Catalog No.
Product Name
Application
Product Information
Citations
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Antiepileptic Compound
Losigamone is an orally active antiepileptic compound that primarily targets sodium channels. It enhances GABA-mediated responses by stimulating neuronal chloride channels, thus increasing chloride influx. This mechanism effectively reduces epileptiform activity induced by chloride channel antagonists, making Losigamone a valuable tool for research in epilepsy and related neuronal disorders. -
Insecticide
Leporin A is an insecticide that primarily targets GABA receptors and sodium channels, disrupting neurotransmission in insects. This mechanism leads to paralysis and mortality, making Leporin A a potent agent for agricultural pest control. It is utilized in research focused on insect physiology and pest management strategies. -
Insecticide
Insecticidal agent 21 is a potent insecticide primarily targeting Culex pipiens larvae with an LC50 of 0.4 μg/mL. This compound exerts multi-target neurotoxicity by inhibiting acetylcholinesterase (AChE) and affecting multiple neural receptors, including nicotinic acetylcholine receptors (nAChR), voltage-gated sodium channels (VGSC), and γ-aminobutyric acid receptors (GABAAR). Insecticidal agent 21 demonstrates a strong insecticidal effect and is suitable for research applications focused on developing novel insecticides to combat resistance in mosquito populations. -
NMDA Receptor Inhibitor
Bupivacaine is an NMDA receptor inhibitor that modulates neuronal excitability by blocking sodium, L-calcium, and potassium channels. It exhibits potent inhibition of SCN5A channels, with an IC50 of 69.5 μM. This compound is primarily utilized in research focused on chronic pain mechanisms and therapeutic interventions. -
NMDA Receptor Inhibitor
Bupivacaine-d9 is a deuterium-labeled analog of Bupivacaine, primarily targeting NMDA receptors. This compound exhibits inhibitory effects on sodium, L-calcium, and potassium channels, with a notable potency against SCN5A channels, characterized by an IC50 value of 69.5 μM. Bupivacaine-d9 is utilized in research related to chronic pain mechanisms and the modulation of excitatory neurotransmission, offering valuable insights into therapeutic applications in pain management. -
Anti-Anrhythmic Agent
Aprindine hydrochloride is an Ib-class anti-arrhythmic agent primarily targeting sodium channels (INa) to reduce the excitability and conduction velocity of cardiac muscle cells. By significantly inhibiting delayed potassium currents, it prolongs the atrial effective refractory period (AERP) and mitigates the risk of atrial fibrillation. Additionally, Aprindine hydrochloride modulates intracellular calcium ion concentration through the inhibition of Na+/Ca2+ exchange current (INCX), further enhancing the stability of cardiac electrical activity. This compound is suitable for research focused on atrial fibrillation (AF) and ventricular arrhythmias. -
Anti-arrhythmic Agent
Aprindine is an Ib-class antiarrhythmic agent that primarily targets sodium channels (INa) to reduce the excitability and conduction velocity of cardiac muscle cells. Its ability to significantly inhibit delayed potassium currents prolongs the atrial effective refractory period (AERP), thereby helping to prevent atrial fibrillation. Additionally, Aprindine modulates intracellular calcium levels by inhibiting the Na+/Ca2+ exchange current (INCX), further stabilizing cardiac electrical activity. This compound is useful for research into atrial fibrillation (AF) and ventricular arrhythmias. -
Nav Channel Blocker
ProTx-I is a potent blocker of voltage-gated Na+ channels, specifically inhibiting NaV1.2, NaV1.6, and NaV1.7 with IC50 values of 104 nM, 21 nM, and 95 nM, respectively. Additionally, ProTx-I exhibits significant activity as a CaV3.1 channel blocker, demonstrating IC50 values of 0.2 μM for hCaV3.1 and 31.8 μM for hCaV3.2. It also inhibits KV 2.1 channels (IC50: 411 nM) and TRPA1 (IC50: 389 nM). This multi-targeting profile makes ProTx-I valuable for research in neurobiology and pain signaling pathways. -
Stable Isotope
Ranolazine-d3 is a deuterated form of Ranolazine, an anti-anginal agent that primarily inhibits the late phase of inward sodium current (INa) with an IC50 value of 6 μM and IKr with an IC50 value of 12 μM, leading to its therapeutic effects without altering heart rate or blood pressure. Additionally, Ranolazine acts as a partial fatty acid oxidation (FAO) inhibitor. This compound serves as a valuable tool in cardiovascular research, particularly in studying sodium channel activity and metabolic modulation in heart physiology. -
Potassium/Sodium Channel Inhibitor
Huwentoxin I is a peptide toxin that specifically inhibits voltage-gated sodium channels and N-type calcium channels. This compound has demonstrated significant inhibitory effects on sodium channels in both rat hippocampus and cockroach dorsal unpaired median (DUM) neurons, with IC50 values of 66.1 nM and 4.80 nM, respectively. Huwentoxin I is valuable for studies focused on neuronal excitability and channelopathy-related research applications. -
Calcium/Sodium Channel Blocker
Elpetrigine is a potent calcium and sodium channel blocker with significant anticonvulsant, antidepressant, antimania, and anxiolytic properties. This compound is primarily utilized in research focused on epilepsy and bipolar disorder, contributing to the understanding of neurological and mood disorders. Its mechanism of action makes it a valuable tool for exploring therapeutic avenues in these conditions. -
N-type Calcium Channel Antagonist
Huwentoxin XVI is a selective antagonist of N-type calcium channels, demonstrating a potent inhibitory effect with an IC50 of approximately 60 nM. Derived from the Chinese tarantula Ornithoctonus huwena, it serves as an analgesic and exhibits no activity against voltage-gated T-type calcium channels, potassium channels, or sodium channels. This specificity makes Huwentoxin XVI valuable in research aimed at understanding pain mechanisms and the role of calcium channels in various physiological processes. -
Broad-Spectrum Antiepileptic Agent
JNJ-26990990 is a broad-spectrum antiepileptic agent that primarily targets voltage-gated sodium channels and N-type calcium channels. It exhibits significant anticonvulsant activity, making it suitable for the study of various seizure models. Although it shows minimal inhibition of human carbonic anhydrase-II with an IC50 of 110 μM, its primary applications lie in the investigation of epilepsy and related neurological disorders. -
Sodium/Calcium Channel Blocker
KT 2-230 is a sodium and calcium channel blocker that exhibits significant anti-inflammatory properties. This compound is utilized in research applications focused on neuropathic pain and various inflammatory conditions. Its ability to modulate ion channel activity makes it a valuable tool for studying the underlying mechanisms of synaptic transmission and neuroprotection. -
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. -
T-type Ca2+ Channel Antagonist
U 92032 is a T-type Ca2+ channel antagonist that effectively inhibits sodium channels. This compound has been shown to disrupt thalamic oscillations, providing valuable insights into the mechanisms underlying neurological disorders. U 92032 is applicable in research focused on various neurological diseases, making it a significant tool for studying calcium signaling and excitability in the central nervous system. -
Calcium Channel/Sodium Channel Antagonist
EO-122 is a potent antagonist targeting calcium and sodium channels. It exhibits significant inhibitory activity, making it a valuable tool for studying mechanisms related to arrhythmias. This compound aids in the exploration of cardiac and neuronal excitability, facilitating research into related therapeutic strategies. -
Calcium/Sodium Channel Blocker
LY393615 free base is an effective blocker of neuronal calcium (Ca²⁺) and sodium (Na⁺) channels, exhibiting IC50 values of 1.9 μM and 5.2 μM for the α1A and α1B calcium channel subunits, respectively. This compound demonstrates substantial brain penetration and offers neuroprotective properties in cerebral ischemia models. It serves as a valuable tool in neurological disease research, providing insight into the pathophysiology of various neurodegenerative conditions. -
Multi-ion channel Blocker
Sulcardine hydrochloride is a multi-ion channel blocker primarily targeting sodium (INa) and calcium (ICa) channels, exhibiting IC50 values of 26.9 µM and 69.2 µM, respectively. This compound effectively inhibits the hNav1.5 channel and demonstrates a mild inhibitory effect on hERG channels. Due to its pharmacological properties, Sulcardine hydrochloride is often utilized in research related to anti-arrhythmic effects and cardiac electrophysiology. -
Stable Isotope
Ranolazine-d8 is a deuterated form of Ranolazine, which primarily targets the late phase of inward sodium current (INa) and potassium current (IKr) with IC50 values of 6 μM and 12 μM, respectively. This compound functions as an anti-anginal agent, alleviating symptoms without influencing heart rate or blood pressure. Additionally, Ranolazine acts as a partial fatty acid oxidation inhibitor, making it valuable for research related to cardiac ischemia and metabolic modulation in heart diseases. -
Calcium Channel Blocker
PD 122860 is a calcium channel blocker that also exhibits the ability to stimulate sodium channels. It is primarily utilized in research focused on cardiovascular and cerebrovascular diseases. By modulating calcium and sodium ion flux, PD 122860 contributes to understanding the underlying mechanisms of these conditions. -
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.
