Catalog No.
Product Name
Application
Product Information
Citations
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NaV1.7 Inhibitor
GDC-0276 is a selective and reversible inhibitor of the NaV1.7 ion channel with an IC50 value of 0.4 nM. This orally active compound demonstrates favorable pharmacokinetic properties and is well tolerated, making it a promising candidate for pain management. GDC-0276 may offer an alternative to existing analgesics, addressing issues such as addiction and off-target side effects in the treatment of various pain disorders. -
Sodium Channel Blocker
A-887826 is a selective voltage-dependent sodium channel blocker targeting Na(v)1.8, exhibiting a potent IC50 of 11 nM. This compound has demonstrated efficacy in attenuating neuropathic tactile allodynia in vivo, making it a valuable tool for researching pain mechanisms and potential therapeutic interventions for neuropathic pain conditions. Its oral bioavailability further supports its utility in preclinical studies. -
Nav1.7 Inhibitor
GDC-0310 is a selective inhibitor of the Voltage-gated sodium channel Nav1.7, demonstrating a potent inhibitory activity with an IC50 of 0.6 nM against hNav1.7. This compound is primarily utilized in research exploring pain mechanisms, particularly in the context of chronic pain and neuropathic pain models. Its specificity makes it a valuable tool for investigating Nav1.7's role in various physiological and pathophysiological processes. -
NaV1.8 Inhibitor
VX-150 is a highly selective inhibitor of the sodium channel NaV1.8. This compound demonstrates significant analgesic properties and shows potential for research in various pain-related indications. Its oral bioavailability makes it a valuable tool for studies investigating pain mechanisms and the development of novel pain therapies. -
Nav1.1 Activator
Lu AE98134 is a selective activator of voltage-gated sodium channel Nav1.1, functioning as a positive modulator. It also enhances the activity of Nav1.2 and Nav1.5 channels, while exhibiting no effect on Nav1.4, Nav1.6, or Nav1.7 channels. This compound serves as a valuable tool for investigating the pathophysiological roles of Nav1.1 in various central nervous system disorders, including potential applications in cognitive improvement in schizophrenia. -
NaV1.6/NaV1.2 Inhibitor
XPC-5462 is a selective inhibitor of the voltage-gated sodium channels NaV1.6 and NaV1.2, exhibiting IC50 values of 10.9 nM and 10.3 nM, respectively. It effectively suppresses epileptiform activity in ex vivo brain slice seizure models, making it a valuable tool for research in epilepsy and related neurological disorders. Its ability to modulate excitability in neuronal populations highlights its potential for studying sodium channel dynamics and their role in neuronal excitability. -
Sodium Channel Inhibitor
RY796 is a selective sodium channel inhibitor targeting voltage-gated sodium channels. Its potent activity has demonstrated analgesic effects, making it relevant for pain research. This compound can be utilized in studies investigating the modulation of sodium channels in various physiological and pathological conditions. -
Nav1.8 Inhibitor
Sodium Channel Inhibitor 6 is a selective Nav1.8 inhibitor primarily targeting voltage-gated sodium channels associated with neuronal excitability. It demonstrates significant biological activity in modulating pain pathways, making it a valuable tool for research on neuropathic pain mechanisms. This compound is suitable for in vitro and in vivo studies aimed at understanding the role of Nav1.8 in pain signaling and potential therapeutic interventions. -
ENaC Inhibitor
Phenamil methanesulfonate is a potent inhibitor of the epithelial sodium channel (ENaC), exhibiting an IC50 of 400 nM. In addition, it competitively inhibits TRPP3, with an IC50 of 140 nM, thereby blocking TRPP3-mediated calcium transport. This compound has potential applications in promoting bone repair by strongly activating the BMP signaling pathway and is valuable in research related to cystic fibrosis lung disease. -
Nerve Conduction Blocker
Butacaine is a reversible nerve conduction blocker that primarily targets voltage-gated sodium channels to inhibit nerve impulses, resulting in sensory and motor paralysis. This compound is commonly utilized in research as a negative control for local anesthetics. Butacaine is known to form inclusion complexes with α-cyclodextrin and β-cyclodextrin, enhancing its solubility and stability in biological applications. Its properties make it valuable for studying mechanisms of local anesthesia and nerve conduction. -
NaV1.8 Inhibitor
PF-04885614 is a potent inhibitor of the sodium channel NaV1.8, primarily involved in pain signaling pathways. Its inhibition may provide therapeutic benefits for managing neurological and neurodevelopmental disorders. This compound is valuable for research applications focused on pain mechanisms and the development of analgesic therapies. -
Pyrethroid Insecticide
S-Bioallethrin, a pyrethroid insecticide, primarily targets voltage-gated sodium channels, disrupting nerve function by altering the gating kinetics between conducting and nonconducting states. This compound exhibits significant biological activities, including the inhibition of lymphocyte proliferation and the induction of histamine release from human basophils. S-Bioallethrin is commonly utilized in studies investigating insecticidal mechanisms and the effects of neurotoxic compounds on immune responses. -
Insecticide
(±)-Indoxacarb is a broad-spectrum oxadiazine insecticide that exerts its effects by blocking sodium channels in insect nerve preparations and isolated neurons. This mechanism results in significant insecticidal activity while maintaining low toxicity to mammals. It is primarily utilized in research applications focusing on pest control and insect physiology. -
Antiarrhythmic Agent
Mexiletine is an orally active antiarrhythmic agent that primarily targets sodium channels to exert its effects, with IC50 values of 75±8 μM for tonic block and 23.6±2.8 μM for use-dependent block. In addition to its antiarrhythmic properties, Mexiletine has demonstrated efficacy in treating myotonia and neuropathic pain. This compound is valuable for research applications in both cardiovascular and neurological studies, providing insights into channelopathies and pain mechanisms. -
Sodium Channel Blocker
Licarbazepine is a voltage-gated sodium channel blocker that demonstrates anticonvulsant and mood-stabilizing properties. Its mechanism of action involves inhibiting sodium influx, which leads to a reduction in neuronal excitability. This compound is primarily utilized in research related to epilepsy and mood disorders, providing a valuable tool for investigating potential therapeutic interventions. -
Pyrethroid
Cyfluthrin is a type II pyrethroid that primarily targets Nav1.8 sodium channels, leading to prolonged stimulation of neuronal activity in insects. This compound exhibits potent insecticidal activity against a variety of pest species, making it suitable for applications in agriculture and veterinary practices, as well as in stored product protection. Its efficacy as an insecticide is attributed to its ability to disrupt normal neural function in target organisms. -
CRMP2-Ubc9 Interaction/NaV1.7 Inhibitor
AZ194 is a novel, orally active inhibitor that targets the interaction between CRMP2 and Ubc9, functioning as a specific inhibitor of NaV1.7 with an IC50 of 1.2 μM. By blocking the SUMOylation process of CRMP2, AZ194 effectively reduces the surface expression of NaV1.7, demonstrating significant antinociceptive properties. This agent is useful for research in pain modulation and associated neurological studies. -
Sodium Channel Inhibitor
3'-Methoxydaidzein is an isoflavone acting as a sodium channel inhibitor. It selectively inhibits sodium channel subtypes NaV1.7, NaV1.8, and NaV1.3 with IC50 values of 181 nM, 397 nM, and 505 nM, respectively. This compound exhibits significant analgesic activity through its modulation of voltage-gated sodium channels, making it a valuable tool for research in pain pathways and related therapeutic applications. -
Sodium Channels Inhibitor
Vormatrigine is an orally active inhibitor of sodium channels, demonstrating anti-epileptic properties. This compound is utilized in research to investigate human focal and generalized epilepsy, providing insights into its mechanisms and potential therapeutic applications. Its effectiveness in modulating sodium channel activity makes it a valuable tool for studying epilepsy-related pathophysiology. -
NaV1.7 Inhibitor
DS-1971a is a selective and orally bioavailable inhibitor of the voltage-gated sodium channel NaV1.7, with IC50 values of 22.8 nM and 59.4 nM for human and murine NaV1.7, respectively. This compound demonstrates significant analgesic properties, making it a valuable tool for research in pain management and neurological studies. Its specificity for NaV1.7 positions DS-1971a as an important reagent for exploring the mechanisms of pain signaling and potential therapeutic interventions. -
Sodium Channel Blocker
Evenamide is an orally available voltage-gated sodium channel blocker (Ki = 0.4 µM) primarily targeted for research in schizophrenia. It demonstrates efficacy across a variety of rodent models representing psychosis, mania, depression, and aggressive behavior. This compound serves as a valuable tool for investigating the underlying mechanisms of these psychiatric conditions and evaluating potential therapeutic interventions. -
Anesthetic Agent
Oxybuprocaine is a short-acting ester anesthetic that targets sodium channels to stabilize neuronal membranes reversibly. It exhibits cutaneous analgesic properties and is known for having a lower potency in inducing central nervous system and cardiovascular toxicity compared to other anesthetics. Commonly utilized in ophthalmology and otolaryngology, Oxybuprocaine is effective for localized anesthesia in various surgical and clinical procedures. -
NaV1.2/1.6 Channel Blocker
NaV1.2/1.6 channel blocker-1 is a selective inhibitor of the NaV1.2 and NaV1.6 sodium channels, exhibiting IC50 values of 9.8 μM for rNaV1.6 and 24.4 μM for hNaV1.2. This compound is valuable for studying the role of sodium channels in neuronal excitability and has potential applications in the research of generalized epilepsy. -
NaV1.7 Inhibitor
GX-201 is a selective inhibitor of the voltage-gated sodium channel NaV1.7, exhibiting an IC50 of less than 3.2 nM for the human NaV1.7 isoform. This compound has demonstrated effectiveness in modulating pain pathways and is valuable for research into pain management, neuropathic pain disorders, and related therapeutic applications. Its high potency and specificity make it a suitable tool for investigating sodium channel-related biological processes. -
Sodium Channel Agonist
Dimethyl lithospermate B is a selective sodium channel agonist that enhances sodium current (INa) by slowing its inactivation. This activity results in an increased inward current during the early phases of the action potential (AP). Dimethyl lithospermate B is utilized in research applications focusing on cardiac and neuronal excitability. -
Nav1.8 Channel Inhibitor
Nav1.8-IN-4 is a potent inhibitor of the Nav1.8 ion channel, demonstrating an IC50 of 0.014 μM. This compound is valuable for studies investigating pain-related disorders, offering insights into the modulation of nociceptive pathways. Its application in research may contribute to the development of novel therapeutic strategies targeting chronic pain mechanisms. -
Active Compound
Z-Gly-Gly-Phe-OH is a substrate for serine proteases such as pepsin and thermolysin, exhibiting an IC50 of 15.8 μM for open sodium channels under pepsin catalysis. This compound effectively participates in enzyme-catalyzed condensation reactions to form peptide bonds with amine components, including H-Leu-NHPh. Z-Gly-Gly-Phe-OH serves as a valuable intermediate in peptide synthesis, making it essential for various biochemical research applications. -
Sodium Channel Blocker
Tocainide is a sodium channel blocker that primarily targets voltage-gated sodium channels in neuronal membranes. It exhibits analgesic properties by inhibiting sodium influx, which contributes to pain signaling. Tocainide is utilized in research related to neuropathic pain and has potential applications in treating conditions such as tinnitus. -
Sodium Channel Inhibitor
XPC-6444 is a highly potent and isoform-selective sodium channel inhibitor, specifically targeting NaV1.6 with an IC50 of 41 nM. It also exhibits significant inhibition of NaV1.2 with an IC50 of 125 nM. This compound demonstrates anticonvulsant activity, making it a valuable tool for research in neuropharmacology and the study of epilepsy-related mechanisms. -
Sodium Channel Blocker
Taplucainium chloride is a sodium channel blocker that demonstrates 70-95% inhibition at a concentration of 10 μM. It exhibits significant analgesic properties, making it a valuable tool for pain research. This reagent can be utilized to investigate sodium channel function and its role in pain signaling pathways. -
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.
