Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Insecticide
Leporin A is an insecticide that primarily targets GABA receptors and sodium channels, disrupting neurotransmission in insects. This mechanism leads to paralysis and mortality, making Leporin A a potent agent for agricultural pest control. It is utilized in research focused on insect physiology and pest management strategies. -
Potassium Channel Opener
Flupirtine hydrochloride is a potassium channel opener (Kv7 activator) recognized for its analgesic and neuroprotective properties. This compound acts as a non-opioid analgesic while also antagonizing NMDA receptors and activating GABA receptors. Flupirtine hydrochloride enhances neuronal stability by reducing oxidative stress and calcium influx, thereby protecting neurons from excitotoxicity and ischemia. It is applicable in research focused on conditions such as focal cerebral ischemia, pain management, Alzheimer’s disease, and multiple sclerosis. -
GABAA Receptor Antagonist
Bicuculline methobromide 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 mammalian models, making it a valuable tool for investigating epilepsy and associated neurological disorders. Additionally, bicuculline methobromide functions as a blocker of Ca2+-activated potassium channels, further expanding its utility in pharmacological research focused on ion channel dynamics and excitability in neuronal systems. -
Stable Isotope
Flupirtine-d4 hydrochloride is a deuterium-labeled variant of Flupirtine hydrochloride, a non-opioid analgesic that crosses the blood-brain barrier. This compound functions primarily as a neuronal potassium channel opener (Kv7 activator) and exhibits properties as an NMDA receptor antagonist and GABA receptor activator. It is utilized in research focused on pain management, neuroprotection, and conditions such as Alzheimer’s disease and multiple sclerosis, offering insights into pathways of ischemic neuron death, oxidative stress modulation, and the maintenance of blood-brain barrier integrity. Flupirtine-d4 hydrochloride serves as a valuable tool for studying the underlying mechanisms and therapeutic approaches for neurological disorders. -
Insecticide
Insecticidal agent 21 is a potent insecticide primarily targeting Culex pipiens larvae with an LC50 of 0.4 μg/mL. This compound exerts multi-target neurotoxicity by inhibiting acetylcholinesterase (AChE) and affecting multiple neural receptors, including nicotinic acetylcholine receptors (nAChR), voltage-gated sodium channels (VGSC), and γ-aminobutyric acid receptors (GABAAR). Insecticidal agent 21 demonstrates a strong insecticidal effect and is suitable for research applications focused on developing novel insecticides to combat resistance in mosquito populations. -
HCN Channel Blocker
Cilobradine hydrochloride is a selective blocker of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels. It has been shown to modulate cardiac pacemaker currents, resulting in significant alterations in heart rhythm. Additionally, cilobradine exhibits antidepressant properties, making it relevant for research in cardiovascular physiology and mood disorder therapies. -
HCN1 Inhibitor
RO-275 is a potent and selective HCN1 inhibitor, demonstrating IC50 values of 0.046 µM for HCN1, while showing significantly lower activity against HCN2 (14.3 µM), HCN3 (4.6 µM), and HCN4 (13.9 µM). This compound has been shown to effectively rescue impaired working memory, highlighting its potential utility in researching cognitive dysfunction associated with various brain disorders. RO-275 serves as a valuable tool for investigations into HCN1-related pathways and their implications in neurobiology. -
HCN2 Inhibitor
HCN2-IN-3 is an orally active inhibitor of HCN2 ion channels. It effectively reduces the activity of HCN2, making it valuable for research into pain mechanisms, tinnitus, and various central nervous system disorders. Additionally, HCN2-IN-3 has potential applications in studies focusing on mental illnesses and mood-related conditions. -
HCN2 Inhibitor
HCN2-IN-6 is a selective inhibitor of the HCN2 ion channel, demonstrating an IC50 value of 7 nM. It exhibits minimal inhibition of HCN4, making it a valuable tool for studying HCN2-specific pathways. This reagent is suitable for research into inflammatory diseases and neurological disorders, facilitating the exploration of potential therapeutic strategies targeting these conditions. -
HCN Inhibitor
pan-HCN-IN-1 is a potent inhibitor of the hyperpolarization-activated and cyclic-nucleotide-gated 1 (HCN1) ion channel, exhibiting an IC50 value of 58 nM. This compound effectively attenuates the voltage sag response and enhances excitatory postsynaptic potential (EPSP) summation in ex vivo rat brain slices. It serves as a valuable tool for investigating the role of HCN1 channels in neuronal excitability and synaptic integration in various research applications. -
HCN Channel Blocker
Ivabradine is a potent HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that selectively inhibits the cardiac pacemaker current (If). This compound effectively reduces heart rate in a dose-dependent manner without affecting blood pressure. In addition to its use in cardiovascular research, Ivabradine exhibits anticonvulsant, anti-ischemic, and anti-anginal properties, making it valuable for diverse biological investigations. -
HCN Channel Inhibitor
MS7710 is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels. It effectively reduces HCN channel-mediated Ih current, leading to decreased firing frequency and burst activity in dopaminergic neurons within the ventral tegmental area. Research has demonstrated that MS7710 ameliorates deficits in social interaction and cognitive flexibility related to reward processing in mice subjected to chronic social defeat stress. This compound is valuable for studies focusing on major depressive disorder and its underlying mechanisms. -
Kv1.3/Kv1.4 Blocker
CP 339818 hydrochloride is a selective blocker of Kv1.3 and Kv1.4 ion channels, with an IC50 of 200 nM for Kv1.3. This compound also inhibits HCN channels, displaying IC50 values of 18.9 μM and 43.4 μM for HCN1 and HCN4, respectively, while having minimal effect on other Kv channels such as Kv1.1 and Kv1.2. By selectively targeting Kv1.3, CP 339818 hydrochloride attenuates the activation of human T cells, making it a valuable tool for investigating the physiological roles of HCN and Kv channels in cellular processes. -
HCN Channel Antagonist
VUANT1 (VU0183254) is an allosteric antagonist targeting HCN channels, specifically inhibiting insect odorant receptor ion channels. This compound effectively disrupts insect odorant receptor signaling through allosteric modulation, providing insights into the molecular mechanisms underlying insect olfactory processes. While its application in pest control may be limited, VUANT1 serves as a valuable pharmacological tool for researchers exploring olfactory signaling pathways in insects. -
HCN/Potassium Channels Blocker
KIO-301 chloride is a photoswitch compound that selectively blocks hyperpolarisation-activated cyclic nucleotide-gated (HCN) channels and voltage-gated potassium channels upon exposure to visible light. This compound can be employed in research to investigate the role of these ion channels in cellular excitability and signaling pathways. Its unique mechanism offers insights into ion channel modulation and potential therapeutic applications in neurobiology and cardiac research. -
HCN2 Inhibitor
HCN2-IN-4 is an orally active inhibitor of the HCN2 ion channel, which plays a crucial role in neuronal excitability and rhythmic activity. This compound effectively inhibits HCN2 channel activity, making it a valuable tool for investigating its involvement in pain mechanisms, tinnitus, and various central nervous system disorders. Researchers may utilize HCN2-IN-4 to explore therapeutic strategies targeting these conditions. -
HCN2 Inhibitor
HCN2-IN-2 is a selective inhibitor of the HCN2 ion channel, characterized by an IC50 of 145 nM. This azaindazole derivative effectively blocks HCN2 channel activity, preventing abnormal firing in peripheral nociceptive neurons. HCN2-IN-2 is suited for research applications focused on pain modulation and the underlying mechanisms of nociceptive signaling. -
HCN Channel Blocker
Ivabradine sulfate is a potent HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker, primarily functioning to inhibit the cardiac pacemaker current (If). This compound effectively reduces heart rate in a dose-dependent manner while maintaining stable blood pressure levels. Ivabradine sulfate also exhibits notable biological activity, including anticonvulsant, anti-ischemic, and anti-anginal effects, making it a valuable reagent for cardiovascular and neurological research applications. -
HCN2 Inhibitor
HCN2-IN-1 is a potent HCN2 inhibitor with an IC50 of 98 nM. This compound selectively targets hyperpolarization-activated cyclic nucleotide-gated channels, making it a valuable tool for investigating central nervous system (CNS) and psychiatric disorders. HCN2-IN-1 can facilitate research into the mechanisms underlying neuronal excitability and potential therapeutic strategies for related conditions. -
HCN2 Inhibitor
HCN2 modulator-6 is a potent inhibitor of the HCN2 ion channel, exhibiting an IC50 of 7 nM. This compound effectively suppresses HCN2 channel activity, making it a valuable tool for investigating mechanisms underlying pain, including inflammatory and neuropathic pain. Additionally, HCN2 modulator-6 is applicable in research focused on tinnitus, central nervous system disorders, psychiatric conditions, and mood disorders. -
HCN Channel Blocker
KIO-301 is a photoswitchable blocker of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels. This compound serves as a versatile tool for research in retinal diseases, specifically targeting the reactivation of HCN channels in models of retinitis pigmentosa. Its ability to be controlled by light makes it particularly useful for studies requiring precise spatiotemporal modulation of channel activity. -
HCN2 Inhibitor
HCN2-IN-5 is a potent HCN2 ion channel inhibitor with an IC50 of 9 nM, exhibiting minimal inhibitory activity on HCN4. This compound is valuable in the study of inflammatory diseases and neurological disorders, providing insights into the modulation of ion channel activity. Its specificity and potency make it a useful tool for elucidating the role of HCN2 in various physiological and pathological processes. -
Kv1.3/Kv1.4 Channel Blocker
CP-339818 is a selective blocker of the Kv1.3 and Kv1.4 potassium channels, exhibiting an IC50 of 200 nM for Kv1.3. This compound also inhibits HCN channels, with IC50 values of 18.9 μM and 43.4 μM for HCN1 and HCN4, respectively, while demonstrating minimal effects on other Kv channels, such as Kv1.1 and Kv1.2. CP-339818 is valuable for investigating the role of Kv1.3 in T cell activation and the physiological functions of HCN and Kv channels in cellular contexts. -
AMPA Receptor Agonist
(S)-AMPA is a selective agonist of the AMPA receptor, primarily involved in excitatory neurotransmission. This S-enantiomer of AMPA exhibits high potency, making it an essential tool for studying synaptic transmission and plasticity in the nervous system. Its applications include understanding the mechanisms of synaptic function and investigating potential therapeutic strategies for neurological disorders. -
AMPA Receptor Antagonist
NBQX disodium is a potent and selective competitive antagonist of the AMPA receptor. It exhibits neuroprotective properties and demonstrates anticonvulsant activity, making it valuable for research into neurological disorders and seizure models. This compound is instrumental in studies aimed at understanding glutamate receptor-mediated signaling pathways and their implications in neurodegenerative diseases. -
AMPA Modulator
IDRA 21 is a positive allosteric modulator of the AMPA receptor, specifically enhancing signaling through GluR1/2 subtypes. This compound promotes excitatory neurotransmission, making it a valuable tool in the investigation of cognitive and memory disorders, including age-related decline. Its properties establish IDRA 21 as a promising candidate for research focusing on synaptic plasticity and cognitive enhancement. -
AMPA Potentiator
Pesampator (PF-04958242) is a selective positive allosteric modulator of the AMPA receptor, enhancing glutamatergic neurotransmission. With an EC50 of 310 nM and a Ki of 170 nM, it potentiates AMPA receptor activity, making it a valuable tool for research in neuropharmacology and cognitive enhancement studies. It can be utilized to investigate the mechanisms underlying synaptic plasticity and the potential therapeutic effects on neurological disorders. -
AMPAR PAM
CX 717 is a positive allosteric modulator of the AMPA receptor, enhancing synaptic transmission and activity. It exhibits antidepressant-like effects, making it a valuable tool in the investigation of mood disorders. Additionally, CX 717 is relevant for research into adult attention deficit hyperactivity disorder (ADHD), providing insights into neurotransmission and behavioral modulation. -
AMPA Receptor Modulator
CX614 is a positive allosteric modulator of AMPA receptors that enhances excitatory postsynaptic potentials by inhibiting and prolonging the inactivation of glutamate responses. This compound can evoke excitatory postsynaptic currents in neuronal cultures, making it particularly useful in the investigation of neurophysiological processes. CX614 has potential applications in the study of psychiatric disorders, including depression. -
AMPA receptor Modulator
JNJ-55511118 is a selective modulator of AMPA receptors, specifically targeting TARP γ-8, with an inhibition constant (Ki) of 26 nM. This compound demonstrates significant biological activity by reducing voluntary intake of sweetened alcohol in male murine models. In addition, it disrupts hippocampal neurotransmission, alters specific electroencephalogram frequency bands, induces transient hyperlocomotion, and impairs cognitive functions such as learning and memory, while also exhibiting anticonvulsant properties. JNJ-55511118 is valuable for research focused on alcohol use disorders and seizure mechanisms. -
AMPA-R Potentiator
HBT1 is a selective AMPA receptor (AMPAR) potentiator that enhances receptor activity in the presence of AMPA by binding to its ligand-binding domain. Unlike traditional AMPA-R potentiators, HBT1 exhibits a limited agonistic effect, minimizing the risk of bell-shaped dose-response curves related to brain-derived neurotrophic factor (BDNF) production. This unique profile allows for broader research applications in neurological and psychiatric disorders, including depression and Alzheimer’s disease. -
AMPAR Inhibitor
TAT-GluA2 3Y is an AMPAR inhibitor that interferes with the endocytosis of AMPA receptors, thereby blocking long-term depression (LTD) at glutamatergic synapses. This peptide has been shown to mitigate pentobarbital-induced spatial memory deficits, highlighting its potential in studying synaptic plasticity and memory-related research applications. TAT-GluA2 3Y serves as a valuable tool for exploring the mechanisms underlying synaptic transmission and cognitive function. -
AMPAR Enhancer
CX1739 is an AMPA-glutamate receptor (AMPAR) enhancer that significantly enhances long-term potentiation in a dose-dependent manner in mouse models. This compound effectively mitigates amphetamine-induced locomotor activity and rapidly reverses opioid-induced respiratory depression. Research applications for CX1739 include studies related to dementia, neuropsychiatric disorders, and complications arising from opiate-induced suppression of endogenous inspiratory breathing rhythms. -
AQP2/CFTR Inhibitor
Steviol is a selective inhibitor of the aquaporin-2 (AQP2) and cystic fibrosis transmembrane conductance regulator (CFTR) proteins. This compound impedes renal cyst growth by inhibiting CFTR activity, which leads to decreased AQP2 expression and promotes the degradation of both AQP2 and CFTR. Steviol is relevant for research focused on polycystic kidney disease and mechanisms underlying renal cyst development. -
EHD4 ATPase Inhibitor
ATPase-IN-4 is a selective inhibitor of EHD4 ATPase activity, with an IC50 value of 0.92 μM. This compound also exhibits inhibitory effects on the ATPase activity of EHD2. ATPase-IN-4 is valuable for research applications focused on understanding the role of EHD proteins in cellular processes and membrane trafficking. -
ATPase Inhibitor
ATPase-IN-2 is a potent ATPase inhibitor with an IC50 value of 0.9 μM. It effectively inhibits the glycohydrolase activity of Clostridium difficile toxin B (TcdB) with an AC50 value of 30.91 μM. This compound serves as a valuable tool for studying ATP-related mechanisms and elucidating the role of ATPases in various biological processes.
