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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
NET Inhibitor
Nisoxetine is a potent and selective inhibitor of the norepinephrine transporter (NET) with a Kd of 0.76 nM. This compound exhibits antidepressant properties and functions as a local anesthetic, in addition to blocking voltage-gated sodium channels. Its mechanisms make it valuable for research in neuropharmacology and the investigation of depression and pain pathways. -
Sodium-Calcium Exchanger Inhibitor
KB-R7943 is a selective inhibitor of the sodium-calcium exchanger, exhibiting an IC50 value of 5.1 µM. This compound is utilized as a valuable tool in studies involving cardiac and renal failure models, facilitating research into calcium homeostasis and its implications in heart and kidney function. -
Sodium Channel Inhibitor
Benzamil is a sodium channel inhibitor, functioning as a non-selective blocker of epithelial sodium channels (ENaC) and a Na+/Ca2+ exchanger (NCX) inhibitor with an IC50 value of approximately 100 nM. Its pharmacological properties include the enhancement of myogenic vasoconstriction. Additionally, Benzamil inhibits TRPP3-mediated Ca2+-activated currents, exhibiting an IC50 of 1.1 μM. This compound is valuable for research applications focused on cardiovascular physiology and electrolyte transport mechanisms. -
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. -
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. -
Furin Inhibitor
BOS-318 is a highly selective and cell-permeable inhibitor of furin, exhibiting an IC50 value of 1.9 nM. This compound demonstrates the ability to protect epithelial sodium channels (ENaC) from activation by neutrophil elastase. BOS-318 is a valuable tool for research focused on cystic fibrosis and related pulmonary conditions. -
Sodium Channel Inhibitor
Mepivacaine hydrochloride is a sodium channel inhibitor that selectively binds to voltage-gated sodium ion channels in neuronal cell membranes. By inhibiting sodium influx and membrane depolarization, it provides significant local anesthetic effects. This compound is widely used in research applications related to nerve conduction studies and pain management investigations. -
Bacterial Inhibitor
Methyl Paraben is a bacterial inhibitor primarily used as a preservative in various applications due to its stability and non-volatility. It has been shown to enhance histamine release and modulate cellular immune responses, in addition to blocking sodium channels. Its properties make it valuable for studies exploring microbial inhibition and the mechanisms of ischemia-reperfusion injury. -
Dopamine Receptor Inhibitor
Fluphenazine dihydrochloride is a potent dopamine receptor antagonist primarily targeting dopamine D2 receptors in the mesolimbic, nigrostriatal, and tuberoinfundibular pathways. This phenothiazine derivative also exhibits the ability to inhibit neuronal voltage-gated sodium channels. Its key biological activities include the suppression of Methylphenidate-induced stereotyped behaviors and climbing in murine models. Fluphenazine dihydrochloride is widely utilized in research related to psychosis, diabetic peripheral neuropathy, and may also have implications for the inhibition of SARS-CoV-2. -
Sodium Channel Inhibitor
Oxybuprocaine hydrochloride is a sodium channel inhibitor that reversibly blocks sodium channels, effectively preventing the propagation of painful nerve impulses in tissues such as the cornea, conjunctiva, and sclera. This compound is primarily utilized in ophthalmology and otolaryngology for its anesthetic properties, providing localized pain relief during various medical procedures. Its ability to inhibit nerve signal transmission makes it valuable for both diagnostic and therapeutic applications in ocular and ear, nose, and throat treatments. -
Sodium Channel Inhibitor
Propafenone hydrochloride is a sodium channel inhibitor primarily used as an anti-arrhythmic agent. It effectively treats conditions related to rapid heartbeats, including atrial and ventricular arrhythmias. This compound is useful in research applications focused on cardiac rhythm disturbances and the pharmacological modulation of ion channels. -
Sodium Channel Inhibitor
Triamterene is a sodium channel inhibitor that selectively blocks epithelial Na+ channels (ENaC) in a voltage-dependent manner. It exhibits mild diuretic properties and is utilized in the management of conditions related to fluid retention. Additionally, Triamterene serves as an inhibitor of the TGR5 receptor, contributing to its diverse biological effects and applications in research related to renal and metabolic processes. -
Sodium Channel Inhibitor
Ropivacaine mesylate acts primarily as a sodium channel inhibitor, serving as a long-acting amide local anesthetic. It effectively blocks impulse conduction by reversibly inhibiting sodium ion influx in nerve fibers, making it suitable for procedures requiring spinal block anesthesia. Additionally, Ropivacaine has been identified as an inhibitor of the K2P potassium channel TREK-1, exhibiting an IC50 value of 402.7 μM in COS-7 cell membranes. This compound is relevant for research into pain management and neuronal activity modulation. -
Sodium Channel Inhibitor
Mepivacaine is an amide-type local anesthetic that functions as a sodium channel inhibitor. By binding to specific voltage-gated sodium ion channels in neuronal cell membranes, Mepivacaine effectively inhibits sodium influx and membrane depolarization. This agent is primarily utilized in various research applications within the fields of pain management and anesthesia. -
Sodium Channel Inhibitor
Riluzole hydrochloride is a sodium channel inhibitor that exhibits anticonvulsant properties. It functions primarily as a use-dependent Na+ channel blocker and also has the capability to inhibit GABA uptake, with an IC50 of 43 μM. This compound is commonly utilized in neurological research applications, particularly in studies focused on epilepsy and neuroprotection. -
Sodium Channel Inhibitor
Ropivacaine hydrochloride is a potent sodium channel inhibitor that effectively disrupts impulse conduction by reversibly blocking sodium ion influx in nerve fibers. Additionally, it inhibits the K2P TREK-1 potassium channel with an IC50 of 402.7 μM in COS-7 cell membranes. This compound is primarily applied in the management of neuropathic pain in various in vivo research contexts. -
Sodium Channel Inhibitor
Propoxycaine hydrochloride is a sodium channel inhibitor that disrupts voltage-gated sodium channel activity, leading to a reduction in ionic flux essential for the initiation and propagation of action potentials. This compound is primarily utilized in research to investigate sensory nerve function and analgesic mechanisms, resulting in local anesthetic effects characterized by a loss of sensation. -
Nav1.7 Inhibitor
Nav1.7-IN-22 is a selective inhibitor of the voltage-gated sodium channel Nav1.7. By blocking the activity of Nav1.7, this compound effectively inhibits abnormal electrical signal generation and conduction in sensory neurons. Nav1.7-IN-22 is utilized in research focused on pain mechanisms, providing insights into potential therapeutic applications for pain management.
