Catalog No.
Product Name
Application
Product Information
Citations
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Glucokinase Activator
Glucokinase activator 3 is a potent activator of glucokinase (GK) with an AC50 of 38 nM. This compound has demonstrated significant efficacy in reducing blood glucose levels in diet-induced obese (DIO) mice, highlighting its potential in type 2 diabetes research. Additionally, glucokinase activator 3 has been shown to inhibit the hERG channel and sodium channels in patch clamp assays, providing insight into its pharmacological profile. -
Analgesic Agent
(+)-Mepivacaine is an amide-type local anesthetic that exhibits potent analgesic and vasoconstrictive properties. By selectively binding to voltage-gated sodium channels on neuronal cell membranes, it effectively inhibits sodium influx, leading to a temporary loss of sensation in targeted areas. This compound is widely utilized in various research applications, particularly in studies focused on pain management and anesthesia. -
Antiarrhythmic Agent
(S)-Propafenone is an antiarrhythmic agent that functions primarily as a sodium channel blocker. This compound exhibits beta-blocking properties and demonstrates class 1 antiarrhythmic activity, making it valuable in the study of cardiac arrhythmias. Its efficacy in modulating myocardial excitability and conduction makes it an important tool for research applications aimed at understanding arrhythmic disorders and developing therapeutic strategies. -
Sodium Channel Blocker
Zilvetrigine is a sodium channel blocker that selectively inhibits voltage-gated sodium channels. This compound exhibits analgesic properties, making it valuable for pain management research. Its mechanism of action can be explored in studies related to neuropathic pain and other conditions mediated by sodium channel activity. -
Cardioactive Agent
DPI 201-106 is a cardiotonic agent that exerts its effects through a synergistic mechanism involving both sarcolemmal and intracellular pathways. It selectively modulates voltage-gated sodium channels (VGSCs), leading to a significant positive inotropic effect. This compound is useful for research applications focused on cardiac function and the modulation of ion channel activity in cardiac tissues. -
Sodium Channel Blocker
Tocainide hydrochloride is a sodium channel blocker that inhibits the activity of voltage-gated sodium channels, effectively reducing neuronal excitability in pain pathways. This compound is primarily used in research related to pain mechanisms and the treatment of conditions such as tinnitus. Tocainide hydrochloride functions as a primary amine analog of lidocaine, providing insights into sodium channel modulation and its therapeutic potential. -
Sodium Channel Inhibitor
Licarbazepine-d4 is a deuterated derivative of Licarbazepine, functioning as a sodium channel inhibitor. This compound exhibits anticonvulsant and mood-stabilizing properties, making it a valuable tool in the study of neurological disorders. It is particularly useful for researchers investigating the mechanisms of epilepsy and mood regulation. -
VGSC Blocker
KC 12291 hydrochloride is a potent blocker of voltage-gated sodium channels (VGSC). It effectively reduces sustained Na+ current amplitude, demonstrating notable anti-ischemic properties. This compound exhibits significant cardioprotective effects in both in vitro and in vivo studies, making it a valuable tool for cardiac research and the investigation of sodium channel-related pathophysiology. -
Sodium Channels Blocker
Phrixotoxin 3 is a selective blocker of voltage-gated sodium channels, demonstrating IC50 values of 0.6 nM for NaV1.2, 42 nM for NaV1.3, 72 nM for NaV1.4, 288 nM for NaV1.1, and 610 nM for NaV1.5. This compound modulates sodium channel activity by shifting gating kinetics in a depolarized direction while inhibiting the inward sodium current. Phrixotoxin 3 is valuable for research focusing on ion channel modulation, neurophysiology, and the investigation of sodium channel-related pathologies. -
Sodium Current Blocker
F-15845 hydrobromide is a potent persistent sodium current blocker, primarily targeting voltage-gated sodium channels. It demonstrates significant cardioprotective properties and anti-ischemic activity, providing both short- and long-term protection following myocardial infarction. This compound is valuable for investigating functional impairments in the myocardium and exploring therapeutic strategies related to cardiac health. -
Sodium Channel Antagonist
Hainantoxin-IV is an antagonist of voltage-gated sodium channels, specifically targeting tetrodotoxin-sensitive (TTX-S) subtypes. This compound exhibits potent inhibitory activity through its interaction with key residues His28 and Lys32, which facilitate binding to the sodium channel. Hainantoxin-IV, characterized by an inhibitor cystine knot motif, is valuable in research applications exploring sodium channel modulation and related neurophysiological processes. -
NMDA Receptor Antagonist
Remacemide hydrochloride is a weak uncompetitive antagonist of the NMDA receptor, exhibiting IC50 values of 68 μM for MK-801 binding and 76 μM for NMDA-induced currents. As a moderate inhibitor of sodium channels, this compound demonstrates anticonvulsant properties, making it a valuable tool in the study of neuropharmacology. Research applications include investigating mechanisms underlying seizure disorders and testing potential therapeutic approaches for neurological conditions. -
AMPA Receptor Antagonist
Irampanel is an AMPA receptor antagonist that selectively blocks excitatory neurotransmission by inhibiting AMPA receptor activity. Additionally, it acts as a voltage-dependent sodium channel blocker, leading to a decrease in neuronal excitability. This compound has demonstrated efficacy in reducing kainate-induced currents in rat cortical neurons, making it a valuable tool for research applications related to neuropharmacology and the investigation of excitatory synaptic transmission. -
AMPA Receptor Antagonist
Irampanel hydrochloride is a potent antagonist of the AMPA receptor, acting primarily on excitatory glutamate signaling pathways. This compound effectively blocks voltage-dependent sodium channels and inhibits kainic acid-induced currents in rat cortical neurons. It is primarily used in research applications focused on neuroprotection, synaptic plasticity, and the study of neurodegenerative diseases. -
NET Inhibitor
Nisoxetine is a potent and selective inhibitor of the norepinephrine transporter (NET) with a Kd of 0.76 nM. This compound exhibits antidepressant properties and functions as a local anesthetic, in addition to blocking voltage-gated sodium channels. Its mechanisms make it valuable for research in neuropharmacology and the investigation of depression and pain pathways. -
Sodium-Calcium Exchanger Inhibitor
KB-R7943 is a selective inhibitor of the sodium-calcium exchanger, exhibiting an IC50 value of 5.1 µM. This compound is utilized as a valuable tool in studies involving cardiac and renal failure models, facilitating research into calcium homeostasis and its implications in heart and kidney function. -
Sodium Channel Inhibitor
Benzamil is a sodium channel inhibitor, functioning as a non-selective blocker of epithelial sodium channels (ENaC) and a Na+/Ca2+ exchanger (NCX) inhibitor with an IC50 value of approximately 100 nM. Its pharmacological properties include the enhancement of myogenic vasoconstriction. Additionally, Benzamil inhibits TRPP3-mediated Ca2+-activated currents, exhibiting an IC50 of 1.1 μM. This compound is valuable for research applications focused on cardiovascular physiology and electrolyte transport mechanisms. -
Antiepileptic Compound
Losigamone is an orally active antiepileptic compound that primarily targets sodium channels. It enhances GABA-mediated responses by stimulating neuronal chloride channels, thus increasing chloride influx. This mechanism effectively reduces epileptiform activity induced by chloride channel antagonists, making Losigamone a valuable tool for research in epilepsy and related neuronal disorders. -
Insecticide
Leporin A is an insecticide that primarily targets GABA receptors and sodium channels, disrupting neurotransmission in insects. This mechanism leads to paralysis and mortality, making Leporin A a potent agent for agricultural pest control. It is utilized in research focused on insect physiology and pest management strategies. -
Insecticide
Insecticidal agent 21 is a potent insecticide primarily targeting Culex pipiens larvae with an LC50 of 0.4 μg/mL. This compound exerts multi-target neurotoxicity by inhibiting acetylcholinesterase (AChE) and affecting multiple neural receptors, including nicotinic acetylcholine receptors (nAChR), voltage-gated sodium channels (VGSC), and γ-aminobutyric acid receptors (GABAAR). Insecticidal agent 21 demonstrates a strong insecticidal effect and is suitable for research applications focused on developing novel insecticides to combat resistance in mosquito populations. -
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. -
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. -
Anti-Anrhythmic Agent
Aprindine hydrochloride is an Ib-class anti-arrhythmic agent primarily targeting sodium channels (INa) to reduce the excitability and conduction velocity of cardiac muscle cells. By significantly inhibiting delayed potassium currents, it prolongs the atrial effective refractory period (AERP) and mitigates the risk of atrial fibrillation. Additionally, Aprindine hydrochloride modulates intracellular calcium ion concentration through the inhibition of Na+/Ca2+ exchange current (INCX), further enhancing the stability of cardiac electrical activity. This compound is suitable for research focused on atrial fibrillation (AF) and ventricular arrhythmias. -
Anti-arrhythmic Agent
Aprindine is an Ib-class antiarrhythmic agent that primarily targets sodium channels (INa) to reduce the excitability and conduction velocity of cardiac muscle cells. Its ability to significantly inhibit delayed potassium currents prolongs the atrial effective refractory period (AERP), thereby helping to prevent atrial fibrillation. Additionally, Aprindine modulates intracellular calcium levels by inhibiting the Na+/Ca2+ exchange current (INCX), further stabilizing cardiac electrical activity. This compound is useful for research into atrial fibrillation (AF) and ventricular arrhythmias. -
Nav Channel Blocker
ProTx-I is a potent blocker of voltage-gated Na+ channels, specifically inhibiting NaV1.2, NaV1.6, and NaV1.7 with IC50 values of 104 nM, 21 nM, and 95 nM, respectively. Additionally, ProTx-I exhibits significant activity as a CaV3.1 channel blocker, demonstrating IC50 values of 0.2 μM for hCaV3.1 and 31.8 μM for hCaV3.2. It also inhibits KV 2.1 channels (IC50: 411 nM) and TRPA1 (IC50: 389 nM). This multi-targeting profile makes ProTx-I valuable for research in neurobiology and pain signaling pathways. -
Stable Isotope
Ranolazine-d3 is a deuterated form of Ranolazine, an anti-anginal agent that primarily inhibits the late phase of inward sodium current (INa) with an IC50 value of 6 μM and IKr with an IC50 value of 12 μM, leading to its therapeutic effects without altering heart rate or blood pressure. Additionally, Ranolazine acts as a partial fatty acid oxidation (FAO) inhibitor. This compound serves as a valuable tool in cardiovascular research, particularly in studying sodium channel activity and metabolic modulation in heart physiology. -
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. -
Calcium/Sodium Channel Blocker
Elpetrigine is a potent calcium and sodium channel blocker with significant anticonvulsant, antidepressant, antimania, and anxiolytic properties. This compound is primarily utilized in research focused on epilepsy and bipolar disorder, contributing to the understanding of neurological and mood disorders. Its mechanism of action makes it a valuable tool for exploring therapeutic avenues in these conditions. -
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. -
Broad-Spectrum Antiepileptic Agent
JNJ-26990990 is a broad-spectrum antiepileptic agent that primarily targets voltage-gated sodium channels and N-type calcium channels. It exhibits significant anticonvulsant activity, making it suitable for the study of various seizure models. Although it shows minimal inhibition of human carbonic anhydrase-II with an IC50 of 110 μM, its primary applications lie in the investigation of epilepsy and related neurological disorders. -
Sodium/Calcium Channel Blocker
KT 2-230 is a sodium and calcium channel blocker that exhibits significant anti-inflammatory properties. This compound is utilized in research applications focused on neuropathic pain and various inflammatory conditions. Its ability to modulate ion channel activity makes it a valuable tool for studying the underlying mechanisms of synaptic transmission and neuroprotection. -
Calcium/Sodium Channel Blocker
LY393615 (NCC1048) is a selective blocker of neuronal calcium (Ca2+) and sodium (Na+) channels, demonstrating IC50 values of 1.9 μM and 5.2 μM for the α1A and α1B calcium channel subunits, respectively. This compound exhibits excellent brain penetration and displays neuroprotective effects in cerebral ischemia models, making it a valuable tool for research in neurological diseases. Its dual-channel blocking mechanism contributes to its potential applications in understanding neuronal excitability and neuroprotection. -
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. -
Nav1.2 Inhibitor
Nav1.2-IN-2 is a potent inhibitor of the voltage-gated sodium channel Nav1.2, demonstrating an IC₅₀ of 0.18 μM for channel inactivation. It effectively reduces both the amplitude and frequency of spontaneous synchronous calcium oscillations with IC₅₀ values of 0.38 μM and 0.88 μM, respectively. Additionally, Nav1.2-IN-2 inhibits calcium influx triggered by Veratridine with an IC₅₀ of 1.89 μM. This reagent is relevant for research into neurological disorders such as epilepsy. -
T-type Ca2+ Channel Antagonist
U 92032 is a T-type Ca2+ channel antagonist that effectively inhibits sodium channels. This compound has been shown to disrupt thalamic oscillations, providing valuable insights into the mechanisms underlying neurological disorders. U 92032 is applicable in research focused on various neurological diseases, making it a significant tool for studying calcium signaling and excitability in the central nervous system. -
Calcium Channel/Sodium Channel Antagonist
EO-122 is a potent antagonist targeting calcium and sodium channels. It exhibits significant inhibitory activity, making it a valuable tool for studying mechanisms related to arrhythmias. This compound aids in the exploration of cardiac and neuronal excitability, facilitating research into related therapeutic strategies. -
Calcium/Sodium Channel Blocker
LY393615 free base is an effective blocker of neuronal calcium (Ca²⁺) and sodium (Na⁺) channels, exhibiting IC50 values of 1.9 μM and 5.2 μM for the α1A and α1B calcium channel subunits, respectively. This compound demonstrates substantial brain penetration and offers neuroprotective properties in cerebral ischemia models. It serves as a valuable tool in neurological disease research, providing insight into the pathophysiology of various neurodegenerative conditions. -
Multi-ion channel Blocker
Sulcardine hydrochloride is a multi-ion channel blocker primarily targeting sodium (INa) and calcium (ICa) channels, exhibiting IC50 values of 26.9 µM and 69.2 µM, respectively. This compound effectively inhibits the hNav1.5 channel and demonstrates a mild inhibitory effect on hERG channels. Due to its pharmacological properties, Sulcardine hydrochloride is often utilized in research related to anti-arrhythmic effects and cardiac electrophysiology. -
Stable Isotope
Ranolazine-d8 is a deuterated form of Ranolazine, which primarily targets the late phase of inward sodium current (INa) and potassium current (IKr) with IC50 values of 6 μM and 12 μM, respectively. This compound functions as an anti-anginal agent, alleviating symptoms without influencing heart rate or blood pressure. Additionally, Ranolazine acts as a partial fatty acid oxidation inhibitor, making it valuable for research related to cardiac ischemia and metabolic modulation in heart diseases. -
Calcium Channel Blocker
PD 122860 is a calcium channel blocker that also exhibits the ability to stimulate sodium channels. It is primarily utilized in research focused on cardiovascular and cerebrovascular diseases. By modulating calcium and sodium ion flux, PD 122860 contributes to understanding the underlying mechanisms of these conditions. -
Furin Inhibitor
BOS-318 is a highly selective and cell-permeable inhibitor of furin, exhibiting an IC50 value of 1.9 nM. This compound demonstrates the ability to protect epithelial sodium channels (ENaC) from activation by neutrophil elastase. BOS-318 is a valuable tool for research focused on cystic fibrosis and related pulmonary conditions. -
Antiarrhythmic Agent
Droxicainide hydrochloride is an antiarrhythmic agent primarily targeting sodium channels. It is effective in the management of ventricular arrhythmias and is utilized in research to investigate cardiac electrophysiology. The compound is valuable for studying interactions in cardiac tissues and assessing the effects of sodium channel modulation on heart rhythm disorders. -
Stable Isotope
Safinamide-d4-1 is a deuterium-labeled derivative of Safinamide, a selective and reversible inhibitor of monoamine oxidase B (MAO-B) with an IC50 of 0.098 μM, demonstrating significantly lower inhibition of MAO-A (IC50=580 μM). In addition to its MAO-B inhibitory activity, Safinamide also interacts with sodium channels and modulates glutamate release, exhibiting a greater affinity at depolarized potentials (IC50=8 μM) compared to resting potentials (IC50=262 μM). This reagent is valuable for research applications related to neurobiology, particularly in the investigation of Parkinson's disease and ischemic stroke mechanisms. -
Drug Impurity
N-(2,6-dimethylphenyl)-2-(ethyl(methyl)amino)acetamide hydrochloride is a recognized impurity associated with the sodium channel inhibitor Lidocaine. This compound may serve as a reference standard for quality control and analytical studies within pharmacological research. It can aid in the assessment of drug purity and the validation of analytical methods used in drug development and manufacturing processes. -
Drug Impurity
Lidocaine impurity 12 is a known impurity of the local anesthetic Lidocaine, which primarily acts as a sodium channel blocker. This compound is valuable for research involving drug formulation and stability studies, as it aids in understanding the impact of impurities on pharmacological profiles. Its characterization is essential for ensuring the quality and safety of Lidocaine-containing formulations. -
Drug Impurity
Ranolazine impurity 10 is a chemical impurity associated with the cardiovascular drug Ranolazine, which primarily targets sodium channels. This impurity is significant for analytical and quality control purposes in pharmaceutical research and development, aiding in the assessment of the drug's purity and safety profile. Its identification and quantification are critical for compliance with regulatory standards in the drug manufacturing process. -
Phosphate Ester Prodrug
Fosphenytoin is a phosphate ester prodrug that acts as a rapid-acting antiepileptic agent, primarily targeting sodium channels to stabilize neuronal membranes. It demonstrates significant efficacy in the acute management of seizures, particularly in emergency settings. Fosphenytoin's formulation allows for convenient intravenous and intramuscular administration, reducing the risk of local adverse reactions and facilitating effective treatment in acute care situations. -
Tropane
Tropacocaine hydrochloride is a tropane derivative that acts primarily as a local anesthetic by blocking sodium channels in neuronal membranes. Its key biological activity includes analgesic effects, making it valuable in pain research and studies of neuronal signaling. Tropacocaine hydrochloride is utilized in investigations of tropane-based compounds and their pharmacological profiles in the context of neurological studies. -
Drug Derivative
Piridocaine hydrochloride is a derivative of ortho-aminobenzoic acid and functions as a local anesthetic agent. It primarily acts by blocking sodium channels, thereby inhibiting action potential propagation in excitable membranes. This compound plays a significant role in research related to pain management, neuromuscular function, and pharmacological studies of anesthetics. Its unique pharmacological profile makes it a valuable tool for investigating local anesthetic mechanisms and applications in various biological systems. -
Drug Derivative
Nav1.7-IN-17 is a derivative compound targeting the voltage-gated sodium channel NaV1.7. This compound demonstrates significant inhibitory activity, making it a valuable tool for studying pain mechanisms and nociception. Its application is particularly relevant in pain research and the development of novel analgesics.
