Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Stable Isotope
Bupivacaine-d9 hydrochloride is a deuterium-labeled analog of Bupivacaine hydrochloride, primarily known for its role as an NMDA receptor inhibitor. This compound effectively blocks sodium, L-calcium, and potassium channels, demonstrating potent inhibition of SCN5A channels with an IC50 value of 69.5 μM. Bupivacaine-d9 hydrochloride is valuable for research focused on chronic pain modulation and neuronal signaling studies. -
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. -
TRPV3 Inhibitor
Trpvicin is a selective inhibitor of the TRPV3 channel, demonstrating IC50 values of 0.41 μM and 0.22 μM for human TRPV3-WT and the hTRPV3-G573S mutant, respectively. Its mechanism of action involves stabilizing TRPV3 in a closed conformation primarily through VSLD-PD binding, while also engaging alternative binding sites in the G573S mutant to impede channel activity. Trpvicin exhibits minimal off-target effects on other TRP family members, making it a valuable tool for studying inflammation, immunology, and conditions associated with itch and hair loss in mouse models. -
TRPA1 Channel Antagonist
ADM 12 is a selective antagonist of the transient receptor potential ankyrin 1 (TRPA1) channel. It effectively inhibits nitroglycerin-induced trigeminal hyperalgesia in animal models, leading to decreased expression of pain-related genes such as c-Fos and TRPA1, as well as neuropeptides including CGRP and substance P. This compound holds potential for research applications in the fields of migraine and neuropathic pain. -
TRPM3 Inhibitor
TRPM3-IN-1 is a potent inhibitor of the TRPM3 ion channel, exhibiting an IC50 value of less than 1 µM. This compound is valuable for research focused on the modulation of pain mechanisms and inflammatory responses. Its ability to selectively target TRPM3 makes it a promising tool for investigating related biological pathways and potential therapeutic applications. -
TRPML1 Agonist
ML-SA5 is a potent agonist of the TRPML1 cation channel, effectively activating the endosomal TRPML1 current in DMD myocytes with an EC50 of 285 nM. This compound demonstrates significant anticancer activity by inhibiting tumor growth, making it valuable for research applications aimed at exploring TRPML1 functions and their implications in cancer biology and muscle disorders. -
TRPC Agonist
IA-Alkyne is a TRPC channel (TRPC) agonist that facilitates the investigation of respiratory infections through enhanced channel activity. This compound serves as a versatile chemical probe for quantitative profiling of cysteine reactivity, enabling isotopic tagging. Additionally, IA-Alkyne features an alkyne functional group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a valuable tool for click chemistry applications in various biological research studies. -
TRPM3 Agonist
CIM0216 is a selective agonist of the TRPM3 ion channel, demonstrating potent stimulation specifically for this target over other TRPM family members such as TRPM1, TRPM2, and TRPM4-8. It activates TRPM3-dependent pathways to induce pain and facilitate the release of neuropeptides from sensory nerve terminals in vitro. This compound serves as an important research tool for investigating the physiological roles of TRPM3 and has applications in the study of neurogenic inflammation. -
TRPC6 Antagonist
BI-749327 is a potent and highly selective antagonist of the TRPC6 channel, exhibiting IC50 values of 13 nM for mouse TRPC6, 19 nM for human TRPC6, and 15 nM for guinea pig TRPC6. This compound demonstrates an 85-fold selectivity for mouse TRPC6 over TRPC3 and a 42-fold selectivity over TRPC7. Due to its oral bioavailability and inhibition of TRPC6, BI-749327 is suitable for research applications involving ion channel modulation and the investigation of associated physiological and pathological processes. -
TRPML1/2/3 Inhibitor
(1R,2R)-ML-SI3 is a selective inhibitor of the TRPML1, TRPML2, and TRPML3 ion channels, with IC50 values of 1.6 μM, 2.3 μM, and 12.5 μM, respectively. This compound is valuable for investigating the physiological roles of TRPML channels in cellular signaling and ion homeostasis. It is well-suited for research applications related to lysosomal function, calcium signaling, and potential therapeutic strategies targeting lysosomal storage disorders. -
TRPV2 Antagonist
SET2 is a selective antagonist of the TRPV2 channel, with an IC50 value of 0.46 μM. This compound effectively inhibits TRPV2-mediated signaling, thereby suppressing the migration of prostate cancer cells. Additionally, SET2 diminishes lysophosphatidic acid (LPA)-induced increases in cytoplasmic calcium levels, making it useful for research focused on cancer biology and calcium signaling pathways. -
TRPV4 Antagonist
GSK205 is a selective antagonist of the Transient Receptor Potential Vanilloid 4 (TRPV4) channel, exhibiting an IC50 of 4.19 μM for TRPV4-mediated calcium influx inhibition. This compound is instrumental in studying TRPV4's role in various physiological and pathological processes, including pain sensation, inflammation, and cellular mechanotransduction. GSK205 is a valuable tool for researchers investigating the therapeutic potential of TRPV4 modulation in various disease models. -
TRPM2 Inihibitor
JNJ-28583113 is a potent TRPM2 inhibitor that exhibits permeability across the blood-brain barrier. By inhibiting TRPM2, JNJ-28583113 effectively blocks the phosphorylation of GSK3α and β subunits, offering protective effects against oxidative stress-induced cell death. Additionally, it reduces cytokine release from microglia in response to pro-inflammatory stimuli, making it a valuable tool for research in neuroinflammation and oxidative stress pathways. -
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. -
TRPC3 Agonist
GSK1702934A is a selective agonist of the TRPC3 ion channel. It enhances cardiac contractility and plays a role in the modulation of arrhythmogenesis through TRPC3 activation. This compound is valuable for research applications investigating cardiac function and the physiological effects of TRPC3 modulation in various disease models. -
TRPA1/TRPV1 Agonist
Hydroxy-α-sanshool is an agonist of the transient receptor potential ankyrin 1 (TRPA1) and TRP vanilloid 1 (TRPV1) channels, exhibiting EC50 values of 69 μM and 1.1 μM, respectively. This compound plays a significant role in pain research by activating these nociceptive pathways, potentially contributing to studies on pain sensation and modulation. -
TRPC4/5 Activator
Englerin A is a selective activator of TRPC4 and TRPC5 channels, exhibiting EC50 values of 11.2 nM and 7.6 nM, respectively. This compound is known to induce cell death in renal carcinoma cells through the mechanism of increased calcium influx and subsequent calcium overload. Englerin A serves as a valuable tool for investigating TRPC channel function and potential therapeutic approaches in cancer research. -
RARβ/RARα Antagonist
LE135 is a selective antagonist of retinoic acid receptors RARα and RARβ, exhibiting a Ki of 1.4 μM for RARα and a significantly higher affinity of 220 nM for RARβ. This compound demonstrates high specificity for these targets, with minimal interaction with RARγ and RXR isoforms. Additionally, LE135 acts as a potent activator of TRPV1 and TRPA1 receptors, with EC50 values of 2.5 μM and 20 μM, respectively, making it a valuable tool for studying pathways involving these ion channels in various biological contexts. -
TRPV2 Blocker
TRPV2-selective blocker 1 is a selective inhibitor of the transient receptor potential vanilloid 2 (TRPV2) channel, exhibiting an IC50 of 6.3 μM. This compound selectively targets TRPV2 without affecting TRPV1, TRPV3, or TRPV4 channels. Its primary biological activities include blocking TRPV2-mediated Ca2+ influx in macrophages and inhibiting macrophage phagocytosis, making it a valuable tool for research on immune responses and cellular signaling pathways involving TRPV2.
