Catalog No.
Product Name
Application
Product Information
Citations
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NaV1.2/1.6 Channel Blocker
NaV1.2/1.6 channel blocker-1 is a selective inhibitor of the NaV1.2 and NaV1.6 sodium channels, exhibiting IC50 values of 9.8 μM for rNaV1.6 and 24.4 μM for hNaV1.2. This compound is valuable for studying the role of sodium channels in neuronal excitability and has potential applications in the research of generalized epilepsy. -
NaV1.7 Inhibitor
GX-201 is a selective inhibitor of the voltage-gated sodium channel NaV1.7, exhibiting an IC50 of less than 3.2 nM for the human NaV1.7 isoform. This compound has demonstrated effectiveness in modulating pain pathways and is valuable for research into pain management, neuropathic pain disorders, and related therapeutic applications. Its high potency and specificity make it a suitable tool for investigating sodium channel-related biological processes. -
Sodium Channel Agonist
Dimethyl lithospermate B is a selective sodium channel agonist that enhances sodium current (INa) by slowing its inactivation. This activity results in an increased inward current during the early phases of the action potential (AP). Dimethyl lithospermate B is utilized in research applications focusing on cardiac and neuronal excitability. -
Nav1.8 Channel Inhibitor
Nav1.8-IN-4 is a potent inhibitor of the Nav1.8 ion channel, demonstrating an IC50 of 0.014 μM. This compound is valuable for studies investigating pain-related disorders, offering insights into the modulation of nociceptive pathways. Its application in research may contribute to the development of novel therapeutic strategies targeting chronic pain mechanisms. -
Active Compound
Z-Gly-Gly-Phe-OH is a substrate for serine proteases such as pepsin and thermolysin, exhibiting an IC50 of 15.8 μM for open sodium channels under pepsin catalysis. This compound effectively participates in enzyme-catalyzed condensation reactions to form peptide bonds with amine components, including H-Leu-NHPh. Z-Gly-Gly-Phe-OH serves as a valuable intermediate in peptide synthesis, making it essential for various biochemical research applications. -
Sodium Channel Blocker
Tocainide is a sodium channel blocker that primarily targets voltage-gated sodium channels in neuronal membranes. It exhibits analgesic properties by inhibiting sodium influx, which contributes to pain signaling. Tocainide is utilized in research related to neuropathic pain and has potential applications in treating conditions such as tinnitus. -
Antiarrhythmic Agent
Encainide is an antiarrhythmic agent classified as a class IC antiarrhythmic. It functions by blocking voltage-dependent potassium channels, thus modulating cardiac excitability. This compound shows promise in research focused on life-threatening ventricular arrhythmias, symptomatic ventricular arrhythmias, and supraventricular arrhythmias. Its role in these conditions makes it valuable for studies aimed at understanding and treating various cardiac arrhythmias. -
Sodium Channel Inhibitor
XPC-6444 is a highly potent and isoform-selective sodium channel inhibitor, specifically targeting NaV1.6 with an IC50 of 41 nM. It also exhibits significant inhibition of NaV1.2 with an IC50 of 125 nM. This compound demonstrates anticonvulsant activity, making it a valuable tool for research in neuropharmacology and the study of epilepsy-related mechanisms. -
Sodium Channel Blocker
Taplucainium chloride is a sodium channel blocker that demonstrates 70-95% inhibition at a concentration of 10 μM. It exhibits significant analgesic properties, making it a valuable tool for pain research. This reagent can be utilized to investigate sodium channel function and its role in pain signaling pathways. -
Nav1.7 Inhibitor
PF-05186462 is a selective inhibitor of the human Nav1.7 voltage-dependent sodium channel, exhibiting an IC50 value of 21 nM. This compound demonstrates a high degree of selectivity for Nav1.7 over other sodium channels, including Nav 1.1, 1.2, 1.3, 1.4, 1.5, 1.6, and 1.8. PF-05186462 is ideally suited for research applications focused on acute and chronic pain mechanisms. -
Antitussive Agent
Benzonatate is a non-narcotic peripheral antitussive agent that acts primarily by inhibiting reversible voltage-gated sodium channels. This compound effectively reduces the activity of cough stretch receptors, leading to a suppression of the cough reflex. Benzonatate is commonly utilized in research focusing on respiratory pathways and the modulation of cough response. -
Nav1.1 Inhibitor
AA43279 is a selective inhibitor of the Nav1.1 sodium channel (SCN1A), with an EC50 of 9.5 μM. This compound modulates the activity of gamma-aminobutyric acid (GABA) fast-firing interneurons, enhancing neuronal firing in vitro. AA43279 demonstrates anticonvulsant properties in the rat MEST model, making it a valuable tool for research involving epilepsy and related neurological disorders. -
Sodium Channel Modulator
ATX-II is a selective sodium channel modulator toxin that enhances late sodium current by preventing complete sodium channel inactivation, leading to persistent current fractions. This compound exhibits pro-arrhythmic effects, characterized by a slowed intrinsic heart rate, prolonged QT interval, and extended sinus node recovery time, potentially resulting in sinus pauses and arrests. ATX-II is valuable for research related to atrial fibrillation, long QT syndrome, and long QT3 syndrome. -
Aconitum Alkaloid
6-Benzoylheteratisine acts as an antagonist of tetrodotoxin and targets sodium channels, demonstrating potential neuroprotective activity. It effectively inhibits the influx of sodium ([Na+]i) and calcium ([Ca2+]i) ions, as well as the release of glutamate, making it relevant for the study of excitatory neurotransmission. Additionally, 6-Benzoylheteratisine has shown inhibitory effects on neuronal activity associated with epileptiform burst discharge, suggesting its utility in neurological research and potential therapeutic applications in epilepsy. -
Nav1.7 Antagonist
GX-674 is a potent antagonist of the voltage-gated sodium channel Nav1.7, exhibiting state-dependent and isoform-selective inhibition with an IC50 of 0.1 nM at -40 mV. This compound is valuable for research focused on pain pathways and neuropathic pain mechanisms, providing insights into the role of Nav1.7 in nociception and related disorders. Its high specificity and potency make it an essential tool for studying the therapeutic potential in pain management. -
Noradrenaline Reuptake Inhibitor
Atomoxetine is a selective noradrenaline reuptake inhibitor primarily targeting norepinephrine transporters with Ki values of 5 nM. It is known to increase dopamine and norepinephrine extracellular levels in the prefrontal cortex, thereby enhancing catecholaminergic neurotransmission. Additionally, Atomoxetine acts as a sodium channel blocker (VGSCs). This compound is widely utilized in research focusing on attention-deficit hyperactivity disorder (ADHD) and related neuropharmacological studies. -
Nav1.7/ Nav1.8 Blocker
ABBV-318 is a potent blocker of the voltage-gated sodium channels Nav1.7 and Nav1.8, demonstrating IC50 values of 2.8 μM and 3.8 μM for hNav1.7 and hNav1.8, respectively. This compound is of significant interest in pain research, providing insights into mechanisms of pain signaling and potential therapeutic avenues for pain management. Its specificity for Nav1.7 and Nav1.8 makes it a valuable tool for elucidating neuronal function and designing targeted analgesic strategies. -
Sodium Channel Blocker
Bliretrigine is a potent sodium channel blocker, primarily targeting voltage-gated sodium channels to modulate neuronal excitability. It has demonstrated significant analgesic properties, making it effective in alleviating pain associated with various neurological conditions. This compound is valuable for research into pain mechanisms and the development of novel analgesic therapies. -
Antiarrhythmic Agent
Ethacizine hydrochloride is a Class Ic antiarrhythmic agent that primarily targets sodium channels to modulate cardiac conduction. This compound is recognized for its long-lasting effects compared to other agents in its class, making it valuable for the management of arrhythmias. Ethacizine hydrochloride is utilized in research applications focused on cardiac electrophysiology and the mechanism of arrhythmias, providing insights into therapeutic interventions for cardiac disorders. -
Nav1.8 Inhibitor
Nav1.8-IN-2 is a selective inhibitor of the voltage-gated sodium channel Nav1.8, exhibiting a potent IC50 value of 0.4 nM. This compound is utilized in research related to various pain disorders, cough disorders, and both acute and chronic itch conditions. Its high affinity for Nav1.8 makes it a valuable tool for elucidating pain signaling pathways and developing therapeutic strategies for sensory nerve modulation. -
Sodium Channel Blocker
Co 102862 is a potent, broad-spectrum sodium channel blocker with state-dependent activity. This compound exhibits significant anticonvulsant properties, making it valuable for research in epilepsy and other neurological disorders. Its oral bioactivity supports its use in in vivo studies aimed at exploring sodium channel modulation in various therapeutic contexts. -
Anesthetic Agent
Etidocaine hydrochloride is a long-acting aminoamide local anesthetic that primarily targets sodium channels to inhibit neuronal excitability. It is effective in suppressing or relieving pain during surgical procedures and other medical applications requiring localized anesthesia. Its prolonged duration of action makes it suitable for various clinical settings. -
Sodium Channel Blocker
Aneratrigine is a selective blocker of the sodium channel protein type 9 subunit alpha, primarily inhibiting its activity. This compound exhibits significant potential in the study of neuropathic pain disorders, making it a valuable tool for research into pain management and associated neurological conditions. Researchers can utilize Aneratrigine to explore mechanisms of sodium channel modulation and its effects on neuronal excitability. -
ENaC Inhibitor
ETD001 is a potent ENaC (epithelial sodium channel) inhibitor, demonstrating an IC50 of 57.5 nM in cultured human bronchial epithelial (HBE) cells. This compound is particularly valuable for research applications related to cystic fibrosis, as it modulates sodium transport and influences fluid secretion in airway epithelium. Its long-acting properties make it an important tool for investigating ENaC's role in pulmonary pathophysiology and potential therapeutic interventions. -
Voltage-gated Sodium Channel Blocker
Mexiletine-d6 hydrochloride is a deuterated analog of Mexiletine hydrochloride, acting primarily as a voltage-gated sodium channel blocker. This compound is classified as a Class IB antiarrhythmic agent and exhibits non-selective inhibition of sodium channels. It is valuable in research applications focused on cardiac rhythm management and the modulation of neuronal excitability. -
NaV1.8 Blocker
PF-06305591 dihydrate is a selective blocker of the voltage-gated sodium channel NaV1.8, exhibiting an IC50 of 15 nM. This compound demonstrates significant potential for neurophatic pain research due to its ability to modulate sodium ion flux and reduce excitability in sensory neurons. Its favorable preclinical in vitro ADME and safety profile make it a valuable tool for studying pain mechanisms and developing analgesic therapies. -
Nav1.7 Inhibitor
PF-05198007 is a selective inhibitor of the Nav1.7 sodium channel, demonstrating potent and orally active properties. This compound is utilized in research focused on pain signaling pathways, specifically in the exploration of pain relief mechanisms and the development of analgesic therapies. Its pharmacodynamic profile aligns closely with that of PF-05089771, making it a valuable tool for studying Nav1.7-related biological processes. -
NaV1.7 Antagonist
(Rac)-AMG8379 is a potent antagonist of the NaV1.7 sodium channel, demonstrating selective inhibition with IC50 values of 8.5 nM for human NaV1.7 and 18.6 nM for mouse NaV1.7. This compound is known for its oral bioavailability and serves as a valuable tool in research focused on pain pathways and sodium channel modulation. Investigations utilizing (Rac)-AMG8379 can advance understanding of the role of NaV1.7 in nociception and related disorders. -
R-enantiomer of Funapide
(R)-Funapide is the R-enantiomer of Funapide, targeting the sodium channels Nav1.7 and Nav1.8, among others, in the peripheral nervous system. This compound exhibits biological activity as a sodium channel inhibitor, which may have implications in pain modulation. Research applications for (R)-Funapide include studies on analgesic mechanisms and the exploration of peripheral nerve functions. -
Glucokinase Activator
Glucokinase activator 3 is a potent activator of glucokinase (GK) with an AC50 of 38 nM. This compound has demonstrated significant efficacy in reducing blood glucose levels in diet-induced obese (DIO) mice, highlighting its potential in type 2 diabetes research. Additionally, glucokinase activator 3 has been shown to inhibit the hERG channel and sodium channels in patch clamp assays, providing insight into its pharmacological profile. -
Analgesic Agent
(+)-Mepivacaine is an amide-type local anesthetic that exhibits potent analgesic and vasoconstrictive properties. By selectively binding to voltage-gated sodium channels on neuronal cell membranes, it effectively inhibits sodium influx, leading to a temporary loss of sensation in targeted areas. This compound is widely utilized in various research applications, particularly in studies focused on pain management and anesthesia. -
Antiarrhythmic Agent
(S)-Propafenone is an antiarrhythmic agent that functions primarily as a sodium channel blocker. This compound exhibits beta-blocking properties and demonstrates class 1 antiarrhythmic activity, making it valuable in the study of cardiac arrhythmias. Its efficacy in modulating myocardial excitability and conduction makes it an important tool for research applications aimed at understanding arrhythmic disorders and developing therapeutic strategies. -
Sodium Channel Blocker
Zilvetrigine is a sodium channel blocker that selectively inhibits voltage-gated sodium channels. This compound exhibits analgesic properties, making it valuable for pain management research. Its mechanism of action can be explored in studies related to neuropathic pain and other conditions mediated by sodium channel activity. -
Cardioactive Agent
DPI 201-106 is a cardiotonic agent that exerts its effects through a synergistic mechanism involving both sarcolemmal and intracellular pathways. It selectively modulates voltage-gated sodium channels (VGSCs), leading to a significant positive inotropic effect. This compound is useful for research applications focused on cardiac function and the modulation of ion channel activity in cardiac tissues. -
Sodium Channel Blocker
Tocainide hydrochloride is a sodium channel blocker that inhibits the activity of voltage-gated sodium channels, effectively reducing neuronal excitability in pain pathways. This compound is primarily used in research related to pain mechanisms and the treatment of conditions such as tinnitus. Tocainide hydrochloride functions as a primary amine analog of lidocaine, providing insights into sodium channel modulation and its therapeutic potential. -
Sodium Channel Inhibitor
Licarbazepine-d4 is a deuterated derivative of Licarbazepine, functioning as a sodium channel inhibitor. This compound exhibits anticonvulsant and mood-stabilizing properties, making it a valuable tool in the study of neurological disorders. It is particularly useful for researchers investigating the mechanisms of epilepsy and mood regulation. -
Endogenous Metabolite
N-Oleoyl Taurine is an endogenous metabolite that acts as an amino-acyl endocannabinoid. It is known to activate transient receptor potential (TRP) channels, specifically TRPV1 and TRPV4, implicating its role in calcium signaling. This compound has been isolated from rat brain and presents potential applications in research studying the physiological effects of TRP channel modulation and its involvement in neurological functions. -
Antiarrhythmic Agent
Droxicainide hydrochloride is an antiarrhythmic agent primarily targeting sodium channels. It is effective in the management of ventricular arrhythmias and is utilized in research to investigate cardiac electrophysiology. The compound is valuable for studying interactions in cardiac tissues and assessing the effects of sodium channel modulation on heart rhythm disorders. -
Endogenous Metabolite
N-Stearoyl Taurine is an endogenous metabolite that exhibits activity as a fatty acyl amide. It demonstrates the ability to activate members of the transient receptor potential (TRP) family of calcium channels, linking it to various physiological processes. This compound is primarily used in research applications related to lipidomics and neurobiology, particularly in studies investigating the role of amino-acyl endocannabinoids in the central nervous system. Its discovery in rat brain lipid profiles underscores its significance in the exploration of neuronal signaling pathways. -
Endogenous Metabolite
N-Lignoceroyl Taurine is an endogenous metabolite and taurine conjugate of lignoceric acid, identified through lipidomic analysis of bovine brain. This compound exhibits distinct biological activity as a substrate for fatty acid amide hydrolase (FAAH), with levels significantly elevated in FAAH knockout mice, indicating a potential role in lipid metabolism. Additionally, N-Lignoceroyl Taurine has been shown to activate transient receptor potential (TRP) calcium channels, including TRPV1 and TRPV4, highlighting its relevance in neurobiology and cellular signaling research. -
Natural Products
Thevetin A is a cardiac glycoside derived from the plant Cascabela thevetioides. It exhibits potent biological activity by inhibiting Na+/K+ ATPase, leading to increased intracellular calcium levels and enhanced contractility of cardiac muscle. This compound is primarily utilized in cardiovascular research to study its effects on cardiac function and potential therapeutic applications in heart disease. -
Endogenous Metabolite
UCCF-029 free base is a potent activator of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel. This compound showcases enhanced activity due to the benzannulation of the flavone A-ring at the 7,8-position, serving as a critical structural reference for the development of more effective flavonoid analogues. UCCF-029 demonstrates superior potency compared to apigenin in activating wild-type CFTR and possesses potential for activating the mutant G551D-CFTR, though its efficacy in this regard is not as pronounced as that of apigenin. This reagent is valuable for research into cystic fibrosis and related therapeutic strategies. -
Endogenous Metabolite
ISQ-1 hydrochloride is an isoquinolinone compound that functions as an inhibitor of the IKur potassium channel. It demonstrates potential to influence cardiac electrophysiology by modulating arrhythmic activity in atrial tissues. This reagent is primarily utilized in research focused on cardiac rhythm disorders and electrophysiological studies of heart functions. -
Endogenous Metabolite
D-myo-Inositol-1,4,5,6-tetraphosphate (D-Ins(1,4,5,6)P4) functions primarily as an endogenous metabolite involved in cellular signaling pathways. This compound exhibits a strong inhibitory effect on calcium-activated chloride channels, effectively operating at concentrations of 8-10 μM. It is commonly utilized in research applications focused on signal transduction and ion channel regulation. -
Biochemical Reagent
D-myo-Inositol-4,5-diphosphate sodium is a critical biochemical reagent that functions as a second messenger in cellular signaling pathways. It primarily targets calcium channels, facilitating the release of intracellular calcium when it binds to its receptor on the endoplasmic reticulum. This compound is valuable for research applications investigating signal transduction, calcium homeostasis, and cellular responses in various biological systems. -
Endogenous Metabolite
Stearoyl serotonin is a hybrid compound designed to target the endogenous metabolite systems and is structurally derived from arachidonoyl serotonin. This compound is investigated for its ability to function as a dual antagonist of fatty acid amide hydrolase (FAAH) and the TRPV1 channel, which are critical pathways in the modulation of pain. Preliminary studies suggest that modifications to the arachidonoyl structure, such as the introduction of an 18-carbon stearoyl moiety, may influence TRPV1 channel activity; replacement with saturated fatty acids has demonstrated significant inhibition of capsaicin-induced activation. This positions stearoyl serotonin as a potential candidate for research into pain mechanisms and therapeutic applications. -
Endogenous Metabolite
SU200 is a TRPV1 agonist that modulates intracellular calcium ion concentrations. It induces distinct calcium ion response patterns, displaying notable reactivity and peak efficacy. The effects of SU200 exhibit varying degrees of response delay and variability across different cell types. This compound offers potential avenues for pharmacological development and further research into calcium signaling pathways. -
Monoamine Transporter Inhibitor
Indatraline hydrochloride is a non-selective monoamine transporter inhibitor, primarily targeting the reuptake of dopamine, serotonin, and norepinephrine. This compound is relevant for research focused on antidepressant mechanisms. Additionally, Indatraline hydrochloride induces autophagy and inhibits cell proliferation, suggesting potential applications in the study of autophagy-related diseases, including atherosclerosis and restenosis. -
Stable Isotope
Safinamide-d4-1 is a deuterium-labeled derivative of Safinamide, a selective and reversible inhibitor of monoamine oxidase B (MAO-B) with an IC50 of 0.098 μM, demonstrating significantly lower inhibition of MAO-A (IC50=580 μM). In addition to its MAO-B inhibitory activity, Safinamide also interacts with sodium channels and modulates glutamate release, exhibiting a greater affinity at depolarized potentials (IC50=8 μM) compared to resting potentials (IC50=262 μM). This reagent is valuable for research applications related to neurobiology, particularly in the investigation of Parkinson's disease and ischemic stroke mechanisms. -
Serotonin Transporter Inhibitor
Lubazodone hydrochloride is a selective serotonin transporter inhibitor that primarily modulates serotonin levels in the central nervous system. Its biological activity is associated with antidepressant effects, making it a valuable compound for research into the treatment of depression and related mood disorders. This reagent can aid in the exploration of serotonin dynamics and its implications in various neurobiological studies.
