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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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 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. -
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. -
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. -
NaV1.7 Inhibitor
GDC-0276 is a selective and reversible inhibitor of the NaV1.7 ion channel with an IC50 value of 0.4 nM. This orally active compound demonstrates favorable pharmacokinetic properties and is well tolerated, making it a promising candidate for pain management. GDC-0276 may offer an alternative to existing analgesics, addressing issues such as addiction and off-target side effects in the treatment of various pain disorders. -
Nav1.7 Inhibitor
GDC-0310 is a selective inhibitor of the Voltage-gated sodium channel Nav1.7, demonstrating a potent inhibitory activity with an IC50 of 0.6 nM against hNav1.7. This compound is primarily utilized in research exploring pain mechanisms, particularly in the context of chronic pain and neuropathic pain models. Its specificity makes it a valuable tool for investigating Nav1.7's role in various physiological and pathophysiological processes. -
NaV1.8 Inhibitor
VX-150 is a highly selective inhibitor of the sodium channel NaV1.8. This compound demonstrates significant analgesic properties and shows potential for research in various pain-related indications. Its oral bioavailability makes it a valuable tool for studies investigating pain mechanisms and the development of novel pain therapies. -
NaV1.6/NaV1.2 Inhibitor
XPC-5462 is a selective inhibitor of the voltage-gated sodium channels NaV1.6 and NaV1.2, exhibiting IC50 values of 10.9 nM and 10.3 nM, respectively. It effectively suppresses epileptiform activity in ex vivo brain slice seizure models, making it a valuable tool for research in epilepsy and related neurological disorders. Its ability to modulate excitability in neuronal populations highlights its potential for studying sodium channel dynamics and their role in neuronal excitability. -
Sodium Channel Inhibitor
RY796 is a selective sodium channel inhibitor targeting voltage-gated sodium channels. Its potent activity has demonstrated analgesic effects, making it relevant for pain research. This compound can be utilized in studies investigating the modulation of sodium channels in various physiological and pathological conditions. -
Nav1.8 Inhibitor
Sodium Channel Inhibitor 6 is a selective Nav1.8 inhibitor primarily targeting voltage-gated sodium channels associated with neuronal excitability. It demonstrates significant biological activity in modulating pain pathways, making it a valuable tool for research on neuropathic pain mechanisms. This compound is suitable for in vitro and in vivo studies aimed at understanding the role of Nav1.8 in pain signaling and potential therapeutic interventions. -
ENaC Inhibitor
Phenamil methanesulfonate is a potent inhibitor of the epithelial sodium channel (ENaC), exhibiting an IC50 of 400 nM. In addition, it competitively inhibits TRPP3, with an IC50 of 140 nM, thereby blocking TRPP3-mediated calcium transport. This compound has potential applications in promoting bone repair by strongly activating the BMP signaling pathway and is valuable in research related to cystic fibrosis lung disease. -
NaV1.8 Inhibitor
PF-04885614 is a potent inhibitor of the sodium channel NaV1.8, primarily involved in pain signaling pathways. Its inhibition may provide therapeutic benefits for managing neurological and neurodevelopmental disorders. This compound is valuable for research applications focused on pain mechanisms and the development of analgesic therapies. -
CRMP2-Ubc9 Interaction/NaV1.7 Inhibitor
AZ194 is a novel, orally active inhibitor that targets the interaction between CRMP2 and Ubc9, functioning as a specific inhibitor of NaV1.7 with an IC50 of 1.2 μM. By blocking the SUMOylation process of CRMP2, AZ194 effectively reduces the surface expression of NaV1.7, demonstrating significant antinociceptive properties. This agent is useful for research in pain modulation and associated neurological studies. -
Sodium Channel Inhibitor
3'-Methoxydaidzein is an isoflavone acting as a sodium channel inhibitor. It selectively inhibits sodium channel subtypes NaV1.7, NaV1.8, and NaV1.3 with IC50 values of 181 nM, 397 nM, and 505 nM, respectively. This compound exhibits significant analgesic activity through its modulation of voltage-gated sodium channels, making it a valuable tool for research in pain pathways and related therapeutic applications. -
Sodium Channels Inhibitor
Vormatrigine is an orally active inhibitor of sodium channels, demonstrating anti-epileptic properties. This compound is utilized in research to investigate human focal and generalized epilepsy, providing insights into its mechanisms and potential therapeutic applications. Its effectiveness in modulating sodium channel activity makes it a valuable tool for studying epilepsy-related pathophysiology. -
NaV1.7 Inhibitor
DS-1971a is a selective and orally bioavailable inhibitor of the voltage-gated sodium channel NaV1.7, with IC50 values of 22.8 nM and 59.4 nM for human and murine NaV1.7, respectively. This compound demonstrates significant analgesic properties, making it a valuable tool for research in pain management and neurological studies. Its specificity for NaV1.7 positions DS-1971a as an important reagent for exploring the mechanisms of pain signaling and potential therapeutic interventions. -
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. -
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. -
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. -
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. -
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. -
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. -
Nav1.8 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. -
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. -
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. -
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. -
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. -
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.
