Catalog No.
Product Name
Application
Product Information
Citations
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Sodium Channel
Tolperisone is a centrally acting muscle relaxant that primarily targets sodium channels, leading to neuronal inhibition. It is effective in alleviating symptoms of spasticity and muscle spasms, making it a valuable tool in neuromuscular research and therapeutic studies. Tolperisone's mechanism of action extends its application in exploring muscle relaxation pathways and their implications in various neurological conditions. -
NaV1.7 Inhibitor
DS43260857 is a selective inhibitor of the sodium channel NaV1.7, exerting strong inhibitory effects on both human and mouse variants of the channel. It demonstrates IC50 values of 6.6 μM for hNaV1.1, 14 μM for hNaV1.5, 0.015 μM for hNaV1.7, and 0.061 μM for mNaV1.7. This compound is useful for investigating pain pathways and assessing the role of NaV1.7 in nociception-related research. -
Nav1.7 Inhibitor
PF 05089771 tosylate is a selective Nav1.7 inhibitor, known for its potent biological activity with IC50 values of 11 nM for human Nav1.7 and varying efficacy across other species. This arylsulfonamide compound is orally active, making it a valuable tool for investigating pain and diabetic neuropathy mechanisms in preclinical research. Its specificity for Nav1.7 highlights its potential application in developing novel analgesic therapies. -
Nav1.8 Inhibitor
Nav1.8-IN-18 is a selective inhibitor of the voltage-gated sodium channel Nav1.8. It exhibits significant activity in modulating neuronal excitability, making it a valuable tool for investigating pain pathways and sensory neuron function. This compound is suited for research applications focused on chronic pain models and neuropathic conditions. -
Sodium Channel Inhibitor
P552-02 mesylate is a sodium channel inhibitor that demonstrates significant potential for the treatment of cystic fibrosis. Its primary mechanism involves enhancing mucociliary clearance in the lungs, contributing to improved respiratory function. Additionally, P552-02 mesylate minimizes the risk of hyperkalaemia, making it a valuable compound for researchers studying respiratory diseases and therapeutic interventions. -
Nav1.7 Inhibitor
QLS-81 is a selective inhibitor of the Nav1.7 ion channel, demonstrating an inhibition constant (IC50) of 1.5 μM. This compound exhibits potent analgesic properties, effectively alleviating both neuropathic and inflammatory pain. By targeting the inactivated state of Nav1.7 channels, QLS-81 mediates frequency-dependent inhibition, making it a valuable tool for research focused on chronic pain mechanisms and potential therapeutic interventions. -
Sodium Channel Inhibitor
Nav1.8-IN-20 is a potent inhibitor of the voltage-gated sodium channel Nav1.8, demonstrating an IC50 value of 14 nM. By blocking the generation and conduction of action potentials in peripheral nociceptive neurons, it exerts significant analgesic effects. This compound is valuable for research into various pain models, including acute pain, chronic pain, inflammatory pain, and neuropathic pain. -
Sodium Channel Blocker
Nav1.7 blocker 1 is a selective sodium channel blocker that exhibits an IC50 value of 0.037 μM against the Nav1.7 target. This compound is primarily utilized in pain research, making it valuable for investigating various pain conditions, including neuropathic pain, postoperative pain, and inflammatory pain. Its potent activity allows for the exploration of mechanisms underlying pain signaling and the development of potential therapeutic strategies. -
Nav1.8 channel Inhibitor
Nav1.8-IN-11 is a potent inhibitor of the Nav1.8 sodium channel, exhibiting an IC50 value of 0.1 nM. This compound is valuable for investigating pain disorders, as it modulates neuronal excitability and may provide insight into the underlying mechanisms of pain signaling and management. Research applications include exploring therapeutic strategies for chronic pain conditions. -
Sodium Channel Inhibitor
L589420-0-2 is a sodium channel inhibitor that modulates intracellular sodium ion concentrations, ultimately influencing the electrophysiological properties of cells. This compound demonstrates specific inhibitory activity in human erythrocytes and can be instrumental in studies related to cardiovascular disease. Its ability to affect sodium ion dynamics makes it a valuable tool for research in cellular biology and pharmacology. -
Sodium Channel
Nifedipine hydrochloride is a calcium channel blocker that primarily targets voltage-gated sodium channels. This compound demonstrates significant vasodilatory effects, making it effective as an antianginal agent and for lowering blood pressure. Nifedipine hydrochloride is extensively utilized in biological research to investigate new antihypertensive and antianginal therapies, contributing to the development of novel cardiovascular treatments. -
Nav1.8 Inhibitor
Nav1.8-IN-13 is a selective inhibitor of the voltage-gated sodium channel Nav1.8, with a reported pIC50 of 7.9. This compound is utilized in research to investigate the role of Nav1.8 in pain signaling pathways and neuronal excitability. Its inhibitory properties make it a valuable tool for studying potential therapeutic approaches for pain management and related neurological disorders. -
NaV1.7 Antagonist
GpTx-1 is a peptide-derived antagonist of the NaV1.7 sodium channel, extracted from the venom of the Chilean spider Grammostola porteri. It exhibits potent inhibitory activity with an IC50 of 10 nM specifically for the NaV1.7 channel, demonstrating substantial selectivity for NaV1.4 (IC50 = 0.301 μM) and NaV1.5 (IC50 = 4.20 μM), highlighting greater than 20-fold and over 950-fold selectivity, respectively. GpTx-1 is valuable in research applications focused on pain modulation and neurological disorders linked to NaV1.7 channel activity. -
nNav1.5 blocker
VGSC blocker-1 is a selective blocker of the neonatal voltage-gated sodium channel subtype Nav1.5 (nNav1.5). This small molecule inhibits peak sodium currents by 34.9% at a concentration of 1 μM, and it demonstrates a significant reduction in cell invasion by 0.3% at the same concentration in the MDA-MB-231 human breast cancer cell line, all while maintaining cell viability. VGSC blocker-1 is valuable for research into mechanisms of cancer metastasis and ion channel function in cellular processes. -
Nav1.5 Channels Blocker
Jingzhaotoxin-III is a highly selective blocker of Nav1.5 sodium channels, exhibiting an IC50 of 348 nM with no significant impact on other sodium channel isoforms. This toxin selectively inhibits the activation of cardiac sodium channels, making it a valuable tool for research focused on cardiac physiology and pathophysiology. Its specificity for the cardiac VGSC subtype positions Jingzhaotoxin-III as an important ligand for studies related to cardiovascular health and disease. -
Sodium Channel Blocker
Aneratrigine hydrochloride is a potent blocker of the sodium channel protein type 9 subunit alpha. This compound exhibits significant efficacy in modulating sodium channel activity, making it a valuable tool for research on neuropathic pain conditions. Its ability to inhibit excitatory neuronal signaling positions Aneratrigine hydrochloride as a promising reagent for studying pain pathways and potential therapeutic interventions. -
Sodium Channel Blocker
Ceratotoxin-2 is a potent blocker of voltage-gated sodium channels, exhibiting IC50 values of 8 nM and 88 nM against Nav1.2/β1 and Nav1.3/β1, respectively. This compound is valuable for investigating sodium channel-related physiological processes and studying disorders associated with sodium channel dysfunction. Its high specificity makes it an essential tool for research in neurobiology and pharmacology, facilitating the development of targeted therapies. -
Nav1.8 channel Inhibitor
Nav1.8-IN-12 is a selective inhibitor of the Nav1.8 sodium channel, known to play a crucial role in transmitting pain signals. This compound is valuable for investigating various pain-related diseases and disorders, facilitating the development of therapeutic strategies targeting neuropathic pain and inflammatory conditions. -
Voltage-Gated Sodium Channel Blocker
Proparacaine is a local anesthetic that functions as a voltage-gated sodium channel blocker. By inhibiting these channels on neuronal cell membranes, Proparacaine effectively disrupts signal conduction and reduces nociceptive signal transmission. This reagent is specifically utilized in ocular research, particularly in studies involving cataracts, to facilitate ocular muscle relaxation and minimize eye movement during surgical procedures. -
Sodium Channel Blocker
ACC-9358 is an orally active sodium channel blocker that exerts antiarrhythmic activity. This compound is valuable for research on cardiovascular diseases, particularly in the study and treatment of arrhythmias. Its mechanism of action and effects on sodium channels make it a useful reagent for understanding cardiac electrophysiology and developing therapeutic strategies. -
Sodium Channel Inhibitor
Oe-9000 is a sodium channel inhibitor that demonstrates local anesthetic activity by effectively blocking voltage-gated Na+ currents in neurons. It targets both TTX-sensitive and TTX-resistant currents, showing enhanced performance compared to other local anesthetics. This compound is valuable for research applications in pain management and neuropharmacology. -
Sodium Channel Blocker
Silperisone hydrochloride is a sodium channel blocker that exhibits centrally acting muscle relaxant properties. This compound selectively inhibits sodium and calcium channels, leading to decreased muscle cell excitability and contraction, which facilitates muscle relaxation and peripheral vasodilation. Silperisone hydrochloride is employed in research on recurrent painful myoclonus post-spinal cord injury, abnormal hypertonia associated with cerebrovascular disease, symptoms of myotonia, pyramidal tonia syndrome, and myospasm related to multiple sclerosis and myelitis. -
Nav1.5 Inhibitor
Nav1.5-IN-1 is a selective inhibitor of the sodium channel Nav1.5, exhibiting an IC50 of 1.38 μM. With demonstrated selectivity over other Nav subtypes, it effectively reduces cardiac conduction in isolated rat hearts. This compound serves as a valuable tool for investigating the mechanisms underlying cardiac arrhythmias. -
Sodium Channel Inhibitor
E-0747 is a sodium channel inhibitor that specifically targets Na[+] channels in cardiomyocytes. By blocking these channels, E-0747 exhibits antiarrhythmic properties, making it valuable for research into cardiac function and arrhythmia management. This compound can be utilized in studies investigating the mechanisms of electrical conduction and the potential therapeutic effects on various cardiac disorders. -
Nav1.8 Inhibitor
Nav1.8-IN-21 is a selective inhibitor of the Nav1.8 sodium channel, known for its role in transmitting pain signals. This compound exhibits significant analgesic activity and is valuable for research applications focused on pain management and neurophysiology. Its targeted inhibition makes it a useful tool for understanding the mechanisms of nociception and developing novel pain therapeutics. -
Nav1.2 Inhibitor
Nav1.2-IN-1 is a selective inhibitor of the Nav1.2 sodium channel, characterized by its structure as a 3-(1,2,3,6-tetrahydropyridine)-4-azaindole derivative. It effectively reduces the peak amplitude of Nav1.2 currents with an IC50 value of 7.79 μM. This compound demonstrates significant antiepileptic properties, exhibiting a potent anticonvulsant effect while maintaining low neurotoxicity in subcutaneous pentetrazole-induced epilepsy models. It serves as a valuable tool for research in epilepsy and sodium channel modulation. -
Nav1.8 channel Inhibitor
Nav1.8-IN-8 is a selective inhibitor of the Nav1.8 ion channel, which is associated with various pain pathways and neuronal excitability. By inhibiting Nav1.8 channels, this compound may help to mitigate pain and other disorders mediated by sodium ion channel dysregulation. Nav1.8-IN-8 serves as a valuable tool for research into pain mechanisms and therapeutic strategies targeting sodium channel activity. -
Sodium Channel Blocker
Pilsicainide is a potent sodium channel blocker and a class Ic antiarrhythmic agent. It inhibits the influx of sodium ions through voltage-gated sodium channels, leading to a stabilizing effect on cardiac membranes. This compound is primarily utilized in research related to arrhythmia and cardiac electrophysiology, contributing to the understanding of sodium channel function and its implications in heart rhythm disorders. -
Sodium Channel Inhibitor
ProTx II is a highly selective inhibitor of Nav1.7 sodium channels, exhibiting an IC50 of 0.3 nM and demonstrating over 100-fold selectivity for Nav1.7 compared to other sodium channel subtypes. This compound inhibits sodium channel conductance and alters the activation threshold to more positive potentials, effectively blocking action potential propagation in nociceptive neurons. ProTx II is valuable for research applications involving pain signaling and neuromodulation. -
Sodium Channel Inhibitor
Detajmium is a sodium channel inhibitor known for its ability to block Na+ channels, thereby affecting ventricular conduction and refractoriness. At a concentration of 0.3 μM, Detajmium prolongs intraventricular conduction time similarly to propafenone, but exhibits a distinct temporal profile during rapid ventricular pacing. This unique characteristic makes Detajmium valuable for research applications focusing on cardiac electrophysiology and arrhythmia management. -
Sodium Channel Blocker
Evenamide hydrochloride is a potent voltage-gated sodium channel (VGSC) blocker with a Ki of 0.4 μM, primarily utilized in the research of schizophrenia. It demonstrates significant efficacy across various rodent models, addressing conditions such as psychosis, mania, depression, and aggressive behaviors. This compound serves as a valuable tool for elucidating the underlying mechanisms of neuropsychiatric disorders. -
Sodium Channel Inhibitor
GX-585 is a sulfonamide analog that selectively inhibits the Nav1.7 sodium channel. This compound exhibits significant analgesic activity, making it a promising candidate for studies focused on neuropathic pain and inflammation management. Its ability to modulate sodium channel activity provides valuable insights into pain pathways and related biological processes. -
Sodium Channel Inhibitor
Sodium Channel Inhibitor 4 is a selective sodium channel inhibitor that disrupts sodium ion influx in excitable cells. This compound exhibits significant activity in modulating neuronal excitability and is useful in the study of pain pathways and seizure disorders. It serves as a valuable tool for researchers investigating the physiological and pharmacological roles of sodium channels in various biological systems. -
Nav1.8 Inhibitor
Nav1.8-IN-22 is a selective inhibitor of the Nav1.8 sodium channel, exerting its effects through direct binding to the channel. This compound modulates sodium channel activity and is intended for research applications related to pain mechanisms. Its specificity for Nav1.8 makes it a valuable tool for investigating pain pathways and developing potential analgesic therapies. -
Nav1.7 Inhibitor
ProTx-III is a potent and selective inhibitor of the voltage-gated sodium channel Nav1.7, exhibiting an IC50 of 2.1 nM. Derived from the venom of the Peruvian green velvet tarantula, this spider venom peptide features a characteristic inhibitor cystine knot (ICK) motif. ProTx-III plays a critical role in reversing pain responses and is instrumental in researching conditions such as chronic pain, epilepsy, and cardiac arrhythmias. -
NaV1.7 Blockage
Nav1.7-IN-8 is a selective inhibitor of NaV1.7, demonstrating a high degree of specificity for this subtype compared to hNaV1.1 and hNaV1.5. It effectively inhibits CYP2C9 and CYP3A4 enzymes with IC50 values of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 exhibits significant analgesic properties, making it a valuable tool for research in pain management and studies related to acute and inflammatory pain pathways. -
Sodium Channel
PF-05150122 is a potent and selective inhibitor of the human Nav1.7 sodium channel, which plays a critical role in pain signaling pathways. This compound effectively modulates pain responses, making it a valuable tool for research into mechanisms of acute and chronic pain. Favorable biopharmacokinetic properties have been observed in microdose studies, supporting its potential for further exploration in pain management applications. The predicted pharmacokinetic profile suggests significant efficacy in reducing the inhibitory concentration (IC50) of Nav1.7, highlighting its promise for therapeutic development. -
Sodium Channel Blocker
AZD-3161 is a potent and selective inhibitor of the NaV1.7 sodium channel, demonstrating an impressive pIC50 of 7.1. This compound exhibits significant analgesic properties and is primarily utilized in research focusing on neuropathic and inflammatory pain mechanisms. Its specificity for NaV1.7 makes it a valuable tool for investigating pain pathways and developing targeted therapeutics in pain management. -
Sodium Channel Blocker
Huwentoxin-IV is a selective sodium channel blocker that primarily targets and inhibits neuronal isoforms Nav1.7, Nav1.2, Nav1.3, and Nav1.4, with IC50 values of 26, 150, 338, and 400 nM, respectively. This compound preferentially binds to neurotoxin receptor site 4 on the peripheral nerve subtype Nav1.7, making it an effective candidate for pain management. Huwentoxin-IV exhibits significant analgesic effects in animal models of both inflammatory and neuropathic pain, highlighting its potential utility in pain research and therapeutic applications. -
Sodium Channel Blockers
PD-85639 is a voltage-gated sodium (Na+) channel blocker that exhibits neuroprotective properties. This compound is valuable in research focused on neurodegenerative diseases and neuronal injury, where modulation of sodium channel activity can influence cellular excitability and promote cell survival. Its potential applications extend to studies investigating the mechanisms underlying neuropathic pain and the pathophysiology of stroke. -
Nav1.8 Inhibitor
Nav1.8-IN-14 is a selective inhibitor of the voltage-gated sodium channel Nav1.8, known for its role in the transmission of pain signals. This compound demonstrates potent activity in modulating Nav1.8 function and has significant implications for the study of pain-related diseases, including neuropathic pain and inflammatory conditions. Research applications include investigations into the mechanistic pathways of pain sensation and the development of novel analgesic therapies. -
Nav1.7 Inhibitor
Nav1.7-IN-13 is a selective inhibitor of the Nav1.7 sodium channel, known for its capacity to significantly reduce Veratridine-induced neuronal activity. This compound effectively inhibits total sodium currents in dorsal root ganglion (DRG) neurons in a concentration-dependent manner and slows the activation of sodium channels. In vivo, Nav1.7-IN-13 demonstrates analgesic properties by markedly alleviating mechanical pain behavior in a rat model of nerve injury (Spared Nerve Injury, SNI), making it a valuable tool for pain research. -
Nav1.5 Channel Inhibitor
GS-462808 is a potent inhibitor of the cardiac Nav1.5 channel, specifically targeting the late sodium current (Late INai) with an IC50 of 1.33 μM. This compound is valuable for investigating the mechanisms underlying arrhythmias, providing insight into potential therapeutic approaches for cardiac disorders. Researchers may utilize GS-462808 to explore the role of Nav1.5 channel inhibition in various cardiac pathologies. -
Nav1.7 Inhibitor
GX-936 is a selective inhibitor of the voltage-gated sodium channel Nav1.7, targeting its activated state in the voltage-sensor domain IV (VSD4). This compound demonstrates potent inhibition of Nav1.7-mediated currents, making it valuable for research into pain pathways and excitability of sensory neurons. Applications include the study of inflammatory and neuropathic pain conditions, as well as the development of novel analgesic therapies. -
Sodium Channel
AFD-21 maleate is a selective sodium channel inhibitor exhibiting antiarrhythmic properties. It binds preferentially to sodium channels in their inactive state, demonstrating both use-dependent and voltage-dependent blocking effects. At specific concentrations, AFD-21 maleate can prolong action potential duration and significantly decrease the maximum rise rate of the action potential. This compound is of particular interest in cardiovascular research for its potential applications in arrhythmia management. -
Antiarrhythmic Agent
Indecainide is an orally active antiarrhythmic agent that primarily targets sodium channels. It demonstrates significant sodium channel-blocking activity, making it valuable for the investigation of ventricular dysfunction and other cardiac arrhythmias. This compound is utilized in research to better understand and develop therapeutic strategies for managing arrhythmic conditions. -
Analgesic Agent
Nefopam is a non-opioid, centrally acting analgesic agent primarily targeting voltage-sensitive sodium channels. Exhibiting an IC50 value of 27 μM, Nefopam modulates glutamatergic transmission and demonstrates significant analgesic properties. This compound is useful for research involving neuropathic pain, anticonvulsant effects, and the mitigation of postoperative shivering and hiccups. -
Nav1.8 Inhibitor
Nav1.8-IN-19 is a selective inhibitor of the voltage-gated sodium channel Nav1.8, exhibiting an IC50 of 0.44 nM in HEK293 cells. This compound is instrumental for research focused on nociception and pain pathways, making it a valuable tool for investigating pain modulation and related therapeutic strategies. -
Paralytic Shellfish Poisoning Toxin
Gonyautoxin II is a potent paralytic shellfish poisoning toxin that selectively targets voltage-gated sodium channels, thereby disrupting axonal nerve impulse propagation. This compound exhibits cytotoxic activity against mouse neuroblastoma cells, making it a valuable tool in cancer research. Additionally, Gonyautoxin II is relevant in studies focused on neurological diseases, aiding in the understanding of neurotoxicity mechanisms and potential therapeutic strategies. -
Pesticide
Cyphenothrin is a pyrethroid pesticide that targets the neuromuscular system of insects. It disrupts the gating mechanism of sodium channels, leading to paralysis and eventual mortality in target pests. This compound is commonly utilized in agricultural and pest control research to study its effectiveness against a variety of insect species.
