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Pathways Recommended: Membrane Transporter/Ion Channel
Results for "

Ion channel blocker

" in MedChemExpress (MCE) Product Catalog:

100

Inhibitors & Agonists

1

Screening Libraries

4

Fluorescent Dyes

6

Peptides

9

Natural
Products

12

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-D0814
    DAPI dihydrochloride
    Maximum Cited Publications
    146 Publications Verification

    4',6-Diamidino-2-phenylindole dihydrochloride

    DNA Stain Sodium Channel Neurological Disease
    DAPI (4',6-Diamidino-2-phenylindole) dihydrochloride is a DAPI dye. DAPI is a fluorescent dye that binds strongly to DNA. It binds to the AT base pair of the double-stranded DNA minor groove, and one DAPI molecule can occupy three base pair positions. The fluorescence intensity of DAPI molecules bound to double-stranded DNA is increased by about 20 times, and it is commonly observed with fluorescence microscopy, and the amount of DNA can be determined based on the intensity of fluorescence. In addition, because DAPI can pass through intact cell membranes, it can be used to stain both live and fixed cells . DAPI (Compound 3) is an acid-sensing ion channel 3 (ASIC3) inhibitor. DAPI binds to ASIC3 and blocks the channel function. DAPI can be used in the study of chronic pain treatment (Ex/Em = 356/451 nm).
    DAPI dihydrochloride
  • HY-B0246
    Carbamazepine
    15+ Cited Publications

    CBZ; NSC 169864

    Sodium Channel Autophagy Mitophagy Potassium Channel Calcium Channel HDAC Neurological Disease Cancer
    Carbamazepine is an orally active pressure-sensitive sodium ion channel blocker with an IC50 of 131 μM. Carbamazepine blocks voltage gated Na +, Ca 2+, and K + channels, and is also a HDAC inhibitor (IC50: 2 μM). Carbamazepine is an anticonvulsant and can be used for research of epilepsy and neuropathic pain .
    Carbamazepine
  • HY-15206
    Glibenclamide
    25+ Cited Publications

    Glyburide

    Potassium Channel Mitochondrial Metabolism Autophagy CFTR P-glycoprotein Metabolic Disease
    Glibenclamide (Glyburide) is an orally active ATP-sensitive K + channel (KATP) inhibitor and can be used for the research of diabetes and obesity . Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR) . Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability . Glibenclamide can induce autophagy .
    Glibenclamide
  • HY-B1906
    Streptomycin
    Maximum Cited Publications
    46 Publications Verification

    Agrept; Agrimycin; Streptomycin A

    Environmental Pollutants Antibiotic Bacterial Infection Neurological Disease
    Streptomycin (Agrept) is an effective antibiotic against M. tuberculosis, is used for the research of tuberculosis (TB). Streptomycin also is a bacteriocidal agent that can be used for the research of a number of bacterial infections. Streptomycin can bind strongly to nucleic acids, interferes and blocks protein synthesis while permitting continued RNA and DNA synthesis. Streptomycin, as a common antibiotic used in culture media, also is a blocker of stretch-activated and mechanosensitive ion channels in neurons and cardiac myocytes .
    Streptomycin
  • HY-B1221
    Flufenamic acid
    5+ Cited Publications

    COX AMPK Potassium Channel Chloride Channel Calcium Channel Parasite Inflammation/Immunology
    Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
    Flufenamic acid
  • HY-P0190
    Iberiotoxin
    2 Publications Verification

    Potassium Channel Cardiovascular Disease
    Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels .
    Iberiotoxin
  • HY-W010950
    Flecainide
    3 Publications Verification

    Potassium Channel Sodium Channel Cardiovascular Disease
    Flecainide is an orally active antiarrhythmic agent. Flecainide can block sodium channels and inhibit calcium ion release mediated by the cardiac ryanodine receptor (RyR2). Flecainide can be used in the research of diseases such as catecholaminergic polymorphic ventricular tachycardia (CPVT) .
    Flecainide
  • HY-B0563
    Ropivacaine
    5+ Cited Publications

    Sodium Channel Potassium Channel Cardiovascular Disease Neurological Disease Cancer
    Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is used for the research of neuropathic pain management .
    Ropivacaine
  • HY-19765
    GSK2798745
    5+ Cited Publications

    TRP Channel Cardiovascular Disease
    GSK2798745 is a potent, selective, and orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. GSK2798745 can be used in cardiac and respiratory diseases research .
    GSK2798745
  • HY-33878

    Potassium Channel Proton Pump Neurological Disease
    2-PPA is a lysosomal potassium and proton channel TMEM175 pore blocker. 2-PPA binds at a TMEM175 pore site to occlude potassium and proton ion permeation pathways. 2-PPA increases lysosomal macromolecule catabolism, accelerates macropinocytosis. 2-PPA binds to hepatic protein in covalent. 2-PPA can be used for the research of Parkinson's disease .
    2-PPA
  • HY-B0338

    1-Rimantadine

    Influenza Virus Autophagy Infection
    Rimantadine (1-Rimantadine) is an orally active inhibitor for M2 protein, which blocks the hydrogen ion channel activity, prevents the entry and replication of the virus, and exhibits board-spectrum antiviral activity. Rimantadine significantly inhibits hepatitis A virus (HAV) replication at the post-entry stage in Huh7 cells. Rimantadine enhances autophagy. Rimantadine has a significant protective effect against H3N2 virus in mouse model .
    Rimantadine
  • HY-B0997

    Dihydroquinidine; (+)-Hydroquinidine; Hydroconquinine

    Others Cardiovascular Disease Cancer
    Hydroquinidine (Dihydroquinidine) is a potent ion channel blocker, which exhibits strong anti-cancer activity on colon, pancreatic, and hepatocellular cancer cells. Hydroquinidine prolongs the QT interval and has antiarrhythmic efficacy .
    Hydroquinidine
  • HY-B0338A

    Influenza Virus Autophagy Infection
    Rimantadine hydrochloride (Flumadine hydrochloride) is an orally active inhibitor for M2 protein, that blocks the hydrogen ion channel activity, prevents the entry and replication of the virus, and exhibits board-spectrum antiviral activity .
    Rimantadine hydrochloride
  • HY-B0563B
    Ropivacaine hydrochloride
    5+ Cited Publications

    Sodium Channel Potassium Channel Cardiovascular Disease Neurological Disease Cancer
    Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for neuropathic pain management in vivo .
    Ropivacaine hydrochloride
  • HY-17436

    Calcium Channel Cardiovascular Disease Cancer
    Clevidipine is a selective, short-acting L-type calcium channel antagonist with an IC50 of 7.1 nM. Clevidipine can competitively bind to calcium channels and exert rapid vasoselective vasodilation by blocking the influx of extracellular calcium ions, thereby reducing peripheral vascular resistance and effectively controlling acute severe hypertension. Clevidipine can also protect the myocardium from reperfusion injury by promoting the release of nitric oxide (NO). Clevidipine can be used in the research of acute hypertension, perioperative blood pressure management, and myocardial ischemia-reperfusion injury .
    Clevidipine
  • HY-D1738
    DAPI dilactate
    110+ Cited Publications

    4',6-Diamidino-2-phenylindole dilactate

    Fluorescent Dye Others
    DAPI (4',6-Diamidino-2-phenylindole) dilactate is a DAPI dye. DAPI is a fluorescent dye that binds strongly to DNA. It binds to the AT base pair of the double-stranded DNA minor groove, and one DAPI molecule can occupy three base pair positions. The fluorescence intensity of DAPI molecules bound to double-stranded DNA is increased by about 20 times, and it is commonly observed with fluorescence microscopy, and the amount of DNA can be determined based on the intensity of fluorescence. DAPI cannot penetrate intact cell membranes and is commonly used for staining both live and fixed cells . DAPI (Compound 3) is an acid-sensing ion channel 3 (ASIC3) inhibitor. DAPI binds to ASIC3 and blocks the channel function. DAPI can be used in the study of chronic pain treatment (Ex/Em = 356/451 nm) .
    DAPI dilactate
  • HY-B0023
    Azelnidipine
    3 Publications Verification

    CS 905

    Calcium Channel MEK Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    Azelnidipine (CS 905) is a dihydropyridine calcium channel blocker that is effective orally. Azelnidipine inhibits the intracellular calcium ion flow and lower blood pressure by selectively blocking L-type calcium channel on the membrane of vascular smooth muscle. Azelnidipine inhibits esophageal squamous cell carcinoma proliferation by targeting MEK1/2. Azelnidipine also has anti-inflammatory, antioxidant and neuroprotective effects .
    Azelnidipine
  • HY-A0082

    Difenidol hydrochloride

    mAChR Sodium Channel Neurological Disease
    Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea .
    Diphenidol hydrochloride
  • HY-15568
    A-317491
    5 Publications Verification

    P2X Receptor Neurological Disease Inflammation/Immunology
    A-317491 is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux .
    A-317491
  • HY-B0563A

    Sodium Channel Potassium Channel Cardiovascular Disease Neurological Disease Cancer
    Ropivacaine hydrochloride monohydrate is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for regional anesthesia and neuropathic pain management in vivo .
    Ropivacaine hydrochloride monohydrate
  • HY-B0563S1

    Isotope-Labeled Compounds Sodium Channel Potassium Channel Cardiovascular Disease Neurological Disease
    Ropivacaine-d7 is deuterium labeled Ropivacaine. Ropivacain is a potent?sodium channel?blocker. Ropivacain blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is used for the research of neuropathic pain?management .
    Ropivacaine-d7
  • HY-136832

    Serotonin Transporter Potassium Channel Arrestin Opioid Receptor Cardiovascular Disease Neurological Disease
    Noribogaine hydrochloride is an orally active, blood-brain barrier permeable SERT inhibitor (IC50=50-300 nM) and hERG channel blocker. Noribogaine hydrochloride enhances serotonergic transmission, activates the κ-opioid receptor (OPRK) G protein signaling pathway and inhibits β-arrestin recruitment. Meanwhile, Noribogaine hydrochloride blocks the μ-opioid receptor (OPRM) signaling pathway as well as ion channels associated with cardiac repolarization. Noribogaine hydrochloride induces neuritogenesis, upregulates GDNF mRNA expression, and modulates opioid tolerance. Noribogaine hydrochloride reduces alcohol-seeking behavior in experimental animals, and is widely used in studies related to depression, addiction, alcoholism, and cardiotoxicity .
    Noribogaine hydrochloride
  • HY-B1090

    Calcium Channel Histamine Receptor Cardiovascular Disease Endocrinology
    Cinnarizine is an orally active, effective and selective inhibitor of L-type calcium channel Cav1.3 with an IC50 of 1.5 μM (in vestibular hair cells). Cinnarizine can cross the blood-brain barrier and regulate calcium homeostasis and dopamine neurotransmission. Cinnarizine inhibits the influx of calcium ions into smooth muscle cells by blocking L-type calcium channels, thereby relaxing vascular smooth muscle, improving cerebral circulation and reducing blood viscosity, while antagonizing dopamine receptors. Cinnarizine can be used in the study of vestibular vertigo, Meniere's disease and cerebrovascular diseases .
    Cinnarizine
  • HY-D2868
    DAPI
    130+ Cited Publications

    4',6-Diamidino-2-phenylindole

    DNA Stain Sodium Channel Neurological Disease
    DAPI (4',6-Diamidino-2-phenylindole) is a DAPI dye. DAPI is a fluorescent dye that binds strongly to DNA. It binds to the AT base pair of the double-stranded DNA minor groove, and one DAPI molecule can occupy three base pair positions. The fluorescence intensity of DAPI molecules bound to double-stranded DNA is increased by about 20 times, and it is commonly observed with fluorescence microscopy, and the amount of DNA can be determined based on the intensity of fluorescence. In addition, because DAPI can pass through intact cell membranes, it can be used to stain both live and fixed cells . DAPI (Compound 3) is an acid-sensing ion channel 3 (ASIC3) inhibitor. DAPI binds to ASIC3 and blocks the channel function. DAPI can be used in the study of chronic pain treatment (Ex/Em = 356/451 nm).
    DAPI
  • HY-105028

    CP-66248

    COX Lipoxygenase Potassium Channel MMP Inflammation/Immunology
    Tenidap (CP-66248) is an orally active dual inhibitor of 5-LOX and COX with anti-inflammatory and immunomodulatory properties. Tenidap downregulates the expression of IL-1 receptors in chondrocytes, reduces the release of pro-inflammatory cytokines such as IL-1, IL-6 and TNF-α, and inhibits MMP production and cartilage degradation. Tenidap also blocks bone resorption and leukocyte adhesion to vascular endothelium, interferes with ion and pH changes associated with mouse sperm capacitation, and selectively enhances the activity of hKir2.3 channels (EC50=1.3 μM). Tenidap is applicable to research related to rheumatoid arthritis .
    Tenidap
  • HY-100607A

    ONO1101 hydrochloride

    Adrenergic Receptor Calcium Channel Potassium Channel Reactive Oxygen Species (ROS) Cardiovascular Disease Inflammation/Immunology Endocrinology
    Landiolol (ONO1101) hydrochloride is a highly selective, ultra-short-acting competitive inhibitor of β1 adrenergic receptors. Landiolol hydrochloride specifically blocks cardiac β1 receptors, reducing heart rate and myocardial oxygen consumption. Landiolol hydrochloride inhibits TNF-α-induced excessive mitochondrial oxygen consumption and reactive oxygen species production in a sepsis model, alleviating renal injury. Landiolol hydrochloride has little effect on cardiac ion channels (such as L-type calcium current and inward rectifier potassium current) and has a weak negative inotropic effect. Landiolol hydrochloride can be used for perioperative tachycardia control and protection studies of sepsis-related acute kidney injury .
    Landiolol hydrochloride
  • HY-B0246R

    CBZ (Standard); NSC 169864 (Standard)

    Reference Standards Sodium Channel Autophagy Mitophagy Potassium Channel Calcium Channel HDAC Neurological Disease Cancer
    Carbamazepine (Standard) is the analytical standard of Carbamazepine. This product is intended for research and analytical applications. Carbamazepine is an orally active pressure-sensitive sodium ion channel blocker with an IC50 of 131 μM. Carbamazepine blocks voltage gated Na +, Ca 2+, and K + channels, and is also a HDAC inhibitor (IC50: 2 μM). Carbamazepine is an anticonvulsant and can be used for research of epilepsy and neuropathic pain .
    Carbamazepine (Standard)
  • HY-W010950A
    Flecainide hydrochloride
    3 Publications Verification

    Potassium Channel Sodium Channel Cardiovascular Disease
    Flecainide hydrochloride is an orally active antiarrhythmic agent. Flecainide hydrochloride can block sodium channels and inhibit calcium ion release mediated by the cardiac ryanodine receptor (RyR2). Flecainide hydrochloride can be used in the research of diseases such as catecholaminergic polymorphic ventricular tachycardia (CPVT) .
    Flecainide hydrochloride
  • HY-A0079

    Amethocaine

    Sodium Channel Calcium Channel Neurological Disease
    Tetracaine (Amethocaine) is a sodium channel inhibitor and ryanodine receptor (RyR) inhibitor. Tetracaine blocks sodium conduction across nerve cell membranes, preventing rapid sodium ion influx and depolarization. Tetracaine exhibits biphasic effects on spontaneous sarcoplasmic reticulum Ca 2+ release in Ca 2+-overloaded ventricular myocytes, and increases sarcoplasmic reticulum Ca 2+ load. Tetracaine can be used in research related to eye diseases .
    Tetracaine
  • HY-15206S1

    Glyburide-d3

    Potassium Channel Mitochondrial Metabolism Autophagy CFTR P-glycoprotein Metabolic Disease
    Glyburide-d3 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
    Glyburide-d3
  • HY-N4246

    Aquaporin PKC Akt PI3K Apoptosis Monoamine Oxidase Pregnane X Receptor (PXR) Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    Bacopaside I is an orally active aquaporin AQP1 inhibitor and PKC modulator with neuroprotective and anticancer activities. Bacopaside I specifically blocks the water channel and cGMP-gated ion channel activities of AQP1 without affecting AQP4, thereby inhibiting the migration of colon cancer cells expressing AQP1. Bacopaside I activates the Akt pathway by interacting with PI3K, specifically inhibits MAO-A, effectively alleviates neuron necrosis and apoptosis induced by oxygen-glucose deprivation, reduces oxidative stress, and regulates the surface expression of neuroreceptors. When combined with Bacopaside II (HY-N6016), Bacopaside I significantly reduces the viability, proliferation and invasion ability of breast cancer cells, and binds to the pregnane X receptor (PXR). Bacopaside I is applicable to the research of colon cancer, breast cancer, vascular dementia, cerebral ischemia and other related diseases .
    Bacopaside I
  • HY-P0190A
    Iberiotoxin TFA
    2 Publications Verification

    Potassium Channel Others
    Iberiotoxin (TFA) is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin (TFA) does not block other types of voltage-dependent ion channels .
    Iberiotoxin TFA
  • HY-N2197
    Hirsuteine
    2 Publications Verification

    nAChR Neurological Disease
    Hirsuteine is an indole alkaloid extracted from Uncaria rhynchophylla. Hirsuteine non-competitively antagonizes nicotine-mediated dopamine release by blocking ion permeation through nicotinic receptor channel complexes .
    Hirsuteine
  • HY-110184

    Potassium Channel Neurological Disease
    PK-THPP is a potent and brain-penetrant TWIK-related acid-sensitive K + ion channel (K2P9.1 or TASK-3) blocker with IC50s of 35 nM and 300 nM for TASK-3 and TASK-1, respectively. PK-THPP shows no or less activity against other K + channels. PK-THPP is an effective breathing stimulant and can be used for the study of breathing disorders .
    PK-THPP
  • HY-178281

    Potassium Channel Sodium Channel Neurological Disease
    E0199 is a novel potent dual-target KV7/NaV modulator that activates the KV7 channel (KV7.2/7.3 (EC50 = 12.78 nM), KV7.2 (EC50 = 0.50 μM), and KV7.5 (EC50 = 27.14 nM) channels) while simultaneously blocks the NaV1.7 (IC50 = 0.52 μM), NaV1.8 (IC50 = 0.24 μM), and NaV1.9 (IC50 = 0.16 μM) channels. E0199 shows a potent analgesic effect without affecting heart and skeletal muscle ion channels critically in a chronic constriction injury (CCI) mouse model. E0199 can be used for Neuropathic pain (NP) research .
    E0199
  • HY-15206S

    Isotope-Labeled Compounds Potassium Channel Mitochondrial Metabolism Autophagy CFTR P-glycoprotein Metabolic Disease
    Glyburide-d11 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity . Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR) . Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability . Glibenclamide can induce autophagy .
    Glyburide-d11
  • HY-B0402S

    1-Adamantanamine-d15; 1-Aminoadamantane-d15

    Influenza Virus Orthopoxvirus SARS-CoV Apoptosis Infection Neurological Disease Cancer
    Amantadine-d15 is the deuterium labeled Amantadine. Amantadine (1-Adamantanamine) is an antiviral agent with activity against influenza A viruses. Amantadine blocks the proton flow through the M2 ion channel (M2 proton channel of influenza A) and thus prevents the release of viral RNA into the cytoplasm of the infected cells. Amantadine is an antiparkinsonian agent .
    Amantadine-d15
  • HY-106282

    HIV Infection
    BIT-225 is an inhibitor for Vpu protein through block of Vpu ion channel, and thus inhibits the release of HIV-1, especially in monocyte-derived macrophages (EC50 is 2.25 μM), without significant cytotoxicity (TC50 is 284 μM) .
    BIT-225
  • HY-B1906R

    Agrept (Standard); Agrimycin (Standard); Streptomycin A (Standard)

    Reference Standards Antibiotic Bacterial Infection Neurological Disease
    Streptomycin (Standard) is the analytical standard of Streptomycin. This product is intended for research and analytical applications. Streptomycin (Agrept) is an effective antibiotic against M. tuberculosis, is used for the research of tuberculosis (TB). Streptomycin also is a bacteriocidal agent that can be used for the research of a number of bacterial infections. Streptomycin can bind strongly to nucleic acids, interferes and blocks protein synthesis while permitting continued RNA and DNA synthesis. Streptomycin, as a common antibiotic used in culture media, also is a blocker of stretch-activated and mechanosensitive ion channels in neurons and cardiac myocytes .
    Streptomycin (Standard)
  • HY-A0236

    Sodium Channel Potassium Channel Calcium Channel Calmodulin Cardiovascular Disease
    Aprindine is an Ib-class anti-arrhythmic agent. Aprindine mainly exerts its effect by blocking sodium channels (INa), thereby reducing the excitability and conduction velocity of cardiac muscle cells. Aprindine significantly inhibits delayed potassium currents, which helps to prolong the atrial effective refractory period (AERP) and inhibit the occurrence of atrial fibrillation. Aprindine can also regulate intracellular calcium ion concentration by inhibiting Na +/Ca 2+ exchange current (INCX), thereby further stabilizing cardiac electrical activity. Aprindine can be used for the study of atrial fibrillation (AF) and ventricular arrhythmias .
    Aprindine
  • HY-N0927

    Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine

    Dopamine Receptor Others Neurological Disease
    (-)-Isocorypalmine (Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine) is a dopamine receptor ligand and modulator capable of crossing the blood-brain barrier. (-)-Isocorypalmine exhibits receptor selectivity, acting as a partial agonist of dopamine D1 and D5 receptors (coupled via Gs proteins), as well as an antagonist of D2, D3 and D4 receptors (by blocking Gi protein-mediated signaling). (-)-Isocorypalmine shows no significant binding to various non-dopamine receptors, ion channels and transporters. (-)-Isocorypalmine is metabolically stable in vivo, effectively inhibits spontaneous and cocaine-induced hyperlocomotion, sensitization and conditioned place preference in mice, and does not induce addictive place preference when administered alone. (-)-Isocorypalmine can be used in addiction research .
    (-)-Isocorypalmine
  • HY-P5142

    ω-ACTX-Hv1; ω-Atracotoxin-HV1

    Insecticide Calcium Channel Apoptosis Necroptosis Cardiovascular Disease Neurological Disease Inflammation/Immunology
    ω-Hexatoxin-Hv1a (ω-ACTX-Hv1; ω-Atracotoxin-HV1) is an orally active insecticidal neurotoxin containing an inhibitor cystine knot motif and a selective calcium channel inhibitor. ω-Hexatoxin-Hv1a blocks L-type voltage-dependent Ca 2+ channels and reduces intracellular calcium ion concentration, thereby decreasing apoptosis, necroptosis and oxidative stress, and promoting cell recovery and energy level elevation. ω-Hexatoxin-Hv1a causes larval paralysis and death by impairing neurotransmission in the central nervous system of insects. It shows high injectable toxicity against insects of multiple orders, but exhibits weak oral toxicity. ω-Hexatoxin-Hv1a is widely applicable to studies related to ischemia-reperfusion injury, atopic dermatitis, and ischemic injury of cardiomyocytes and neurons .
    ω-Hexatoxin-Hv1a
  • HY-W008581

    3-O-Methyl estradiol; 17β-Estradiol 3-methyl ether; 3-Methoxyestradiol

    Biochemical Assay Reagents TRP Channel Microtubule/Tubulin Autophagy Metabolic Disease Cancer
    Estradiol 3-methyl ether (EDME) is a highly selective TRPML1 ion channel antagonist and microtubule (microtubule) depolymerizing agent, with IC50 values of 0.22 μM and 3.8 μM against TRPML1 and TRPML2, respectively; it shows no activity against TRPML3. Estradiol 3-methyl ether induces the disruption of cytoplasmic microtubule networks in mammalian cells, with an EC50 of 9 μM. Independent of estrogen receptors, Estradiol 3-methyl ether blocks autophagy (autophagy), TFEB nuclear translocation, and inhibits the migration and invasion of triple-negative breast cancer cells by suppressing TRPML1. Estradiol 3-methyl ether is applicable for relevant research on triple-negative breast cancer .
    Estradiol 3-methyl ether
  • HY-15568A
    A-317491 sodium salt hydrate
    5 Publications Verification

    P2X Receptor Neurological Disease Inflammation/Immunology
    A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 sodium salt hydrate is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux .
    A-317491 sodium salt hydrate
  • HY-161092A

    HCN Channel Potassium Channel Neurological Disease
    KIO-301 chloride hydrochloride is an azobenzene photoswitchable compound that blocks voltage-gated ion channels, including hyperpolarization-activated cyclic nucleotide gating (HCN, during exposure to visible light) ) and voltage-gated potassium channels (voltage-gated potassium channels) .
    KIO-301 chloride hydrochloride
  • HY-161092

    HCN Channel Potassium Channel Neurological Disease
    KIO-301 chloride is an azobenzene photoswitch compound that can block voltage-gated ion channels, including hyperpolarisation-activated cyclic nucleotide-gated (HCN) and voltage-gated potassium channels during exposure to visible light .
    KIO-301 chloride
  • HY-135000

    DcSTX; DecarbamoylSTX

    Endogenous Metabolite Drug Metabolite Neurological Disease
    Decarbamoylsaxitoxin is a sodium channel inhibitor that blocks the influx of sodium ions through the membranes of excitable nerves and skeletal muscle cells, thereby preventing the formation of action potentials. Decarbamoylsaxitoxin is an acidic hydrolysis product of saxitoxin, and its toxic effects on mice are identical to those of saxitoxin. Decarbamoylsaxitoxin inhibits veratridine- and ouabain-induced swelling and lysis of mouse neuroblastoma cells by blocking Na + channels. Decarbamoylsaxitoxin can be used in studies related to paralytic shellfish poisoning .
    Decarbamoylsaxitoxin
  • HY-P2707

    α-DTX

    Sodium Channel Potassium Channel Neurological Disease
    α-Dendrotoxin (α-DTX) is a voltage-gated K + channel blocker and an acid-sensing ion channel (ASIC) inhibitor. α-Dendrotoxin blocks Kv1.1, Kv1.2, Kv1.6 and D-type (ID) voltage-gated K + channels, and reversibly inhibits slowly inactivating potassium currents. α-Dendrotoxin induces epilepsy-related behaviors in mice. α-Dendrotoxin can be used in studies related to tonic-clonic seizures .
    α-Dendrotoxin
  • HY-W009065

    Others Cardiovascular Disease Cancer
    Hydroquinidine hydrochloride is a potent ion channel blocker, which exhibits strong anti-cancer activity on colon, pancreatic, and hepatocellular cancer cells. Hydroquinidine hydrochloride prolongs the QT interval and has antiarrhythmic efficacy .
    Hydroquinidine hydrochloride
  • HY-A0236A

    Sodium Channel Potassium Channel Calcium Channel Calmodulin Cardiovascular Disease
    Aprindine hydrochloride is an Ib-class anti-arrhythmic agent. Aprindine hydrochloride mainly exerts its effect by blocking sodium channels (INa), thereby reducing the excitability and conduction velocity of cardiac muscle cells. Aprindine hydrochloride significantly inhibits delayed potassium currents, which helps to prolong the atrial effective refractory period (AERP) and inhibit the occurrence of atrial fibrillation. Aprindine hydrochloride can also regulate intracellular calcium ion concentration by inhibiting Na +/Ca 2+ exchange current (INCX), thereby further stabilizing cardiac electrical activity. Aprindine hydrochloride can be used for the study of atrial fibrillation (AF) and ventricular arrhythmias .
    Aprindine hydrochloride

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