Shop By
Catalog No.
Product Name
Application
Product Information
Citations
-
Human EAAT2 Inhibitor
WAY-213613 hydrochloride is a potent and selective inhibitor of the human excitatory amino acid transporter 2 (EAAT2). With an IC50 value of 85 nM, it effectively modulates glutamate transport, making it a valuable tool for investigating glutamatergic signaling in the central nervous system. This compound is suitable for research applications exploring neurobiology and potential therapeutic interventions related to neurodegenerative diseases. -
EAAT1 Inhibitor
UCPH-102 is a highly selective inhibitor of the excitatory amino acid transporter 1 (EAAT1), exhibiting an IC50 value of 0.43 µM. This compound demonstrates significant anti-proliferative effects on T-cell acute lymphoblastic leukemia (T-ALL) cells. Furthermore, UCPH-102's favorable blood-brain barrier permeability makes it a valuable tool for research in neurodegenerative diseases such as amyotrophic lateral sclerosis and Alzheimer’s disease, as well as conditions related to chronic pain and obsessive-compulsive disorder. -
EAAT Inhibitor
L-threo-3-Hydroxyaspartic acid functions as a selective inhibitor of excitatory amino acid transporters (EAATs), exhibiting inhibitory constants (Kis) of 11, 19, and 14 μM for EAAT1, EAAT2, and EAAT3, respectively, in HEK293 cell lines. This compound plays a crucial role in the study of neurotransmitter regulation and excitotoxicity, making it valuable for research related to neurological disorders and synaptic transmission. Its ability to modulate glutamate signaling contributes to understanding potential therapeutic pathways for conditions such as epilepsy and neurodegenerative diseases. -
EAAT3 Inhibitor
SLC1A1/EAAT3-IN-1 is a selective inhibitor of the excitatory amino acid transporter 3 (EAAT3), exhibiting an IC50 of 7.2 μM for human EAAT3 while showing significantly reduced inhibition of EAAT1, 2, and 4 (IC50: ~250 μM). This compound is primarily utilized in research related to psychiatric disorders, including obsessive-compulsive disorder and schizophrenia, and can aid in the investigation of neurotransmitter dynamics and therapeutic strategies targeting EAAT3. -
EAAT Inhibitor
DL-TBOA ammonium is a selective inhibitor of excitatory amino acid transporters (EAATs), demonstrating IC50 values of 70 μM, 6 μM, and 6 μM for EAAT1, EAAT2, and EAAT3, respectively. This compound effectively inhibits the uptake of [14C]glutamate in COS-1 cells expressing human EAAT1 and EAAT2, with Ki values of 42 μM and 5.7 μM. Additionally, DL-TBOA ammonium competitively inhibits EAAT4 and EAAT5, featuring Ki values of 4.4 μM and 3.2 μM, respectively. Its distinct mechanism renders it a valuable tool for studies on excitatory neurotransmission and the role of glutamate transporters in neurological research. -
EAAT2/4 Inhibitor
(±)-threo-3-Methylglutamic acid is a potent inhibitor of excitatory amino acid transporters EAAT2 and EAAT4. It functions as an ionotropic glutamate receptor agonist and is effective in inhibiting glutamate uptake in rod outer segments. This compound is valuable for research applications focusing on glutamatergic signaling and transport mechanisms in the nervous system. -
GABA Uptake Inhibitor
Nipecotic acid is a potent inhibitor of GABA uptake in neurons and glial cells, significantly impacting GABAergic neurotransmission. This compound has also been shown to directly activate GABAA-like chloride channels, with an effective concentration (EC50) of approximately 300 μM. Its biological activity makes nipecotic acid valuable for research applications focused on GABAergic signaling and associated neurological processes. -
BCRP Inhibitor
5,7-Dimethoxyflavone is a potent inhibitor of the Breast Cancer Resistance Protein (BCRP). It exhibits significant biological activities, including anti-obesity, anti-inflammatory, and antineoplastic effects. Additionally, this compound has been shown to inhibit cytochrome P450 (CYP) 3A enzymes, making it valuable for research applications focused on drug resistance and metabolic pathways in cancer therapy. -
Sodium Channel Inhibitor
(-)-Sparteine sulfate pentahydrate is a sodium channel inhibitor that acts as a class 1a antiarrhythmic agent. It has demonstrated notable biological activity in modulating cardiac excitability and can be utilized in research focusing on arrhythmias and pharmacological studies related to ion channel function. This reagent is suitable for investigating the effects of sodium channel blockade in various biological models. -
Nav1.7 Inhibitor
Nav1.7-IN-6 is a selective inhibitor targeting the voltage-gated sodium channel Nav1.7, which is important in pain signaling pathways. This compound demonstrates significant biological activity in modulating neuronal excitability, making it a valuable tool for research on pain mechanisms and potential therapeutic interventions in pain disorders. Its specificity for Nav1.7 enhances its utility in elucidating the role of this channel in nociception and related studies. -
Sodium Channel Inhibitor
B-GYKI-38233 hydrochloride is a sodium channel inhibitor that exhibits potent antiarrhythmic properties. This compound is utilized in research focused on the modulation of sodium channels, which play a critical role in cardiac excitability and conductivity. Its mechanism of action makes it a valuable tool for the investigation of arrhythmias and related cardiovascular disorders. -
Nav1.8 channel Inhibitor
Nav1.8-IN-10 is a selective inhibitor of the Nav1.8 ion channel. At a concentration of 4 nM, it achieves an impressive blocking rate of 79.4%, demonstrating its potency. This compound is primarily utilized in the research of pain disorders, facilitating investigations into the modulation of pain pathways and potential therapeutic interventions. -
Nav1.8 Inhibitor
Nav1.8-IN-5 is a selective inhibitor of the voltage-gated sodium channel Nav1.8. It demonstrates potent biological activity against Nav1.8-mediated pain and pain-related disorders, making it a valuable tool for research in these areas. Additionally, Nav1.8-IN-5 can facilitate studies related to cardiovascular diseases, including conditions such as atrial fibrillation, by modulating sodium channel activity. -
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.
