Catalog No.
Product Name
Application
Product Information
Citations
-
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. -
Nav1.7 Inhibitor
Nav1.7-IN-19 is a selective inhibitor of the voltage-gated sodium channel Nav1.7, demonstrating a potent inhibitory activity with an IC50 of 0.49 μM. This compound exhibits significant selectivity for Nav1.7, with 312-fold and 662-fold selectivity over Nav1.1 and Nav1.5 in their inactivated states, respectively. Additionally, Nav1.7-IN-19 shows minimal inhibition of hERG potassium channels. Due to its analgesic properties, Nav1.7-IN-19 is valuable for research focused on neurological diseases. -
Antiarrhythmic Agent
Flecainide is an orally active antiarrhythmic agent that primarily targets sodium channels to modulate cardiac excitability. By inhibiting calcium ion release mediated by the ryanodine receptor (RyR2), it plays a critical role in the study of arrhythmias. Research applications include the investigation of diseases such as catecholaminergic polymorphic ventricular tachycardia (CPVT), where it may help elucidate underlying mechanisms and therapeutic strategies. -
Antiarrhythmic Agent
Flecainide hydrochloride is a potent antiarrhythmic agent that primarily targets sodium channels in cardiac tissues. By inhibiting the release of calcium ions mediated by the cardiac ryanodine receptor (RyR2), it effectively stabilizes cardiac membrane excitability. This compound is utilized in research studies focusing on cardiac arrhythmias, including catecholaminergic polymorphic ventricular tachycardia (CPVT) and other related cardiovascular diseases. -
Sodium Channel Inhibitor
Ropivacaine hydrochloride monohydrate is a potent sodium channel inhibitor that reversibly blocks sodium ion influx, thereby disrupting impulse conduction in nerve fibers. Additionally, it inhibits the K2P potassium channel TREK-1 with an IC50 of 402.7 μM in COS-7 cell membranes. This compound is widely utilized for regional anesthesia and in the management of neuropathic pain in vivo, making it a valuable reagent in pain research and therapeutic applications. -
Stable Isotope
Ropivacaine-d7 is a deuterium-labeled derivative of Ropivacaine, a potent sodium channel blocker. It works by reversibly inhibiting sodium ion influx, thereby blocking impulse conduction in nerve fibers. Additionally, Ropivacaine acts as an inhibitor of the K2P (two-pore domain potassium channel) TREK-1, exhibiting an IC50 of 402.7 μM in COS-7 cell membranes. This reagent is primarily used in studies focused on the management of neuropathic pain. -
KV7 Activator/NaV Inhibitor
E0199 is a potent dual-target KV7 activator and NaV inhibitor, specifically enhancing KV7.2/7.3 (EC50 = 12.78 nM), KV7.2 (EC50 = 0.50 μM), and KV7.5 (EC50 = 27.14 nM) channels while inhibiting NaV1.7 (IC50 = 0.52 μM), NaV1.8 (IC50 = 0.24 μM), and NaV1.9 (IC50 = 0.16 μM) channels. This compound demonstrates significant analgesic properties in a chronic constriction injury mouse model, effectively managing neuropathic pain without adversely impacting cardiac and skeletal muscle ion channels. E0199 serves as a valuable tool for research in neuropathic pain mechanisms and therapeutic strategies. -
Stable Isotope
(Rac)-Ropivacaine-d7 is a deuterium-labeled analogue of (Rac)-Ropivacaine, a local anesthetic that primarily acts by blocking voltage-gated sodium channels. This stable isotope is valuable in pharmacokinetic studies and metabolic research, enabling researchers to investigate the drug's distribution, metabolism, and elimination in biological systems. The incorporation of deuterium enhances the sensitivity and specificity of analytical methods such as mass spectrometry. -
Nav1.8 Modulator
Nav1.8 modulator 1 is a selective modulator targeting the Nav1.8 sodium channel, which plays a crucial role in the transmission of pain signals. This compound exhibits potent modulation properties, making it a valuable tool for pain research. Its ability to influence neuronal excitability can aid in the exploration of pain pathways and the development of novel analgesic therapies. -
Antiarrhythmic Agent
(-)-(S)-Cibenzoline is an antiarrhythmic agent that primarily targets sodium channels. This S(+)-enantiomer of Cibenzoline demonstrates significant efficacy in the modulation of cardiac rhythm. It is commonly utilized in research focused on the treatment of arrhythmias and the investigation of cardiac electrophysiology. -
Stable Isotope
Ropivacaine-d7 hydrochloride is a deuterium-labeled derivative of Ropivacaine, primarily functioning as a potent sodium channel blocker. It inhibits sodium ion influx in nerve fibers, leading to reversible blockade of impulse conduction. Additionally, Ropivacaine acts as an inhibitor of the TREK-1 potassium channel, demonstrating an IC50 of 402.7 μM in COS-7 cell membranes. This reagent is valuable for research in neuropathic pain management and the study of ion channel dynamics. -
Antiarrhythmic Agent
Disopyramide hydrochloride is a class IA antiarrhythmic agent primarily targeting cardiac sodium channels. It effectively treats both ventricular and atrial arrhythmias by blocking fast inward sodium currents and prolonging the duration of cardiac action potentials. Additionally, disopyramide inhibits HERG-encoded potassium channels and demonstrates significant negative inotropic effects. This compound is valuable for research investigating cardiac electrophysiology and the mechanisms underlying arrhythmogenic conditions. -
Nav1.8 Inhibitor
Nav1.8-IN-7 is a selective inhibitor of the Nav1.8 ion channel, demonstrating over 50% inhibition at a concentration of 100 nM. This compound selectively targets Nav1.8 while exhibiting an IC50 for hERG of 15.6 μM. Nav1.8-IN-7 is particularly relevant for research in pain mechanisms and the development of analgesic therapies. -
Ion Channel Inhibitor
Nerispirdine is an ion channel inhibitor that selectively targets voltage-gated potassium channels K(v)1.1 and K(v)1.2, exhibiting IC50 values of 3.6 µM and 3.7 µM, respectively, and also inhibits voltage-dependent sodium channels with an IC50 of 11.9 µM. As a derivative of 4-aminopyridine, Nerispirdine serves as a valuable tool in the investigation of neurological disorders, contributing to research focused on channelopathies and synaptic transmission. Its potential for modulating ion channel activity makes it a significant compound for studying electrophysiological processes. -
Stable Isotope
Flecainide-d3 is a deuterium-labeled form of Flecainide, a clinically utilized antiarrhythmic agent. Its primary mechanism involves blocking sodium channels while also inhibiting calcium ion release through the cardiac ryanodine receptor (RyR2). This reagent is valuable in research focused on cardiac arrhythmias, particularly in the study of catecholaminergic polymorphic ventricular tachycardia (CPVT) and related cardiac conditions. Its stable isotope labeling facilitates advanced pharmacokinetic and metabolic studies. -
Sodium Channel Blocker, NaV1.8 Inhibitor
Suzetrigine is a selective inhibitor of the sodium channel NaV1.8, functioning as a sodium channel blocker. This compound exhibits significant analgesic properties, making it a valuable tool for pain research. It is particularly promising for studying acute pain management following surgical procedures such as abdominoplasty and bunionectomy. -
SCN8A Blocker
Zandatrigine is a selective inhibitor of the voltage-gated sodium channel NaV1.6 (SCN8A), exhibiting potent activity at the blood-brain barrier. By non-covalently binding to the VSD4 region of NaV1.6, Zandatrigine effectively blocks sodium influx, thereby mitigating persistent currents associated with pathological conditions. This compound has demonstrated a significant ability to reduce neuronal hyperexcitability and decrease the frequency of epileptic seizures. With 134-756-fold selectivity over other sodium channel isoforms such as NaV1.1 and NaV1.2, Zandatrigine serves as a valuable tool in research focused on SCN8A-related developmental epileptic encephalopathy (SCN8A-DEE) and adult focal epilepsy. -
Nav1.7 Inhibitor
PF-04856264 is a selective inhibitor of the Nav1.7 sodium channel, exhibiting IC50 values of 28 nM for human, 131 nM for mouse, 19 nM for cynomolgus monkey, and 42 nM for dog Nav1.7. It displays limited activity against rat Nav1.7, highlighting its specificity. PF-04856264 is primarily utilized in research focused on pain pathways and has demonstrated notable analgesic effects, making it a valuable tool for investigating pain-related mechanisms and potential therapeutic applications. -
Sodium Channel Blocker
QX-314 bromide is a membrane-impermeable sodium channel blocker that exerts its effects by binding to the intracellular side of sodium channels, effectively inhibiting neuronal activation. Its permanent positive charge prevents diffusion across cellular membranes, making it useful for investigating the role of sodium channels in physiological and pathological states. QX-314 bromide is commonly utilized in pain research, neurobiology, and studies of excitability in various cell types. -
NaV1.7 Blocker
PF-06456384 trihydrochloride is a highly potent and selective blocker of the NaV1.7 sodium channel, exhibiting an IC50 value of 0.01 nM for human NaV1.7, 75 nM for rat NaV1.7, and less than 0.1 nM for mouse NaV1.7. This compound is instrumental in researching pain pathways and the physiological role of NaV1.7 in nociception. Notably, PF-06456384 trihydrochloride has shown minimal analgesic efficacy in animal models such as the mouse Formalin pain model, highlighting its specificity in sodium channel modulation. -
Sodium Channel Inhibitor
Dibucaine hydrochloride is a sodium channel inhibitor that effectively blocks the influx of sodium ions, thereby preventing the propagation of action potentials in excitable tissues. This compound exhibits potent activity as an anesthetic and is utilized in various research applications, including studies of nerve conduction and muscle excitability. Additionally, it serves as a significant inhibitor of serum cholinesterase, contributing to its utility in pharmacological investigations and the development of anesthetic protocols. -
NaV1.8 Inhibitor
LTGO-33 is a potent and selective inhibitor of the voltage-gated sodium channel NaV1.8. With nanomolar potency and over 600-fold selectivity against human NaV1.1-NaV1.7 and NaV1.9 channels, LTGO-33 demonstrates state-independent inhibition across closed and inactivated conformations. It effectively reduces TTX-resistant NaV1.8 currents in non-human primate and human dorsal root ganglion neurons, leading to decreased action potential firing. LTGO-33 is a valuable tool for research into pain disorders and related mechanisms. -
Sodium Channel Modulator
Suzetrigine phenol is a sodium channel modulator that acts by selectively altering the gating of sodium channels. This compound exhibits significant biological activity related to the modulation of neuronal excitability and has potential applications in the study of pain pathways and neuroprotection. Research utilizing Suzetrigine phenol can aid in understanding sodium channel function and developing therapeutic strategies for neurological disorders. -
ENaC Activator
S3969 is a potent and reversible activator of the human epithelial sodium channel (hENaC). With an apparent EC50 of 1.2 μM, S3969 enhances sodium transport across epithelial tissues. This compound serves as a valuable tool for investigating cellular mechanisms related to sodium homeostasis and may be applied in studies of conditions such as hypertension and edema. -
Nav1.7 Inhibitor
TC-N 1752 is a selective inhibitor of the voltage-gated sodium channel Nav1.7, exhibiting potent activity with an IC50 of 0.17 μM. It also demonstrates inhibitory effects on other sodium channels, including hNav1.3, hNav1.4, hNav1.5, and rNav1.8. This compound has been shown to provide analgesic effects in the Formalin model of pain, making it a valuable tool for research in pain mechanisms and related therapies. -
Nav1.1 Activator
Nav1.1 activator 1 is a potent activator of the Nav1.1 sodium channel, effectively enhancing the decay time constant (tau) of Nav1.1 currents at a concentration of 0.03 μM. This compound demonstrates significant selectivity for Nav1.1 over other sodium channels, including Nav1.2, Nav1.5, and Nav1.6, facilitating targeted research. Its ability to penetrate the blood-brain barrier makes it a valuable tool for studying neurological function and related therapeutic applications. -
Sodium Current Inhibitor
Relutrigine is an orally active sodium current inhibitor that specifically targets persistent sodium channels. It demonstrates potent inhibition of persistent INa induced by both ATX-II (Nav 1.5 activator) and the SCN8A mutation N1768D, with IC50 values of 141 nM and 75 nM, respectively. In addition to exhibiting a strong use-dependent block, Relutrigine effectively reduces intrinsic neuronal excitability and possesses significant anticonvulsant properties, making it valuable for research in neuropharmacology and epilepsy studies. -
Sodium Channel Activator
Bifenthrin is a synthetic pyrethroid insecticide that acts as a sodium channel activator, specifically targeting Nav1.8 sodium channels. By prolonging the opening time of these channels, Bifenthrin induces membrane depolarization and disrupts neural function in insects. It exhibits potent insecticidal activity with reported lethal doses (LD50) of 0.15 ng/mg against Aedes gambiae and 0.16 ng/mg against Culex quinquefasciatus, making it an effective agent for control of both susceptible and resistant mosquito populations. Its efficacy in inhibiting blood-sucking behavior presents potential applications in developing mosquito-repellent materials.
