Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Paralytic Shellfish Poisoning Toxin
Gonyautoxin III (GTX-III) is a potent paralytic shellfish poisoning toxin that acts by blocking voltage-gated sodium channels at the axonal level, displaying an IC50 of 14.9 nM. This inhibition disrupts the propagation of nerve impulses, leading to significant neurotoxicity. Gonyautoxin III demonstrates cytotoxic activity against mouse neuroblastoma cells, making it a valuable tool for research focused on cancer biology and neurological disorders. -
Sodium Channel Blocker
N-Depropylpropafenone is a sodium channel blocker and an active metabolite of Propafenone, produced primarily by the CYP450 enzyme system, particularly CYP2D6. It inhibits sodium ion channels, leading to a reduction in myocardial conduction velocity and displaying antiarrhythmic properties. This compound is valuable in the study of cardiac physiology and the mechanisms of arrhythmias. -
NaV1.7 Inhibitor
Sodium Channel-IN-8 is a potent inhibitor of the voltage-gated sodium channel NaV1.7. It has demonstrated significant activity in modulating pain pathways, making it a valuable tool for research into pain mechanisms and therapeutic interventions. This compound is suitable for studies focused on pain management and related neurological disorders. -
Stable Isotope
Licarbazepine-d8 is a deuterium-labeled derivative of Licarbazepine, a potent voltage-gated sodium channel blocker known for its anticonvulsant and mood-stabilizing properties. The stable isotope labeling enhances research applications in pharmacokinetic studies and metabolic investigations of Licarbazepine. This compound is valuable for elucidating the mechanisms of action and efficacy of sodium channel modulation in neurological disorders. -
Sodium Channel Inhibitor
Atelopidtoxin, a sodium channel inhibitor derived from the Panamanian frog Atelopus zeteki, exhibits potent biological activity with an LD50 of 0.016 mg/kg in mice. Its effects include inducing hypotension and ventricular fibrillation in rabbit models, making it a valuable reagent for research focused on cardiovascular physiology and sodium channel function. This compound serves as a significant tool for studies investigating the physiological and pharmacological roles of sodium channels. -
Stable Isotope
Propafenone-d5 Ethyl hydrochloride is a deuterium-labeled derivative of Propafenone hydrochloride, an anti-arrhythmic medication classified as a Class 1C agent. It primarily targets sodium channels to inhibit cardiac arrhythmias, making it effective in managing conditions such as atrial and ventricular arrhythmias. This stable isotope is valuable for pharmacokinetic studies and metabolic investigations in cardiovascular research applications. -
Stable Isotope
Methocarbamol-d3 is a deuterium-labeled analog of Methocarbamol, a centrally acting muscle relaxant that targets the Nav1.4 sodium channel. This stable isotope aids in studies related to muscle spasms and pain syndromes by providing insights into the voltage-dependent inactivation mechanisms of the Nav1.4 channel. Its unique labeling facilitates enhanced tracking and analysis in pharmacokinetic and metabolic studies. -
Stable Isotope
Atomoxetine-d7 is a stable isotope-labeled form of Atomoxetine, a selective norepinephrine reuptake inhibitor. With Ki values of 5, 77, and 1451 nM for norepinephrine, serotonin, and dopamine transporters, respectively, it is known to enhance catecholaminergic neurotransmission and elevate dopamine and norepinephrine levels in the prefrontal cortex. Additionally, Atomoxetine functions as a potent blocker of voltage-gated sodium channels. This reagent is applicable in research focused on attention-deficit hyperactivity disorder (ADHD) and related neural mechanisms. -
NaV1.7 Inhibitor
GNE-3565 is a potent NaV1.7 inhibitor belonging to the arylsulfonamide class, exhibiting subnanomolar potency for channel blockade with mixed subtype selectivity. This compound is primarily utilized in research focusing on pain mechanisms and is instrumental in studying pain pathways and the development of novel analgesics. -
Sodium Channel Inhibitor
CL-424032 is a selective sodium channel inhibitor that modulates neuronal excitability. It has demonstrated efficacy in reducing action potential firing in various neuronal models. This compound serves as a valuable tool in the study of neuropathic pain and various cardiovascular disorders, making it relevant for research in neurobiology and pharmacology. -
Sodium Channel Inhibitor
LG 83-6-05 is a selective inhibitor of sodium channels, exhibiting potent effects on sodium ion permeability. This compound is primarily utilized in research focused on cardiac rhythm disorders, as it can help elucidate the role of sodium channels in arrhythmogenesis and related pathophysiological conditions. Additionally, LG 83-6-05 may serve as a valuable tool in the development of therapeutic strategies targeting sodium channel dysfunction. -
Antiarrhythmic Agent
Pentisomide is an orally active antiarrhythmic agent that primarily targets sodium channels. It exhibits Vaughan-Williams class I antiarrhythmic activity, making it useful in the management of various arrhythmias. This compound is valuable for research applications exploring cardiac electrophysiology and the mechanisms of arrhythmia modulation. -
Sodium Channel Inhibitor
(R)-(+)-Bupivacaine hydrochloride is a selective inhibitor of voltage-gated sodium channels. By blocking these channels on nerve cell membranes, it effectively inhibits sodium ion influx, thereby preventing the generation and conduction of nerve impulses, which results in local anesthetic activity. This compound is particularly relevant in the study of acute pain mechanisms and pain management strategies in research settings. -
Sodium Channel Modulator
PF-05661014 is a selective sodium channel modulator that primarily targets the Nav1.3 and Nav1.7 currents. By stabilizing inactivated channels through its interaction with the D4 voltage-sensor domain (VSD), PF-05661014 serves as an important tool in the study of sodium channel modulation. This reagent is valuable for research applications focused on understanding the role of sodium channels in various physiological and pathological processes. -
Sodium Channel blocker
Ralitoline is a sodium channel blocker with an IC50 of 2 μM. It exhibits anticonvulsant activity, making it a valuable tool for research in epilepsy and related neurological disorders. Ralitoline's ability to modulate sodium channel activity supports its potential in pharmacological studies aimed at understanding seizure mechanisms and developing therapeutic interventions. -
Deuterated Licarbazepine
Licarbazepine-d3 is the deuterated form of Licarbazepine, a potent blocker of voltage-gated sodium channels. This compound exhibits significant anticonvulsant properties and mood-stabilizing effects, making it valuable in neurological research and the study of mood disorders. Licarbazepine-d3 is utilized in various applications, including metabolic studies and pharmacokinetic investigations, leveraging its isotopic labeling for enhanced analytical sensitivity. -
Sodium Channel Inhibitor
Propafenone-d7 hydrochloride is a deuterated derivative of Propafenone, primarily acting as a sodium channel inhibitor. It exhibits significant anti-arrhythmic activity, making it valuable in the study of cardiac arrhythmias. This compound can be utilized in pharmacokinetic studies and metabolic tracing in research applications related to cardiac electrical activity and drug metabolism. -
Sodium Channel Blocker
NaV1.7 blocker-801 is a selective blocker of voltage-gated sodium channel NaV1.7, crucial for neuronal excitability and pain signaling. This compound is primarily used in the investigation of pain pathways and neurological disorders, offering insights into potential therapeutic strategies for conditions such as neuropathic pain and other related diseases. Researchers can utilize NaV1.7 blocker-801 to explore its effects on neuronal activity and pain modulation in various experimental settings. -
Sodium Channel Control
Lamotrigine N2-Oxide is a metabolite of the anticonvulsant agent Lamotrigine, targeting sodium channels to modulate neuronal excitability. This compound is primarily utilized in the study of epilepsy and related neurological disorders, providing insights into the pharmacological profiles of sodium channel modulators. Its role in research facilitates a better understanding of mechanisms underlying anticonvulsant activity and the potential development of novel therapeutic strategies. -
Stable Isotope
Mexiletine-d6 is a deuterated form of Mexiletine, an orally bioavailable antiarrhythmic compound known for its ability to alleviate myotonia and neuropathic pain. This reagent functions primarily by blocking sodium channels, demonstrating an IC50 of 75±8 μM for tonic block and 23.6±2.8 μM for use-dependent block. Its unique isotopic labeling makes Mexiletine-d6 suitable for applications in cardiovascular and neurological research, allowing for enhanced tracing and understanding of molecular interactions in biological systems. -
Pyrethroid Insecticide
Zeta-Cypermethrin is a type II pyrethroid insecticide that primarily targets voltage-gated sodium channels in neuronal cells. Its mechanism leads to delayed channel closure, resulting in sustained nerve excitation and convulsions. Notably, Zeta-Cypermethrin promotes high metabolic resistance in Drosophila, which can be assessed through screening, and demonstrates in vitro genotoxicity in human peripheral blood lymphocytes, making it relevant for studies in neurotoxicity and resistance mechanisms. -
Sodium Channel Antagonist
(5R)-BW-4030W92 is a sodium channel antagonist that targets voltage-gated sodium channels in a non-selective and use-dependent manner. This compound exhibits significant biological activity by inhibiting sodium channel-mediated excitability, making it of interest in research on pain management, epilepsy, and neuroprotection. Its pharmacological properties provide a valuable tool for investigating the role of sodium channels in various physiological and pathological processes. -
TRPM8 Channel Blocker
AMTB hydrochloride is a selective antagonist of the TRPM8 channel, effectively inhibiting icilin-induced TRPM8 activation with a pIC50 of 6.23. This reagent is valuable in the study of overactive bladder conditions and painful bladder syndrome. Additionally, AMTB hydrochloride exhibits non-selective inhibition of voltage-gated sodium channels, providing a broader context for its use in electrophysiological research. -
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.
