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Catalog No.
Product Name
Application
Product Information
Citations
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Sodium Channel Inhibitor
R 59494 is a sodium channel inhibitor that effectively blocks Na+ and Ca2+ uptake triggered by veratridine exposure. This compound exhibits significant anti-ischemic properties, making it valuable for research in cardiovascular and neuroprotective studies. Its ability to modulate ion channel activity positions R 59494 as a useful tool for investigating the mechanisms of ischemia-related cellular damage. -
NaV1.8 Channel Inhibitor
Analgesic agent-2 is a selective NaV1.8 channel inhibitor, exhibiting a reported IC50 of 50.18 nM in HEK293 cells expressing the human NaV1.8 channel. It demonstrates significant analgesic activity, making it a valuable tool for pain research. This compound is ideal for studies investigating the role of NaV1.8 in nociception and the development of novel analgesic therapies. -
Nav1.8 Inhibitor
Nav1.8-IN-15 is a potent inhibitor of the voltage-gated sodium channel Nav1.8. It demonstrates significant analgesic effects and is relevant for research exploring pathways involved in chronic pain management. This compound can facilitate the study of Nav1.8's role in pain signaling and aid in the development of novel therapeutic strategies for pain relief. -
NaV1.7 Inhibitor
Sodium Channel-IN-7 is a selective inhibitor of the NaV1.7 voltage-gated sodium channel. It interacts with the voltage-sensor domain 4 (VSD4) binding pocket of NaV1.7, demonstrating limited interaction with residue Try1537. This compound is primarily utilized in research focused on pain mechanisms and pain-related disorders. -
Sodium Channel Inhibitor
Cofirasersen is a sodium channel inhibitor that targets the epithelial sodium channel (ENaC). It is specifically developed to downregulate ENaC expression in the lungs, where hyperactivity of ENaC is implicated in cystic fibrosis, a disorder linked to mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) gene. This compound has potential applications in research related to cystic fibrosis and the modulation of sodium transport in pulmonary tissues. -
NaV1.7 Inhibitor
PF-06456384 is a potent and selective inhibitor of NaV1.7, exhibiting an IC50 of 0.01 nM. This compound is primarily utilized in research involving pain mechanisms, particularly in formalin pain model studies, to elucidate the role of NaV1.7 in nociceptive signaling. Its high selectivity makes it an important reagent for exploring therapeutic strategies targeting chronic pain conditions. -
Sodium Channel Inhibitor
Nav1.8-IN-1 is a selective inhibitor of the Na(v)1.8 sodium channel, demonstrating significant potency in blocking its activity. This compound is particularly relevant for research focused on inflammatory and neuropathic pain pathways, providing valuable insights into pain mechanisms and potential therapeutic strategies. Its ability to modulate sodium channel function makes it a promising tool for understanding pain-related conditions. -
NaV1.7 Inhibitor
DS43260857 is a selective inhibitor of the sodium channel NaV1.7, exerting strong inhibitory effects on both human and mouse variants of the channel. It demonstrates IC50 values of 6.6 μM for hNaV1.1, 14 μM for hNaV1.5, 0.015 μM for hNaV1.7, and 0.061 μM for mNaV1.7. This compound is useful for investigating pain pathways and assessing the role of NaV1.7 in nociception-related research. -
Nav1.7 Inhibitor
PF 05089771 tosylate is a selective Nav1.7 inhibitor, known for its potent biological activity with IC50 values of 11 nM for human Nav1.7 and varying efficacy across other species. This arylsulfonamide compound is orally active, making it a valuable tool for investigating pain and diabetic neuropathy mechanisms in preclinical research. Its specificity for Nav1.7 highlights its potential application in developing novel analgesic therapies. -
Nav1.8 Inhibitor
Nav1.8-IN-18 is a selective inhibitor of the voltage-gated sodium channel Nav1.8. It exhibits significant activity in modulating neuronal excitability, making it a valuable tool for investigating pain pathways and sensory neuron function. This compound is suited for research applications focused on chronic pain models and neuropathic conditions. -
Sodium Channel Inhibitor
P552-02 mesylate is a sodium channel inhibitor that demonstrates significant potential for the treatment of cystic fibrosis. Its primary mechanism involves enhancing mucociliary clearance in the lungs, contributing to improved respiratory function. Additionally, P552-02 mesylate minimizes the risk of hyperkalaemia, making it a valuable compound for researchers studying respiratory diseases and therapeutic interventions. -
Nav1.7 Inhibitor
QLS-81 is a selective inhibitor of the Nav1.7 ion channel, demonstrating an inhibition constant (IC50) of 1.5 μM. This compound exhibits potent analgesic properties, effectively alleviating both neuropathic and inflammatory pain. By targeting the inactivated state of Nav1.7 channels, QLS-81 mediates frequency-dependent inhibition, making it a valuable tool for research focused on chronic pain mechanisms and potential therapeutic interventions. -
Sodium Channel Inhibitor
Nav1.8-IN-20 is a potent inhibitor of the voltage-gated sodium channel Nav1.8, demonstrating an IC50 value of 14 nM. By blocking the generation and conduction of action potentials in peripheral nociceptive neurons, it exerts significant analgesic effects. This compound is valuable for research into various pain models, including acute pain, chronic pain, inflammatory pain, and neuropathic pain. -
Nav1.8 channel Inhibitor
Nav1.8-IN-11 is a potent inhibitor of the Nav1.8 sodium channel, exhibiting an IC50 value of 0.1 nM. This compound is valuable for investigating pain disorders, as it modulates neuronal excitability and may provide insight into the underlying mechanisms of pain signaling and management. Research applications include exploring therapeutic strategies for chronic pain conditions. -
Sodium Channel Inhibitor
L589420-0-2 is a sodium channel inhibitor that modulates intracellular sodium ion concentrations, ultimately influencing the electrophysiological properties of cells. This compound demonstrates specific inhibitory activity in human erythrocytes and can be instrumental in studies related to cardiovascular disease. Its ability to affect sodium ion dynamics makes it a valuable tool for research in cellular biology and pharmacology. -
Nav1.8 Inhibitor
Nav1.8-IN-13 is a selective inhibitor of the voltage-gated sodium channel Nav1.8, with a reported pIC50 of 7.9. This compound is utilized in research to investigate the role of Nav1.8 in pain signaling pathways and neuronal excitability. Its inhibitory properties make it a valuable tool for studying potential therapeutic approaches for pain management and related neurological disorders. -
Nav1.8 channel Inhibitor
Nav1.8-IN-12 is a selective inhibitor of the Nav1.8 sodium channel, known to play a crucial role in transmitting pain signals. This compound is valuable for investigating various pain-related diseases and disorders, facilitating the development of therapeutic strategies targeting neuropathic pain and inflammatory conditions. -
Sodium Channel Inhibitor
Oe-9000 is a sodium channel inhibitor that demonstrates local anesthetic activity by effectively blocking voltage-gated Na+ currents in neurons. It targets both TTX-sensitive and TTX-resistant currents, showing enhanced performance compared to other local anesthetics. This compound is valuable for research applications in pain management and neuropharmacology. -
Nav1.5 Inhibitor
Nav1.5-IN-1 is a selective inhibitor of the sodium channel Nav1.5, exhibiting an IC50 of 1.38 μM. With demonstrated selectivity over other Nav subtypes, it effectively reduces cardiac conduction in isolated rat hearts. This compound serves as a valuable tool for investigating the mechanisms underlying cardiac arrhythmias. -
Sodium Channel Inhibitor
E-0747 is a sodium channel inhibitor that specifically targets Na[+] channels in cardiomyocytes. By blocking these channels, E-0747 exhibits antiarrhythmic properties, making it valuable for research into cardiac function and arrhythmia management. This compound can be utilized in studies investigating the mechanisms of electrical conduction and the potential therapeutic effects on various cardiac disorders. -
Nav1.8 Inhibitor
Nav1.8-IN-21 is a selective inhibitor of the Nav1.8 sodium channel, known for its role in transmitting pain signals. This compound exhibits significant analgesic activity and is valuable for research applications focused on pain management and neurophysiology. Its targeted inhibition makes it a useful tool for understanding the mechanisms of nociception and developing novel pain therapeutics. -
Nav1.2 Inhibitor
Nav1.2-IN-1 is a selective inhibitor of the Nav1.2 sodium channel, characterized by its structure as a 3-(1,2,3,6-tetrahydropyridine)-4-azaindole derivative. It effectively reduces the peak amplitude of Nav1.2 currents with an IC50 value of 7.79 μM. This compound demonstrates significant antiepileptic properties, exhibiting a potent anticonvulsant effect while maintaining low neurotoxicity in subcutaneous pentetrazole-induced epilepsy models. It serves as a valuable tool for research in epilepsy and sodium channel modulation. -
Nav1.8 channel Inhibitor
Nav1.8-IN-8 is a selective inhibitor of the Nav1.8 ion channel, which is associated with various pain pathways and neuronal excitability. By inhibiting Nav1.8 channels, this compound may help to mitigate pain and other disorders mediated by sodium ion channel dysregulation. Nav1.8-IN-8 serves as a valuable tool for research into pain mechanisms and therapeutic strategies targeting sodium channel activity. -
Sodium Channel Inhibitor
ProTx II is a highly selective inhibitor of Nav1.7 sodium channels, exhibiting an IC50 of 0.3 nM and demonstrating over 100-fold selectivity for Nav1.7 compared to other sodium channel subtypes. This compound inhibits sodium channel conductance and alters the activation threshold to more positive potentials, effectively blocking action potential propagation in nociceptive neurons. ProTx II is valuable for research applications involving pain signaling and neuromodulation. -
Sodium Channel Inhibitor
Detajmium is a sodium channel inhibitor known for its ability to block Na+ channels, thereby affecting ventricular conduction and refractoriness. At a concentration of 0.3 μM, Detajmium prolongs intraventricular conduction time similarly to propafenone, but exhibits a distinct temporal profile during rapid ventricular pacing. This unique characteristic makes Detajmium valuable for research applications focusing on cardiac electrophysiology and arrhythmia management. -
Sodium Channel Inhibitor
GX-585 is a sulfonamide analog that selectively inhibits the Nav1.7 sodium channel. This compound exhibits significant analgesic activity, making it a promising candidate for studies focused on neuropathic pain and inflammation management. Its ability to modulate sodium channel activity provides valuable insights into pain pathways and related biological processes. -
Sodium Channel Inhibitor
Sodium Channel Inhibitor 4 is a selective sodium channel inhibitor that disrupts sodium ion influx in excitable cells. This compound exhibits significant activity in modulating neuronal excitability and is useful in the study of pain pathways and seizure disorders. It serves as a valuable tool for researchers investigating the physiological and pharmacological roles of sodium channels in various biological systems. -
Nav1.8 Inhibitor
Nav1.8-IN-22 is a selective inhibitor of the Nav1.8 sodium channel, exerting its effects through direct binding to the channel. This compound modulates sodium channel activity and is intended for research applications related to pain mechanisms. Its specificity for Nav1.8 makes it a valuable tool for investigating pain pathways and developing potential analgesic therapies. -
Nav1.7 Inhibitor
ProTx-III is a potent and selective inhibitor of the voltage-gated sodium channel Nav1.7, exhibiting an IC50 of 2.1 nM. Derived from the venom of the Peruvian green velvet tarantula, this spider venom peptide features a characteristic inhibitor cystine knot (ICK) motif. ProTx-III plays a critical role in reversing pain responses and is instrumental in researching conditions such as chronic pain, epilepsy, and cardiac arrhythmias. -
Nav1.8 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. -
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. -
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. -
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. -
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. -
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 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. -
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. -
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. -
TRPML1/2/3 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. -
TRPM4 Inhibitor
TRPM4-IN-2 is a potent inhibitor of the transient receptor potential melastatin 4 (TRPM4) channel, exhibiting an IC50 value of 0.16 µM. This compound is particularly relevant in the study of prostate and colorectal cancers, providing valuable insights into TRPM4's role in tumor biology and potential therapeutic pathways. Its ability to modulate TRPM4 activity makes it a useful tool in cancer research and drug development. -
TRPV1/A1 Inhibitor
Resolvin D2 is a potent TRPV1 and TRPA1 inhibitor with a primary mechanism targeting these transient receptor potential channels in primary sensory neurons. As a metabolite of docosahexaenoic acid (DHA), it exhibits significant anti-inflammatory and anti-infective properties, effectively regulating leukocyte function and controlling microbial sepsis. This compound's high potency and specificity make it a valuable tool in research focused on pain modulation and inflammatory responses. -
TRPM4 Inhibitor
TRPM4-IN-1 is a selective inhibitor of the TRPM4 ion channel, exhibiting an IC50 value of 1.5 μM. This compound is primarily utilized in studies related to cardiac diseases and prostate cancer, facilitating insights into the role of TRPM4 in these conditions. Its potency makes it a valuable tool for investigating the modulation of calcium signaling pathways in various biological contexts. -
TRPA1 Inhibitor
AP-18 is a selective inhibitor of the transient receptor potential ankyrin 1 (TRPA1), effectively blocking TRPA1 activation by 50 µM cinnamaldehyde with IC50 values of 3.1 µM for human and 4.5 µM for mouse TRPA1. This compound demonstrates significant analgesic properties, as it reverses complete Freund's adjuvant-induced mechanical hyperalgesia in murine models. Additionally, AP-18 significantly reduces AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 µM, making it a valuable tool for research into pain mechanisms and TRPA1-related pathways. -
TRPM7 Inhibitor
VPC01091.4 is a potent TRPM7 inhibitor that effectively blocks TRPM7 current at low micromolar concentrations. This compound is capable of crossing the blood-brain barrier, making it suitable for neurological studies. Additionally, VPC01091.4 demonstrates significant anti-inflammatory properties, halting systemic inflammation in vivo, and can be utilized in research focused on inflammation and neuronal signaling pathways. -
TRPA1 Inhibitor
BAY-390 is a selective TRPA1 inhibitor that effectively penetrates the blood-brain barrier. It demonstrates potent inhibitory activity with IC50 values of 16 nM for human TRPA1 (hTRPA1) FLIPR, 82 nM for hTRPA1 electrophysiology (Ephys), 63 nM for rat TRPA1 (rTRPA1) FLIPR, and 35 nM for rat dorsal root ganglion (DRG) Ephys. BAY-390 is suitable for investigating the role of TRPA1 in inflammation-related research.
