Membrane Transporters-Ion Channels

Items 2451-2500 of 2532

Page
per page
Set Descending Direction
Catalog No.
Product Name
Application
Product Information
Citations
  1. Antiarrhythmic Agent

    R-(–)-Flecainide is an orally active antiarrhythmic agent that primarily targets voltage-gated sodium channels to inhibit ectopic ventricular activity. It effectively stabilizes cardiac cell membranes and is utilized in the management of various cardiac arrhythmias. Research applications include studies on cardiac electrophysiology and drug interactions in arrhythmogenic conditions.
  2. KM-001 Isomer

    KM-001-E2 is the (S)-enantiomer of KM-001, a selective antagonist of the TRPV3 channel. This compound plays a significant role in investigating the mechanisms underlying skin itching and keratinization disorders. Its application in research may provide insights into TRPV3-related pathophysiology and potential therapeutic strategies for skin conditions.
  3. Drug Isomer

    2-Methylethcathinone hydrochloride is an isomer of the psychoactive compound ethcathinone. It primarily functions as a stimulant, exerting its effects by interacting with monoamine transporters, leading to increased levels of neurotransmitters such as dopamine and norepinephrine. This compound is utilized in research focused on neuropharmacology and the study of designer drugs, contributing to the understanding of their mechanisms of action and potential therapeutic applications.
  4. S-isomer Of Ranolazine

    (S)-Ranolazine is the S-isomer of the antianginal agent Ranolazine, which primarily targets the cardiomyocyte sodium channels. It demonstrates significant biological activity in reducing myocardial ischemia and angina by modulating ion currents and improving cardiac energy metabolism. This compound is used in cardiovascular research to explore mechanisms of action related to cardiac function and ischemia.
  5. Drug Isomer

    2-Methylethcathinone (2-MEC) is an isomer of the psychoactive substance methcathinone, primarily acting as a monoamine transporter inhibitor. This compound exhibits stimulant properties, influencing the release and reuptake of neurotransmitters such as dopamine, norepinephrine, and serotonin. 2-MEC is utilized in research exploring its pharmacological effects, potential therapeutic implications, and the underlying mechanisms of psychostimulants.
  6. Isomer of 4-Bromoamphetamine

    2-Bromoamphetamine hydrochloride is an isomer of 4-Bromoamphetamine, primarily targeting monoamine transporters. This compound exhibits psychoactive properties, influencing neurotransmitter systems such as serotonin and dopamine. It is utilized in scientific research to explore the mechanisms underlying mood regulation and behavioral responses.
  7. VMAT2 Substrate

    FFN 206 dihydrochloride is a selective substrate for the Vesicular Monoamine Transporter 2 (VMAT2), exhibiting an apparent Km of 1.16 μM. This fluorescent probe enables the detection of VMAT2 activity in intact cells via fluorescence microscopy, allowing for the visualization of subcellular localization to VMAT2-expressing acidic compartments while minimizing labeling of other organelles. Its application is essential for studying monoamine transport dynamics and cellular compartmentalization in neurobiological research.
  8. H+, K+-ATPase Inhibitor

    Esomeprazole magnesium, a potent H+, K+-ATPase inhibitor, is utilized in research related to upper intestinal disorders and gastroesophageal reflux disease. Its primary mechanism involves the inhibition of proton pumps, leading to decreased gastric acid secretion. Additionally, Esomeprazole magnesium exhibits properties as an exosome inhibitor by blocking exosome release through the inhibition of vacuolar H+-ATPases, making it valuable for studies on cellular communication and disease progression.
  9. Antiarrhythmic Agent

    Propafenone, a sodium channel blocker, functions as an antiarrhythmic agent by modulating cardiac ion currents. It displays significant binding affinity for β receptors (IC50 = 32 nM) and effectively inhibits the transient outward current (Ito) and sustained delayed rectifier potassium current (Isus) with IC50 values of 4.9 μM and 8.6 μM, respectively. Additionally, Propafenone demonstrates potential in anticancer research by suppressing the proliferation of esophageal cancer cells through the induction of mitochondrial dysfunction and apoptosis.
  10. Anti-malarial Agent

    Quinine hydrochloride dihydrate is an anti-malarial agent primarily known for its inhibitory action on potassium channels. It effectively inhibits wild-type mouse Slo3 (KCa5.1) channel currents in response to voltage pulses, exhibiting an IC50 value of 169 μM. This compound is essential for research into malaria treatment and the study of ion channel modulation in various biological contexts.
  11. Antiepileptic Agent

    Rufinamide is an oral antiepileptic agent that primarily inhibits sodium channel activation, leading to reduced neuronal hyperexcitability and anticonvulsant effects. This compound is particularly relevant in the study of Lennox-Gastaut syndrome, providing insights into its mechanisms and potential therapeutic strategies. Rufinamide's efficacy in mitigating seizures makes it a valuable tool for research in epilepsy and related neurological disorders.
  12. Stable Isotope

    Atazanavir-d9 is a deuterated analog of Atazanavir, a highly selective HIV-1 protease inhibitor. This compound targets the HIV-1 protease enzyme, facilitating the treatment of HIV infections with its ability to inhibit viral replication. Additionally, Atazanavir acts as both a substrate and inhibitor of CYP3A4, as well as an inducer of P-glycoprotein (P-gp). Furthermore, Atazanavir possesses inhibitory activity against SARS-CoV 3CLpro, with an IC50 of 3.49 μM, making it relevant for research in antiviral therapies.
  13. Na+/Ca2+ Channel Blocker

    Flunarizine dihydrochloride is a potent dual blocker of Na+ and Ca2+ channels, specifically targeting T-type calcium channels. This compound exhibits significant anticonvulsant and antimigraine properties, making it valuable for neurological research. Additionally, Flunarizine dihydrochloride demonstrates peripheral vasodilatory effects, enhancing its potential applications in vascular studies.
  14. Sodium Channel Inhibitor

    Mepivacaine hydrochloride is a sodium channel inhibitor that selectively binds to voltage-gated sodium ion channels in neuronal cell membranes. By inhibiting sodium influx and membrane depolarization, it provides significant local anesthetic effects. This compound is widely used in research applications related to nerve conduction studies and pain management investigations.
  15. Muscarinic Receptor Antagonist

    Afacifenacin is a potent and orally active muscarinic receptor antagonist that targets the bladder afferent pathway. It exerts its biological activity by inhibiting sodium channels, leading to increased bladder volume and a reduction in the frequency of urination and incontinence. This compound is valuable for research focused on overactive bladder (OAB) and related urological conditions.
  16. K+ Channel Blocker

    Dendrotoxin-I (DTX-I) is a potent inhibitor of voltage-gated potassium channels, specifically targeting the KV1.1, KV1.2, and KV1.6 subunits with IC50 values ranging from 0.13 to 50 nM. This neurotoxin exhibits significant biological activity that can influence neuronal excitability and synaptic transmission. Dendrotoxin-I is primarily utilized in research applications related to cancer and neurobiology, providing insights into ion channel function and their roles in disease mechanisms.
  17. Antitumor Agent

    Chlorotoxin is a 36 amino acid peptide derived from the venom of the Israeli scorpion, Leiurus quinquestriatus, known for its antitumor properties. By functioning as a chloride channel blocker, Chlorotoxin inhibits the proliferation of cancer cells and modulates ion channel activity. This compound is valuable for cancer research, particularly in studies investigating tumor biology and the development of targeted therapies.
  18. Na+ Channel Activator

    Brevetoxin-3 (PbTx-3) is a potent allosteric activator of voltage-gated Na+ channels. It demonstrates high affinity for site 5 on these channels, effectively inhibiting their inactivation and prolonging the mean open time. This compound is valuable for research into airway hyperresponsiveness and lung inflammation, as repeated exposure has been shown to induce these conditions. Brevetoxin-3 serves as a critical tool for studying sodium channel modulation and its implications in respiratory pathophysiology.
  19. SERCA Inhibitor

    2,5-Di-tert-butylhydroquinone is a potent inhibitor of Sarco/endoplasmic reticulum Ca2+ ATPase (SERCA), demonstrating an IC50 of 400 nM. This compound disrupts the gating function of Glu309, thereby preventing calcium ions from accessing their binding site. Additionally, 2,5-Di-tert-butylhydroquinone influences the activity of key enzymes such as 5-lipoxygenase and COX-2, with IC50 values of 1.8 μM and 14.1 μM, respectively. It is utilized in research focused on cellular calcium regulation and inflammatory processes.
  20. Calcium Channel Antagonist

    Ginsenoside Ro functions as a calcium channel antagonist, exhibiting an effective antiplatelet activity with an IC50 of 155 µM. This compound notably reduces the production of thromboxane A2 (TXA2) while minimally affecting the activities of cyclooxygenase-1 (COX-1) and thromboxane synthase (TXAS). Ginsenoside Ro is valuable in research related to cardiovascular diseases and platelet aggregation studies.
  21. Calcium Channels Antagonist

    L-Phenylalanine, a competitive antagonist of the α2δ subunit of voltage-dependent calcium channels, exhibits a Ki of 980 nM. It also interacts with glycine- and glutamate-binding sites on N-methyl-D-aspartate receptors (NMDARs), with a KB value of 573 μM. This essential amino acid plays a significant role in various biological processes and is frequently utilized in research concerning neuropharmacology and receptor interactions, as well as in the synthesis of food flavors and pharmaceuticals.
  22. hERG Channel Blocker

    Tannic acid is identified as a novel hERG channel blocker, exhibiting an IC50 of 3.4 μM. This compound has significant implications in cardiovascular research, particularly in studying drug-induced long QT syndrome and cardiac arrhythmias. Its capacity to modulate ion channel activity makes it a valuable tool in pharmacological studies focused on cardiac safety and ion channel function.
  23. Sodium Channel Activator

    3-Deoxyaconitine is a diterpenoid alkaloid identified as a sodium channel activator. It exhibits significant biological activity by modulating ion channel dynamics, making it a valuable tool for research into neuronal signaling and pain pathways. This compound can be utilized in studies focusing on the physiological and pharmacological roles of sodium channels.
  24. Calcium Channel Activator

    Gomisin J is a lignan derived from Schisandra chinensis that primarily acts as a calcium channel activator. It enhances nitric oxide bioavailability through eNOS activation and regulates lipid metabolism via the AMPK pathway. Additionally, Gomisin J exhibits anti-inflammatory effects by inhibiting fetuin-A and NF-κB, while its activation of Nrf2/HO-1 boosts antioxidant capacity. This compound is relevant for studies focused on hypertension, non-alcoholic fatty liver disease, and cerebral ischemia-reperfusion injury.
  25. Calcium Channel Antagonist

    Praeruptorin E serves as a calcium channel antagonist and is the primary bioactive constituent derived from Peucedanum praeruptorum, commonly known as Bai-Hua Qian Hu. This compound exhibits a pD2′ value of 5.2, indicating its efficacy in inhibiting calcium influx in target cells. Its biological activity makes it a valuable tool for research applications exploring calcium signaling pathways and related physiological processes.
  26. Bacterial Inhibitor

    Methyl Paraben is a bacterial inhibitor primarily used as a preservative in various applications due to its stability and non-volatility. It has been shown to enhance histamine release and modulate cellular immune responses, in addition to blocking sodium channels. Its properties make it valuable for studies exploring microbial inhibition and the mechanisms of ischemia-reperfusion injury.
  27. Antimicrobial Agent

    Danofloxacin mesylate is a fluoroquinolone antimicrobial agent that exerts its bactericidal activity primarily through the inhibition of bacterial DNA gyrase, a crucial enzyme for DNA replication. This compound displays a broad spectrum of effectiveness against various bacterial strains. Additionally, Danofloxacin mesylate is recognized as a substrate for ATP-dependent efflux transporters, including P-glycoprotein (P-gp) and multidrug resistance protein 2 (MRP2), making it relevant for studies on drug resistance mechanisms in bacteria. This agent is primarily utilized in veterinary medicine and research on antibiotic efficacy and resistance.
  28. TASK-1 Inhibitor

    Doxapram hydrochloride hydrate is a TASK-1 inhibitor that enhances respiratory function by stimulating the brain's respiratory centers and peripheral chemoreceptors. This compound effectively increases both the rate and depth of breathing, while demonstrating inhibitory effects on TASK-1, TASK-3, and their heterodimeric channels with EC50 values of 410 nM, 37 μM, and 9 μM, respectively. Additionally, it inhibits Ca²⁺-activated and Ca²⁺-independent potassium currents in type I cells of the carotid body, with IC50 values of approximately 13 μM and 20 μM, respectively. Doxapram hydrochloride hydrate serves as a useful reagent for research on respiratory depression conditions, including post-anesthesia recovery, chronic obstructive pulmonary disease, and apnea of prematurity.
  29. Calcium Channel Inhibitor

    Ethosuximide is a calcium channel inhibitor primarily targeting T-type calcium channels, specifically blocking low voltage-activated currents. This compound is extensively used in research for its anti-epileptic properties as well as its potential therapeutic effects in various neurodegenerative disease models. Ethosuximide facilitates the study of calcium signaling pathways and their involvement in neuronal excitability and degeneration.
  30. Dopamine Receptor Inhibitor

    Fluphenazine dihydrochloride is a potent dopamine receptor antagonist primarily targeting dopamine D2 receptors in the mesolimbic, nigrostriatal, and tuberoinfundibular pathways. This phenothiazine derivative also exhibits the ability to inhibit neuronal voltage-gated sodium channels. Its key biological activities include the suppression of Methylphenidate-induced stereotyped behaviors and climbing in murine models. Fluphenazine dihydrochloride is widely utilized in research related to psychosis, diabetic peripheral neuropathy, and may also have implications for the inhibition of SARS-CoV-2.
  31. Sodium Channel Inhibitor

    Oxybuprocaine hydrochloride is a sodium channel inhibitor that reversibly blocks sodium channels, effectively preventing the propagation of painful nerve impulses in tissues such as the cornea, conjunctiva, and sclera. This compound is primarily utilized in ophthalmology and otolaryngology for its anesthetic properties, providing localized pain relief during various medical procedures. Its ability to inhibit nerve signal transmission makes it valuable for both diagnostic and therapeutic applications in ocular and ear, nose, and throat treatments.
  32. Sodium Channel Inhibitor

    Propafenone hydrochloride is a sodium channel inhibitor primarily used as an anti-arrhythmic agent. It effectively treats conditions related to rapid heartbeats, including atrial and ventricular arrhythmias. This compound is useful in research applications focused on cardiac rhythm disturbances and the pharmacological modulation of ion channels.
  33. Sodium Channel Inhibitor

    Triamterene is a sodium channel inhibitor that selectively blocks epithelial Na+ channels (ENaC) in a voltage-dependent manner. It exhibits mild diuretic properties and is utilized in the management of conditions related to fluid retention. Additionally, Triamterene serves as an inhibitor of the TGR5 receptor, contributing to its diverse biological effects and applications in research related to renal and metabolic processes.
  34. TRP Channel Agonist

    Camphor ((±)-Camphor) is recognized as a TRP channel agonist, primarily targeting TRPV3. This compound exhibits notable antiviral, antitussive, and anticancer activities, making it valuable for various research applications. Although utilized topically for its anti-infective and anti-pruritic properties, caution is advised as camphor can be toxic when ingested. Its diverse biological activities make it a significant candidate for studies related to TRPV channel modulation.
  35. Repellent Agent

    Vanillyl butyl ether serves as a repellent agent primarily through its modulation of TRPV1 and TRPM8 channels in mammalian systems. This compound exhibits notable activity against pests such as Tribolium castaneum, T. confusum, and L. bostrychophila, demonstrating its potential in pest control applications. Additionally, it acts as a mild warming agent, promoting enhanced blood circulation while retaining its eco-friendly and non-toxic profile.
  36. Antiarrhythmic Agent

    Mexiletine hydrochloride is an orally active antiarrhythmic agent that primarily functions by inhibiting sodium channels, with an IC50 value of 75±8 μM for tonic block and 23.6±2.8 μM for use-dependent block. This compound has demonstrated efficacy in the management of myotonia and neuropathic pain, making it a valuable tool in both cardiovascular and neurological research. Its ability to modulate ion channel activity allows for insights into the mechanisms of arrhythmias and other related disorders.
  37. Antiarrhythmic Agent

    Disopyramide phosphate is a class IA antiarrhythmic agent that primarily targets cardiac sodium channels, effectively blocking the fast inward sodium current. This compound prolongs cardiac action potentials, making it suitable for the treatment of both ventricular and atrial arrhythmias. In addition, disopyramide phosphate inhibits HERG-encoded potassium channels and exhibits significant negative inotropic effects, contributing to its complex pharmacological profile in heart rhythm management. Its diverse biological activities make it valuable for research in electrophysiology and cardiac pharmacology.
  38. Voltage-operated Sodium Channels Blocker

    Mebeverine hydrochloride is a musculotropic agent acting primarily as a voltage-operated sodium channels blocker. It effectively inhibits intestinal peristalsis and reduces intracellular calcium accumulation, making it valuable for research on gastrointestinal motility disorders. Its ability to modulate sodium channels also supports studies related to excitability in smooth muscle tissues.
  39. Sodium Channel Inhibitor

    Ropivacaine mesylate acts primarily as a sodium channel inhibitor, serving as a long-acting amide local anesthetic. It effectively blocks impulse conduction by reversibly inhibiting sodium ion influx in nerve fibers, making it suitable for procedures requiring spinal block anesthesia. Additionally, Ropivacaine has been identified as an inhibitor of the K2P potassium channel TREK-1, exhibiting an IC50 value of 402.7 μM in COS-7 cell membranes. This compound is relevant for research into pain management and neuronal activity modulation.
  40. Sodium Channel Blocker

    Ajmaline is a sodium channel blocker and a class 1A anti-arrhythmic agent. It effectively inhibits HERG currents with an IC50 of 1 μM in HEK293 cells and 42.3 μM in Xenopus oocytes. This compound is utilized in research focused on ventricular tachyarrhythmia and other cardiac rhythm disorders, contributing to a better understanding of arrhythmic conditions.
  41. Sodium Channel Inhibitor

    Mepivacaine is an amide-type local anesthetic that functions as a sodium channel inhibitor. By binding to specific voltage-gated sodium ion channels in neuronal cell membranes, Mepivacaine effectively inhibits sodium influx and membrane depolarization. This agent is primarily utilized in various research applications within the fields of pain management and anesthesia.
  42. Potassium Channel Inhibitor

    Cloperastine hydrochloride is a potassium channel inhibitor primarily targeting hERG K+ currents. It demonstrates concentration-dependent inhibition, with an IC50 value of 27 nM. This reagent is employed in research applications focused on cardiac ion channel function and drug interactions, providing valuable insights into cardiovascular safety and pharmacology.
  43. Proton Pump Inhibitor

    Ilaprazole sodium is a potent proton pump inhibitor that irreversibly targets H+/K+-ATPase, demonstrating a dose-dependent inhibition with an IC50 of 6 μM in rabbit parietal cell assays. This compound is primarily utilized in research focused on gastric ulcers, providing insights into gastric acid secretion regulation. Additionally, Ilaprazole sodium acts as an effective inhibitor of TOPK (T-lymphokine-activated killer cell-originated protein kinase), facilitating studies related to immune responses and cancer therapeutics.
  44. Antitussive Agent

    Benzonatate (PEGn) is a non-narcotic antitussive agent that exerts its effects primarily through sodium channel blockade and local anesthetic activity on respiratory stretch receptors. It is commonly utilized in research involving cough reflex modulation and respiratory control mechanisms. This compound is valuable for studies aimed at understanding cough pathology and developing cough suppression therapies.
  45. VMAT2 Inhibitor

    Valbenazine tosylate is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2), exhibiting a Ki value in the range of 110-190 nM. It is primarily employed in research related to neuropharmacology and the treatment of movement disorders, such as tardive dyskinesia. By inhibiting VMAT2, Valbenazine tosylate modulates neurotransmitter release, making it a valuable tool for studying dopaminergic signaling and associated pathologies.
  46. Calcium Channel Antagonist

    Bepridil hydrochloride hydrate is a non-selective, long-acting calcium channel antagonist that also inhibits sodium and potassium channels. It exhibits antianginal properties and functions as a type I antiarrhythmic agent. Additionally, Bepridil hydrochloride hydrate inhibits the cardiac sodium-calcium exchanger (NCX1), making it valuable for research into cardiovascular disorders.
  47. Sodium Channel Inhibitor

    Riluzole hydrochloride is a sodium channel inhibitor that exhibits anticonvulsant properties. It functions primarily as a use-dependent Na+ channel blocker and also has the capability to inhibit GABA uptake, with an IC50 of 43 μM. This compound is commonly utilized in neurological research applications, particularly in studies focused on epilepsy and neuroprotection.
  48. Calcium Channel Blocker

    Amlodipine maleate is a dihydropyridine calcium channel blocker that primarily targets voltage-dependent L-type calcium channels. By inhibiting calcium influx, it serves as an effective antianginal agent and contributes to the management of hypertension. Amlodipine maleate is utilized in research applications related to cardiovascular health, hypertension, and potential anticancer effects.
  49. Sodium Channel Inhibitor

    Ropivacaine hydrochloride is a potent sodium channel inhibitor that effectively disrupts impulse conduction by reversibly blocking sodium ion influx in nerve fibers. Additionally, it inhibits the K2P TREK-1 potassium channel with an IC50 of 402.7 μM in COS-7 cell membranes. This compound is primarily applied in the management of neuropathic pain in various in vivo research contexts.
  50. ENaC Blocker

    Benzamil hydrochloride is a selective blocker of the epithelial sodium channel (ENaC) and serves as an inhibitor of the Na+/Ca2+ exchanger (NCX) with an IC50 of approximately 100 nM. This compound also enhances myogenic vasoconstriction and inhibits TRPP3-mediated Ca2+-activated currents at an IC50 of 1.1 μM. Benzamil hydrochloride is employed in various research applications aimed at studying ion channel regulation and cardiovascular physiology.

Items 2451-2500 of 2532

Page
per page
Set Descending Direction