Catalog No.
Product Name
Application
Product Information
Citations
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Type-2 Chloride Channel Activator
Cobiprostone is a type-2 chloride channel activator known for its protective effects against NSAID-induced cellular damage. It effectively prevents Indomethacin-induced depolarization of mitochondrial membrane potential and reverses subsequent loss of membrane integrity. This compound is valuable for research focused on mitochondrial function and cellular responsiveness to ion channel modulation. -
Chloride Channel Inhibitor
NS3736 is an orally bioavailable inhibitor of chloride channels, specifically targeting the CIC-7 channel in osteocytes. This compound effectively blocks osteoclast acidification and resorption in vitro, exhibiting an IC50 of 30 μM. In preclinical studies using a rat model of ovariectomy-induced osteoporosis, NS3736 has demonstrated the ability to enhance bone strength and increase bone density, making it a valuable tool for researching osteoporosis. -
BK/ClC-2 Chloride Channels Activator
Unoprostone is an activator of BK (large conductance Ca2+-activated K+) channels and ClC-2 chloride channels. This compound has demonstrated the ability to protect retinal cells from oxidative stress and light-induced damage, while also improving phagocytic function. Additionally, Unoprostone effectively reduces intraocular pressure, making it a valuable tool for research into glaucoma, ocular hypertension, and retinitis pigmentosa. -
Anxiolytic Agent
BTG 1640 is a potent anxiolytic agent classified as an isoxazoline. It selectively inhibits GABA- and glutamate-gated chloride channels, contributing to its anxiolytic effects. This compound is of significant interest in neuropharmacological research for studying anxiety disorders and their treatment mechanisms. -
GABAA Receptor Chloride channel Inhibitor
Leptophos oxon is a potent GABAA receptor chloride channel inhibitor, exhibiting an IC50 value of 89.6 μM. This compound effectively inhibits GABA-induced chloride influx through binding to the TBPS sites associated with GABAA receptors, as well as inhibiting TBPS binding to voltage-dependent chloride channels. Leptophos oxon is primarily utilized in studies related to neurological diseases and functions as an insecticide, making it relevant for research in both neurobiology and pest management. -
Chloride Channel Inhibitor
NS5818 is a potent chloride channel inhibitor that effectively disrupts acidification and bone resorption processes. Its mechanism of action makes it a valuable tool for studying osteoporosis and associated bone metabolic disorders. Researchers can utilize NS5818 to gain insights into chloride channel functions and their implications in bone health. -
Chloride Channel Inhibitor
Alilusem potassium is a selective chloride channel inhibitor known for its diuretic properties. Studies have demonstrated its effectiveness in reducing free water clearance while enhancing sodium and chloride excretion in urine during water diuresis in anesthetized canine models. Additionally, Alilusem potassium, when administered with Furosemide or Hydrochlorothiazide, further diminished free water clearance. This compound has also been shown to inhibit lumen-positive transepithelial voltage and chloride flux across isolated rabbit cortical thick ascending limbs of Henle, making it a valuable tool for research in renal physiology and electrolyte transport mechanisms. -
Stable Isotope
Niflumic Acid-d5 is a deuterium-labeled derivative of Niflumic acid, which acts primarily as a calcium-activated chloride channel blocker. This compound exhibits significant analgesic and anti-inflammatory properties, making it useful in the management of conditions such as rheumatoid arthritis. Its stable isotope form is valuable for research applications in pharmacokinetics, metabolic studies, and mechanistic investigations of calcium channel modulation. -
CRM1 Degrader
CRM1 Degrader 1 is a targeted agent that selectively degrades chromosome region maintenance 1 (CRM1), a nuclear exporter critical for the transport of various tumor suppressor proteins. By inducing apoptosis in gastric carcinoma cells, CRM1 Degrader 1 demonstrates significant anti-proliferative effects, making it a valuable tool for cancer research. This compound is primarily used to explore therapeutic strategies aimed at regulating CRM1-related pathways in cancer biology. -
EAAT Inhibitor
DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters (EAATs), specifically targeting EAAT1, EAAT2, and EAAT3 with IC50 values of 70 μM, 6 μM, and 6 μM, respectively. This compound effectively inhibits the uptake of [14C]glutamate in COS-1 cells expressing human EAAT1 and EAAT2, demonstrating Ki values of 42 μM and 5.7 μM, respectively. Additionally, DL-TBOA competitively blocks EAAT4 and EAAT5 with Ki values of 4.4 μM and 3.2 μM, respectively. This reagent is valuable for studying excitatory neurotransmission and related pathologies in research applications. -
GLT-1/EAAT2 Activator
LDN-212320 is a potent activator of the glutamate transporter GLT-1 (EAAT2), primarily functioning at the translational level. This compound is known to mitigate nociceptive pain by enhancing astroglial GLT-1 expression in both the hippocampus and anterior cingulate cortex. LDN-212320 is valuable in research focused on pain modulation and neuroprotection, offering insights into the role of glutamate transporters in neurological conditions. -
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. -
EAAT2 PAM
NA-014 is a selective positive allosteric modulator (PAM) of the excitatory amino acid transporter 2 (EAAT2), exhibiting an EC50 of 3 nM. This compound enhances the transport activity of EAAT2, which is crucial for regulating glutamate levels in the synaptic cleft. NA-014 is valuable for research into neurodegenerative diseases and synaptic dysfunction, providing insights into therapeutic strategies that target glutamate homeostasis. -
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. -
EAAT Modulator
Nε-(Carboxyethyl)lysine is a known modulator of excitatory amino acid transporters (EAATs). As an advanced glycation end product (AGE), it facilitates protein cross-linking, leading to alterations in protein structure and function, ultimately resulting in protein denaturation. Nε-(Carboxyethyl)lysine interacts with RAGE receptors, influencing cell signaling pathways critical for inflammatory response, cell proliferation, and apoptosis. Additionally, it affects glutamate transporter activity, reducing glutamate uptake and S100B protein secretion, thereby impacting neurotransmission and demonstrating neurotoxic effects associated with diabetes. -
EAAT2 Activator
EAAT2 Activator 1 is a potent activator of the excitatory amino acid transporter 2 (EAAT2), a critical protein responsible for the clearance of glutamate from synaptic clefts. This compound enhances EAAT2 protein levels in a dose-dependent manner, promoting efficient glutamate uptake. EAAT2 Activator 1 is relevant for research applications aimed at understanding glutamatergic signaling and neuroprotection in various neurological disorders. -
EAAT2 Modulator
(R)-AS-1 is a selective positive allosteric modulator of the excitatory amino acid transporter 2 (EAAT2), exhibiting an EC50 of 11 nM. This compound enhances spontaneous locomotor activity in murine models at doses of 60 and 90 mg/kg. Additionally, (R)-AS-1 demonstrates significant anticonvulsant effects in various seizure models, with ED50 values of 66.3 mg/kg for maximal electroshock, 36.3 mg/kg for pentylenetetrazole, and 41.6 mg/kg for electrical stimuli. This agent is valuable for research in neurological disorders. -
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 Blocker
(±)-HIP-B is a non-competitive blocker of excitatory amino acid transporters (EAATs), demonstrating effective inhibition of glutamate uptake with an IC50 of 17-18 μM. This compound serves as a valuable lead in research focused on ischemia-induced neuronal degeneration. Its application extends to the investigation of various neurological disorders, contributing to a deeper understanding of excitotoxicity and neuronal survival mechanisms. -
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. -
EAAT2 Positive Allosteric Modulator, neurological disease
DA-023 is a selective positive allosteric modulator of the excitatory amino acid transporter 2 (EAAT2) with an EC50 value of 1 nM. This compound enhances EAAT2 activity, which is crucial for glutamate regulation in the central nervous system. DA-023 is particularly relevant for research into neurological diseases, offering potential insights into therapeutic strategies for conditions associated with glutamate dysregulation. -
EAAT Blocker
(±)-HIP-A is a non-competitive blocker of excitatory amino acid transporters (EAATs) that inhibits glutamate uptake with an IC50 value of 17-18 μM. This compound serves as a lead candidate for research into ischemia-induced neuronal degeneration. (±)-HIP-A is particularly valuable for studying the pathophysiology of neurological diseases and the mechanisms underlying excitotoxicity. -
GABAA Receptor Antagonist
Bicuculline (methochloride) is a selective antagonist of the GABAA receptor, exhibiting an IC50 value of 3 μM. This compound is known to induce clonic-tonic convulsions in mammals and is also capable of blocking Ca2+-activated potassium channels. Bicuculline (methochloride) is utilized in research focused on epilepsy and related psychiatric disorders, providing valuable insights into neuronal excitability and inhibitory transmission. -
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. -
Potassium Channel Opener
Flupirtine is a non-opioid analgesic that acts primarily as a potassium channel opener, specifically targeting Kv7 channels. This compound exhibits notable neuroprotective properties by stabilizing blood-brain barrier integrity, reducing oxidative stress, and counteracting focal cerebral ischemia. Flupirtine is utilized in research related to pain management, Alzheimer's disease, multiple sclerosis, and neuroprotection due to its ability to lessen neuronal excitotoxicity and maintain resting membrane potential without exhibiting antipyretic or antiphlogistic effects. -
ATPase
Creatine phosphokinase, Rabbit muscle (CPK) is an enzyme that catalyzes the reversible conversion of creatine and ATP into phosphocreatine and ADP. By facilitating the maintenance of an optimal ATP/ADP ratio, CPK plays a critical role in energy metabolism, particularly during periods of high energy demand. This enzyme is widely used in biochemical research to study cellular energy dynamics and various metabolic disorders. -
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 Blocker
CAY10568 is a sodium channel blocker that modulates neuronal excitability. This compound, a derivative of QX-314, exhibits a smaller and less hydrophobic profile, making it suitable for exploring its effects on inflammation and pain perception. CAY10568 is valuable for research applications aimed at understanding pain mechanisms and developing analgesic therapies. -
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. -
NaV1.7 Antagonist
AMG8379 is a selective sulfonamide antagonist targeting the voltage-gated sodium channel NaV1.7. It demonstrates potent inhibition with IC50 values of 8.5 nM for human NaV1.7 and 18.6 nM for mouse NaV1.7, effectively blocking TTX-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM. This compound is useful for research applications related to pain pathways and sodium channel modulation. -
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. -
Nav1.7 Blocker
NAV 26 is a selective blocker of the voltage-gated sodium channel Nav1.7, exhibiting an IC50 of 0.37 μM. This compound is valuable for investigating pain mechanisms and developing novel analgesics. Its specificity for Nav1.7 makes it a crucial tool in researching pain pathways and potential therapeutic interventions. -
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 Antagonist
AMG8380 is a selective antagonist of the voltage-gated sodium channel NaV1.7, exhibiting IC50 values of 0.907 µM and 0.387 µM in human and mouse tissues, respectively. This compound effectively inhibits Tetrodotoxin (TTX)-sensitive native channels with an IC50 of 2560 nM, making it a valuable tool for research on pain pathways and sodium channel function. Its properties allow for exploration of NaV1.7's role in nociception and related applications in pharmacological studies. -
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 Antagonist
Nav1.7-IN-15 is a potent state-dependent antagonist of the sodium channel Nav1.7, exhibiting an IC50 of 0.42 μM for human Nav1.7 PX. This compound is valuable for studying pain mechanisms and is useful in research focusing on neuropathic pain and other conditions associated with Nav1.7 activity. Its ability to selectively inhibit Nav1.7 makes it an important tool for investigating the therapeutic potential of sodium channel modulation. -
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. -
Sodium Channel Blocker
BW-4030W92 is a selective sodium channel blocker that inhibits sodium ion influx. This compound is utilized in research to study the role of sodium channels in neuronal excitability and can induce ataxia, providing insights into neurological disorders. Its application is significant in pharmacological studies aiming to investigate the mechanisms of action of sodium channel modulation. -
NaV Modulator
Clathrodin is a marine alkaloid derived from Agelas sponges that functions as a modulator of voltage-gated sodium (NaV) channels. As a sodium channel neurotoxin, Clathrodin impacts sodium channel ionic conductance, making it a valuable tool for studying excitability in neurons and muscle cells. This reagent is useful in research applications involving neuropathic pain, neurotoxicity assessments, and the physiological characterization of sodium channel function. -
Sodium Channel Blocker
Olisutrigine bromide is a potent sodium channel blocker that exhibits significant analgesic properties. This compound is primarily utilized in research focused on pain modulation and the investigation of sodium channel dynamics in neurological disorders. Its efficacy in inhibiting sodium influx makes it a valuable tool for exploring therapeutic interventions in pain management. -
Sodium Channel
Tolperisone is a centrally acting muscle relaxant that primarily targets sodium channels, leading to neuronal inhibition. It is effective in alleviating symptoms of spasticity and muscle spasms, making it a valuable tool in neuromuscular research and therapeutic studies. Tolperisone's mechanism of action extends its application in exploring muscle relaxation pathways and their implications in various neurological conditions.
