Catalog No.
Product Name
Application
Product Information
Citations
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Nav1.7 Inhibitor
PF-05186462 is a selective inhibitor of the human Nav1.7 voltage-dependent sodium channel, exhibiting an IC50 value of 21 nM. This compound demonstrates a high degree of selectivity for Nav1.7 over other sodium channels, including Nav 1.1, 1.2, 1.3, 1.4, 1.5, 1.6, and 1.8. PF-05186462 is ideally suited for research applications focused on acute and chronic pain mechanisms. -
Antitussive Agent
Benzonatate is a non-narcotic peripheral antitussive agent that acts primarily by inhibiting reversible voltage-gated sodium channels. This compound effectively reduces the activity of cough stretch receptors, leading to a suppression of the cough reflex. Benzonatate is commonly utilized in research focusing on respiratory pathways and the modulation of cough response. -
Nav1.1 Inhibitor
AA43279 is a selective inhibitor of the Nav1.1 sodium channel (SCN1A), with an EC50 of 9.5 μM. This compound modulates the activity of gamma-aminobutyric acid (GABA) fast-firing interneurons, enhancing neuronal firing in vitro. AA43279 demonstrates anticonvulsant properties in the rat MEST model, making it a valuable tool for research involving epilepsy and related neurological disorders. -
Sodium Channel Modulator
ATX-II is a selective sodium channel modulator toxin that enhances late sodium current by preventing complete sodium channel inactivation, leading to persistent current fractions. This compound exhibits pro-arrhythmic effects, characterized by a slowed intrinsic heart rate, prolonged QT interval, and extended sinus node recovery time, potentially resulting in sinus pauses and arrests. ATX-II is valuable for research related to atrial fibrillation, long QT syndrome, and long QT3 syndrome. -
Aconitum Alkaloid
6-Benzoylheteratisine acts as an antagonist of tetrodotoxin and targets sodium channels, demonstrating potential neuroprotective activity. It effectively inhibits the influx of sodium ([Na+]i) and calcium ([Ca2+]i) ions, as well as the release of glutamate, making it relevant for the study of excitatory neurotransmission. Additionally, 6-Benzoylheteratisine has shown inhibitory effects on neuronal activity associated with epileptiform burst discharge, suggesting its utility in neurological research and potential therapeutic applications in epilepsy. -
Nav1.7 Antagonist
GX-674 is a potent antagonist of the voltage-gated sodium channel Nav1.7, exhibiting state-dependent and isoform-selective inhibition with an IC50 of 0.1 nM at -40 mV. This compound is valuable for research focused on pain pathways and neuropathic pain mechanisms, providing insights into the role of Nav1.7 in nociception and related disorders. Its high specificity and potency make it an essential tool for studying the therapeutic potential in pain management. -
Noradrenaline Reuptake Inhibitor
Atomoxetine is a selective noradrenaline reuptake inhibitor primarily targeting norepinephrine transporters with Ki values of 5 nM. It is known to increase dopamine and norepinephrine extracellular levels in the prefrontal cortex, thereby enhancing catecholaminergic neurotransmission. Additionally, Atomoxetine acts as a sodium channel blocker (VGSCs). This compound is widely utilized in research focusing on attention-deficit hyperactivity disorder (ADHD) and related neuropharmacological studies. -
Nav1.7/ Nav1.8 Blocker
ABBV-318 is a potent blocker of the voltage-gated sodium channels Nav1.7 and Nav1.8, demonstrating IC50 values of 2.8 μM and 3.8 μM for hNav1.7 and hNav1.8, respectively. This compound is of significant interest in pain research, providing insights into mechanisms of pain signaling and potential therapeutic avenues for pain management. Its specificity for Nav1.7 and Nav1.8 makes it a valuable tool for elucidating neuronal function and designing targeted analgesic strategies. -
Sodium Channel Blocker
Bliretrigine is a potent sodium channel blocker, primarily targeting voltage-gated sodium channels to modulate neuronal excitability. It has demonstrated significant analgesic properties, making it effective in alleviating pain associated with various neurological conditions. This compound is valuable for research into pain mechanisms and the development of novel analgesic therapies. -
Antiarrhythmic Agent
Ethacizine hydrochloride is a Class Ic antiarrhythmic agent that primarily targets sodium channels to modulate cardiac conduction. This compound is recognized for its long-lasting effects compared to other agents in its class, making it valuable for the management of arrhythmias. Ethacizine hydrochloride is utilized in research applications focused on cardiac electrophysiology and the mechanism of arrhythmias, providing insights into therapeutic interventions for cardiac disorders. -
Nav1.8 Inhibitor
Nav1.8-IN-2 is a selective inhibitor of the voltage-gated sodium channel Nav1.8, exhibiting a potent IC50 value of 0.4 nM. This compound is utilized in research related to various pain disorders, cough disorders, and both acute and chronic itch conditions. Its high affinity for Nav1.8 makes it a valuable tool for elucidating pain signaling pathways and developing therapeutic strategies for sensory nerve modulation. -
Sodium Channel Blocker
Co 102862 is a potent, broad-spectrum sodium channel blocker with state-dependent activity. This compound exhibits significant anticonvulsant properties, making it valuable for research in epilepsy and other neurological disorders. Its oral bioactivity supports its use in in vivo studies aimed at exploring sodium channel modulation in various therapeutic contexts. -
Anesthetic Agent
Etidocaine hydrochloride is a long-acting aminoamide local anesthetic that primarily targets sodium channels to inhibit neuronal excitability. It is effective in suppressing or relieving pain during surgical procedures and other medical applications requiring localized anesthesia. Its prolonged duration of action makes it suitable for various clinical settings. -
Sodium Channel Blocker
Aneratrigine is a selective blocker of the sodium channel protein type 9 subunit alpha, primarily inhibiting its activity. This compound exhibits significant potential in the study of neuropathic pain disorders, making it a valuable tool for research into pain management and associated neurological conditions. Researchers can utilize Aneratrigine to explore mechanisms of sodium channel modulation and its effects on neuronal excitability. -
ENaC Inhibitor
ETD001 is a potent ENaC (epithelial sodium channel) inhibitor, demonstrating an IC50 of 57.5 nM in cultured human bronchial epithelial (HBE) cells. This compound is particularly valuable for research applications related to cystic fibrosis, as it modulates sodium transport and influences fluid secretion in airway epithelium. Its long-acting properties make it an important tool for investigating ENaC's role in pulmonary pathophysiology and potential therapeutic interventions. -
Voltage-gated Sodium Channel Blocker
Mexiletine-d6 hydrochloride is a deuterated analog of Mexiletine hydrochloride, acting primarily as a voltage-gated sodium channel blocker. This compound is classified as a Class IB antiarrhythmic agent and exhibits non-selective inhibition of sodium channels. It is valuable in research applications focused on cardiac rhythm management and the modulation of neuronal excitability. -
NaV1.8 Blocker
PF-06305591 dihydrate is a selective blocker of the voltage-gated sodium channel NaV1.8, exhibiting an IC50 of 15 nM. This compound demonstrates significant potential for neurophatic pain research due to its ability to modulate sodium ion flux and reduce excitability in sensory neurons. Its favorable preclinical in vitro ADME and safety profile make it a valuable tool for studying pain mechanisms and developing analgesic therapies. -
Nav1.7 Inhibitor
PF-05198007 is a selective inhibitor of the Nav1.7 sodium channel, demonstrating potent and orally active properties. This compound is utilized in research focused on pain signaling pathways, specifically in the exploration of pain relief mechanisms and the development of analgesic therapies. Its pharmacodynamic profile aligns closely with that of PF-05089771, making it a valuable tool for studying Nav1.7-related biological processes. -
NaV1.7 Antagonist
(Rac)-AMG8379 is a potent antagonist of the NaV1.7 sodium channel, demonstrating selective inhibition with IC50 values of 8.5 nM for human NaV1.7 and 18.6 nM for mouse NaV1.7. This compound is known for its oral bioavailability and serves as a valuable tool in research focused on pain pathways and sodium channel modulation. Investigations utilizing (Rac)-AMG8379 can advance understanding of the role of NaV1.7 in nociception and related disorders. -
R-enantiomer of Funapide
(R)-Funapide is the R-enantiomer of Funapide, targeting the sodium channels Nav1.7 and Nav1.8, among others, in the peripheral nervous system. This compound exhibits biological activity as a sodium channel inhibitor, which may have implications in pain modulation. Research applications for (R)-Funapide include studies on analgesic mechanisms and the exploration of peripheral nerve functions. -
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. -
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. -
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 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. -
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. -
Alkaloid
Lipoaconitine is a natural alkaloid known for its regulatory effects on voltage-gated sodium channels. It exhibits notable biological activity, including analgesic and anti-inflammatory properties, making it a valuable tool for research in pain management and neurobiology. Its unique pharmacological profile provides insights into the mechanisms underlying sodium channel modulation and potential therapeutic applications. -
Drug Derivative
Flumethrin is a synthetic pyrethroid insecticide that acts primarily by modulating sodium channels in the nervous system of insects, leading to paralysis and death. This compound exhibits potent insecticidal activity against a wide range of pests, making it valuable in agricultural and veterinary applications. Flumethrin is primarily utilized in research settings to study insect behavior, insecticide resistance, and neurological pathways relevant to pest control strategies. -
Tocainid Analog
2-Amino-N-phenylpropanamide hydrochloride is an analog of Tocainid, an antiarrhythmic agent that modulates cardiac sodium channels. This compound exhibits potential in cardiac research by influencing ion channel function and demonstrating effects on arrhythmia management. It serves as a valuable tool for studies related to cardiovascular pharmacology and the development of novel antiarrhythmic therapies. -
Drug Derivative
Leucinocaine is a drug derivative that acts as a local anesthetic by inhibiting sodium channel activity, thereby blocking nerve impulse conduction. Its primary biological activity involves pain relief in localized areas, making it useful for various clinical and research applications in pain management and anesthetic studies. This compound can also serve as a valuable tool in neuropharmacological research and the development of new analgesic agents. -
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.
