits notable neuroprotective properties by stabilizing blood-brain barrier integrity, reducing oxidative stress, and counteracting focal cerebral ischemia. Flupirtine is utilized in research related to pain management, Alzheimer's disease, multiple sclerosis, and neuroprotection due to its ability to lessen neuronal excitotoxicity and maintain resting membrane potential without exhibiting antipyretic or antiphlogistic effects.
  32. Potassium Channel Opener

    Flupirtine hydrochloride is a potassium channel opener (Kv7 activator) recognized for its analgesic and neuroprotective properties. This compound acts as a non-opioid analgesic while also antagonizing NMDA receptors and activating GABA receptors. Flupirtine hydrochloride enhances neuronal stability by reducing oxidative stress and calcium influx, thereby protecting neurons from excitotoxicity and ischemia. It is applicable in research focused on conditions such as focal cerebral ischemia, pain management, Alzheimer’s disease, and multiple sclerosis.
  33. GABAA Receptor Antagonist

    Bicuculline methobromide is a selective antagonist of the GABAA receptor, exhibiting an IC50 value of 3 μM. This compound is known to induce clonic-tonic convulsions in mammalian models, making it a valuable tool for investigating epilepsy and associated neurological disorders. Additionally, bicuculline methobromide functions as a blocker of Ca2+-activated potassium channels, further expanding its utility in pharmacological research focused on ion channel dynamics and excitability in neuronal systems.
  34. Stable Isotope

    Flupirtine-d4 hydrochloride is a deuterium-labeled variant of Flupirtine hydrochloride, a non-opioid analgesic that crosses the blood-brain barrier. This compound functions primarily as a neuronal potassium channel opener (Kv7 activator) and exhibits properties as an NMDA receptor antagonist and GABA receptor activator. It is utilized in research focused on pain management, neuroprotection, and conditions such as Alzheimer’s disease and multiple sclerosis, offering insights into pathways of ischemic neuron death, oxidative stress modulation, and the maintenance of blood-brain barrier integrity. Flupirtine-d4 hydrochloride serves as a valuable tool for studying the underlying mechanisms and therapeutic approaches for neurological disorders.
  35. Kv1.3/Kv1.4 Blocker

    CP 339818 hydrochloride is a selective blocker of Kv1.3 and Kv1.4 ion channels, with an IC50 of 200 nM for Kv1.3. This compound also inhibits HCN channels, displaying IC50 values of 18.9 μM and 43.4 μM for HCN1 and HCN4, respectively, while having minimal effect on other Kv channels such as Kv1.1 and Kv1.2. By selectively targeting Kv1.3, CP 339818 hydrochloride attenuates the activation of human T cells, making it a valuable tool for investigating the physiological roles of HCN and Kv channels in cellular processes.
  36. HCN/Potassium Channels Blocker

    KIO-301 chloride is a photoswitch compound that selectively blocks hyperpolarisation-activated cyclic nucleotide-gated (HCN) channels and voltage-gated potassium channels upon exposure to visible light. This compound can be employed in research to investigate the role of these ion channels in cellular excitability and signaling pathways. Its unique mechanism offers insights into ion channel modulation and potential therapeutic applications in neurobiology and cardiac research.
  37. Kv1.3/Kv1.4 Channel Blocker

    CP-339818 is a selective blocker of the Kv1.3 and Kv1.4 potassium channels, exhibiting an IC50 of 200 nM for Kv1.3. This compound also inhibits HCN channels, with IC50 values of 18.9 μM and 43.4 μM for HCN1 and HCN4, respectively, while demonstrating minimal effects on other Kv channels, such as Kv1.1 and Kv1.2. CP-339818 is valuable for investigating the role of Kv1.3 in T cell activation and the physiological functions of HCN and Kv channels in cellular contexts.
  38. NMDA Receptor Inhibitor

    Bupivacaine is an NMDA receptor inhibitor that modulates neuronal excitability by blocking sodium, L-calcium, and potassium channels. It exhibits potent inhibition of SCN5A channels, with an IC50 of 69.5 μM. This compound is primarily utilized in research focused on chronic pain mechanisms and therapeutic interventions.
  39. Potassium Supplement

    Potassium chloride, AR, 99.5% serves as an essential potassium supplement, playing a critical role in various biochemical applications. This compound is particularly valuable in research related to hyperkalemia, where it aids in studying potassium ion regulation in biological systems. Additionally, it functions as a potassium source in agronomy, contributing to plant nutrition and growth.
  40. Potassium Channel Blocker

    Azimilide dihydrochloride is a class III antiarrhythmic agent that functions primarily as a potassium channel blocker, targeting both IKs and IKr channels with IC50 values of 2.6 μM and 1 μM, respectively. Additionally, it inhibits the HERG channel at frequencies of 0.1 and 1 Hz, with IC50 values of 1.4 μM and 5.2 μM. Azimilide dihydrochloride also suppresses L-type calcium current and sodium current, with IC50 values of 17.8 μM and 19 μM, respectively. This compound is valuable for researching conditions such as atrial fibrillation and ventricular fibrillation.
  41. NMDA Receptor Inhibitor

    Bupivacaine-d9 is a deuterium-labeled analog of Bupivacaine, primarily targeting NMDA receptors. This compound exhibits inhibitory effects on sodium, L-calcium, and potassium channels, with a notable potency against SCN5A channels, characterized by an IC50 value of 69.5 μM. Bupivacaine-d9 is utilized in research related to chronic pain mechanisms and the modulation of excitatory neurotransmission, offering valuable insights into therapeutic applications in pain management.
  42. Potassium/Sodium Channel Inhibitor

    Huwentoxin I is a peptide toxin that specifically inhibits voltage-gated sodium channels and N-type calcium channels. This compound has demonstrated significant inhibitory effects on sodium channels in both rat hippocampus and cockroach dorsal unpaired median (DUM) neurons, with IC50 values of 66.1 nM and 4.80 nM, respectively. Huwentoxin I is valuable for studies focused on neuronal excitability and channelopathy-related research applications.
  43. NMDA Receptor Inhibitor

    Bupivacaine hydrochloride monohydrate is an NMDA receptor inhibitor that effectively modulates excitatory neurotransmission. It possesses the ability to block sodium, L-calcium, and potassium channels, with a notable potency in inhibiting SCN5A channels, exhibiting an IC50 value of 69.5 μM. This compound is primarily utilized in research focused on chronic pain mechanisms and the development of analgesic strategies.
  44. Antiarrhythmic Agent

    AZD-1305 is an antiarrhythmic agent that selectively blocks sodium and potassium channels in the atria. This compound significantly prolongs action potential duration and reduces excitability, leading to atrial-selective effective refractory period (ERP) prolongation and acute termination of atrial fibrillation. AZD-1305 is a valuable tool for research related to atrial fibrillation and its underlying mechanisms.
  45. Stable Isotope

    Ranolazine-d5 is a deuterium-labeled analogue of Ranolazine, which primarily targets the late phase of inward sodium current (INa) and potassium channels (IKr), exhibiting IC50 values of 6 μM and 12 μM, respectively. This compound functions as an anti-anginal agent by alleviating myocardial ischemia without influencing heart rate or blood pressure. Additionally, Ranolazine-d5 serves as a partial inhibitor of fatty acid oxidation (FAO), making it valuable for research in cardiovascular pharmacology and metabolic studies.
  46. N-type Calcium Channel Antagonist

    Huwentoxin XVI is a selective antagonist of N-type calcium channels, demonstrating a potent inhibitory effect with an IC50 of approximately 60 nM. Derived from the Chinese tarantula Ornithoctonus huwena, it serves as an analgesic and exhibits no activity against voltage-gated T-type calcium channels, potassium channels, or sodium channels. This specificity makes Huwentoxin XVI valuable in research aimed at understanding pain mechanisms and the role of calcium channels in various physiological processes.
  47. Stable Isotope

    Bupivacaine-d9 hydrochloride is a deuterium-labeled analog of Bupivacaine hydrochloride, primarily known for its role as an NMDA receptor inhibitor. This compound effectively blocks sodium, L-calcium, and potassium channels, demonstrating potent inhibition of SCN5A channels with an IC50 value of 69.5 μM. Bupivacaine-d9 hydrochloride is valuable for research focused on chronic pain modulation and neuronal signaling studies.
  48. TRPV4-KCa2.3 Protein Complex Enhancer

    TRPV4-KCa2.3 modulator 1 is a modulator that enhances the TRPV4-KCa2.3 protein complex, exhibiting significant antihypertensive activity. This compound promotes hyperpolarization and vasodilation in endothelial cells. Its ability to influence vascular responses makes it a valuable tool for investigating hypertension and related cardiovascular disorders in research settings.
  49. Potassium/Calcium/Sodium Channel Blocker

    NIP-142 is a benzopyran derivative that functions as a potassium, calcium, and sodium channel blocker. It selectively inhibits potassium channels abundant in atrial muscle, leading to an increase in the effective refractory period (ERP) and action potential duration (APD) in the atrium, while sparing ventricular repolarization. Additionally, NIP-142 dampens L-type and T-type calcium channels and sodium channels, enhancing its anti-arrhythmic properties. This compound is particularly useful in the study of atrial fibrillation and related arrhythmias.
  50. Hypoglycemic Agent

    AZ-DF 265 is a hypoglycemic agent that promotes insulin secretion through the inhibition of ATP-sensitive potassium channels and the activation of voltage-dependent calcium channels. This results in the influx of calcium ions, which is crucial for insulin release. AZ-DF 265 is applicable in diabetes research, providing insights into glucose metabolism and insulin regulation mechanisms.

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