Catalog No.
Product Name
Application
Product Information
Citations
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GABA Aminotransferase Inhibitor
Gabaculine is a potent inhibitor of GABA aminotransferase, an enzyme responsible for the degradation of gamma-aminobutyric acid (GABA). This compound, derived from the microbial strain Streptomyces toyocaensis, effectively increases GABA levels, thereby modulating neurotransmission and exhibiting potential anxiolytic effects. Gabaculine is widely utilized in neurobiological research to study neurotransmitter dynamics and the role of GABA in various neurological disorders. -
GABAA Receptor Partial Agonist
ELB-139 is a GABAA receptor partial agonist known for its anxiolytic and anticonvulsant properties. This progesterone analogue modulates GABAA receptor activity, demonstrating significant effects on neurotransmitter levels, particularly enhancing extracellular serotonin (5-HT) in the striatum and medial prefrontal cortex of rodent models. ELB-139 holds potential for research applications related to anxiety disorders and seizure disorders. -
GABA Receptor
Epi-Aszonalenin A is a benzodiazepine fungal metabolite that targets the GABA receptor. It exhibits psychoactive properties, making it a valuable compound for studying the modulation of neurotransmission and its effects on behavior. This compound has potential applications in neuroscientific research related to anxiety, sedation, and other disorders associated with GABAergic signaling. -
GABA Receptor
Carburazepam is a benzodiazepine derivative that targets GABA receptors, enhancing the inhibitory neurotransmitter's effects within the central nervous system. Its primary biological activity includes anxiolytic and sedative properties, making it useful in research related to anxiety disorders and sleep disturbances. As a research reagent, Carburazepam provides valuable insight into the pharmacological mechanisms of benzodiazepines and their impact on neuronal signaling pathways. -
GABA Receptor
Suclofenide is an anticonvulsant compound that modulates GABA receptor activity, influencing GABA metabolism. It exhibits potential neuroprotective effects and has been utilized in research related to epilepsy and seizure disorders. Suclofenide serves as a valuable tool for investigating GABAergic signaling and its implications in various neurological conditions. -
GABA Receptor
CGP11952 is a triazolyl-benzophenone that acts as a positive allosteric modulator of the GABA receptor. This compound exhibits characteristics similar to benzodiazepines, contributing to its pharmacological profile. CGP11952 is primarily utilized in research to investigate GABAergic signaling and its implications in neurological disorders. -
GABA Receptor Agonist
Ro 41-3290 is a selective GABA receptor agonist, acting primarily as a partial agonist at the benzodiazepine site. This compound demonstrates potent biological activity in modulating GABAergic neurotransmission, making it valuable for research in the fields of neuropharmacology and anxiety disorders. Its mechanisms may provide insights into therapeutic approaches for conditions such as anxiety, insomnia, and seizure disorders. -
GABA Receptor Agonist
FG8119 is a novel benzodiazepine agonist that targets GABA receptors, enhancing their activity. This compound demonstrates significant anxiolytic and sedative effects, making it valuable for research in neuropharmacology and the study of anxiety disorders. FG8119 can be utilized to investigate the modulation of GABAergic neurotransmission and its implications in various neurological conditions. -
Glycine/NMDA Receptor Antagonist
ZD 9379 sodium acts as a competitive antagonist at the glycine-binding site of the NMDA receptor, exhibiting an IC50 value of 75 nM for the glutamate site. This compound inhibits glycine binding, mitigating excitotoxicity and demonstrating therapeutic potential in conditions such as acute ischemic stroke. ZD 9379 sodium reduces the frequency of cortical spreading depression, decreases infarct volume, and enhances neurological function in preclinical mouse models, making it a valuable tool for research in neuroprotection and stroke mechanisms. -
Positive Allosteric Modulator Of GluN1/GluN3 NMDA Receptors
UCM-A86 is a selective positive allosteric modulator of the GluN1/GluN3 NMDA receptors, exhibiting EC50 values of 21 µM and 19 µM for GluN1/GluN3A and GluN1/GluN3B receptors, respectively. This compound preferentially enhances signaling through GluN1/GluN3A/B receptors while displaying minimal activity at GluN1/GluN2A-D receptors. UCM-A86 serves as a valuable tool for research focused on central nervous system disorders and the modulation of NMDA receptor activity. -
NMDA Receptor Antagonist
Dizocilpine is a potent, non-competitive antagonist of the NMDA receptor, characterized by a Kd of 37.2 nM in rat brain membranes. By binding to a specific site within the NMDA-associated ion channel, it effectively inhibits calcium ion (Ca2+) influx. This compound is widely used in research focused on epilepsy, neurotoxicity, and neurodegenerative diseases, making it a valuable tool for studying excitotoxicity and synaptic function. -
NMDA Receptor Antagonist
Cycloleucine is a selective NMDA receptor antagonist that targets the glycine site, exhibiting a Ki value of 600 μM. This compound inhibits S-adenosyl-methionine-mediated methylation and acts as a competitive inhibitor of ATP: L-methionine-S-adenosyl transferase in vitro. Cycloleucine demonstrates anxiolytic and cytostatic properties, making it a valuable tool for research in neurobiology and cancer studies. Its unique mechanism of action provides insights into the underlying pathways of excitotoxicity and cellular regulation. -
NMDA Receptor Antagonist
5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine binding site on the NMDA receptor, exhibiting a KB value of 65 nM. This compound effectively reduces NMDA-induced neuronal injury and enhances social interaction and exploration behaviors in rodent models. Additionally, 5,7-DCKA demonstrates anxiolytic-like effects, facilitating research into the role of glycine in NMDA receptor-mediated synaptic activity and associated psychiatric disorders. -
NMDAR Agonist
N,N-Dimethylglycine is a natural N-methylated glycine that serves as a partial agonist at the N-methyl-D-aspartate receptor (NMDAR) glycine site. It functions as a methyl donor, enhancing immune response and exhibiting antioxidant properties to mitigate oxidative stress by scavenging free radicals. Additionally, N,N-Dimethylglycine has demonstrated antidepressant-like effects and surfactant activity, making it valuable for various research applications in neuropharmacology and immunology. -
NMDA Antagonist
Orphenadrine is a skeletal muscle relaxant that acts as an NMDA antagonist, primarily inhibiting the binding of [3H]MK-801 to the PCP binding site of the NMDA receptor. This compound exhibits a range of biological activities including antiparkinsonian, antihistaminic, antitremor, antispasmodic, and analgesic effects. Additionally, Orphenadrine has been shown to induce oxidative stress through CAR nuclear translocation and may have implications in pro-tumor activities. It also demonstrates neuroprotective properties by safeguarding rat cerebellar granule cells from 3-NPA-induced cytotoxicity, suggesting potential therapeutic applications in neurodegenerative diseases associated with NMDA receptor overactivation. -
FLNA Modulator
Simufilam hydrochloride is an orally active modulator of filamin A (FLNA) that targets neuronal signaling pathways. This compound restores NMDAR signaling and Arc expression while inhibiting dysregulated mTOR activity. Additionally, it enhances insulin sensitivity and mitigates Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam hydrochloride is applicable in research related to Alzheimer's disease, particularly in understanding the underlying mechanisms of neurodegeneration. -
Gly/NMDA Receptor Antagonist
CGP 78608 hydrochloride is a highly potent and selective antagonist at the glycine-binding site of the NMDA receptor, exhibiting an IC50 of 6 nM. This compound acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC50 in the low nM range (26.3 nM). CGP 78608 hydrochloride is primarily employed in research investigating its anticonvulsant activity and the modulation of excitatory neurotransmission. -
NMDA Receptor Agonist
L-Homocysteic acid is an endogenous excitatory amino acid functioning as a NMDA receptor agonist, with an effective concentration (EC50) of 14 μM. Its neurotoxic properties make it a valuable tool in the investigation of neurological disorders. L-Homocysteic acid enables researchers to explore the roles of excitatory neurotransmission and contribute to the understanding of related pathophysiological conditions. -
NMDA Receptor PAM
Plazinemdor is a positive allosteric modulator of the N-methyl-D-aspartate (NMDA) receptor. This compound enhances NMDA receptor activity, making it a valuable tool for investigating its role in psychiatric, neurological, and neurodevelopmental disorders. Plazinemdor is suitable for research applications focused on understanding the underlying mechanisms of various nervous system diseases. -
NMDA Antagonist
Fluoroethylnormemantine is an N-methyl-D-aspartate (NMDA) receptor antagonist, serving as a derivative of Memantine. This compound showcases neuroprotective, anti-amnesic, and antidepressant-like properties, making it valuable in neurological research. Additionally, [18F]-Fluoroethylnormemantine is utilized as a positron emission tomography (PET) tracer, enhancing imaging studies related to NMDA receptor activity and its implications in various mental health disorders. -
NMDA Receptor Inhibitor
Pregnanolone sulfate (pyridinium) is an endogenous neurosteroid that functions as an inhibitor of NMDA receptors. This compound exhibits neuroprotective properties, making it a valuable tool for investigating neurodegenerative disorders and synaptic plasticity. Its ability to modulate excitatory neurotransmission highlights its potential applications in both basic research and therapeutic development. -
NMDA Receptor Modulator
Rapastinel Trifluoroacetate is a modulator of the NMDA receptor, functioning as a partial agonist at the glycine site. This compound has shown potential for the treatment of major depressive disorder, contributing to neuroplasticity and synaptic function. It is utilized in research exploring depression and related neurological conditions, providing insights into the therapeutic effects of NMDA receptor modulation. -
NMDA Agonist
Cis-Piperidine-2,3-dicarboxylic acid primarily targets NMDA receptors and acts as a partial agonist. This compound is known for its ability to block general excitatory synaptic transmission by interfering with NMDA, AMPA, and kainate ionotropic receptors. Cis-Piperidine-2,3-dicarboxylic acid is valuable for research applications related to neuropharmacology and the study of synaptic plasticity. -
NMDAR Allosteric Modulator
GNE-9278 is a selective positive allosteric modulator of the N-methyl-D-aspartate receptor (NMDAR), targeting the GluN1 transmembrane domain. It enhances peak current and agonist affinity in activated NMDARs, offering potential insights into synaptic transmission and plasticity. This compound is valuable for research investigating NMDAR-related neurological disorders and synaptic function. -
NMDA Receptor Partial Agonist
Zelquistinel (AGN-241751) is a potent orally active partial agonist of the N-methyl-D-aspartate (NMDA) receptor. It has demonstrated significant biological activity relevant to the research of neuropsychiatric conditions, including depression and anxiety. Zelquistinel serves as a valuable tool for studying the pharmacological mechanisms underlying these disorders and evaluating potential therapeutic interventions. -
GluN2B-NMDAR Antagonist
GluN2B-NMDAR antagonist-1 is an orally active antagonist of the GluN2B subtype of the N-methyl-D-aspartate receptor (NMDAR). This compound exhibits neuroprotective properties, making it a valuable tool in studying ischemic injury and related neurodegenerative conditions. It is primarily used in research to explore mechanisms of neuronal damage and potential therapeutic interventions. -
FLNA Modulator
Simufilam is an orally active modulator of filamin A (FLNA) that restores NMDA receptor (NMDAR) signaling and Arc expression. It effectively inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, which results in improved insulin sensitivity and a reduction in Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. This compound is particularly valuable for research applications focused on Alzheimer's disease and related neurodegenerative disorders. -
NMDA Receptor Antagonist
Co 101244 hydrochloride is a selective antagonist of the NMDA receptor, specifically targeting the NR2B subunit. This compound is utilized in research to investigate the role of NMDA receptors in synaptic plasticity, neurodegeneration, and various neurological disorders. Its properties make it a valuable tool for studying excitatory neurotransmission and the mechanisms underlying synaptic function. -
Acetylcholinesterase Inhibitor, Butyrylcholinesterase Inhibitor, Carbonic Anhydrase I/II Inhibitor, α-Glycosidase Inhibitor
Vescalagin is a hexahydroxyphenol that acts as an inhibitor of acetylcholinesterase and butyrylcholinesterase, as well as carbonic anhydrases I and II, and α-glycosidase. It demonstrates potent inhibitory activity with Ki values of 5.87 nM for AChE, 3.89 nM for BChE, 11.75 nM for hCA I, 16.23 nM for hCA II, and 16.08 nM for α-glycosidase. Vescalagin exhibits non-competitive inhibition for hCA I, hCA II, and α-glycosidase, while also reducing hyperglycemia and hypertriglyceridemia in dietary models. Additionally, it possesses anti-inflammatory and antioxidant activities, making it a valuable compound for research in diabetes and metabolic disorders. -
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. -
Stable Isotope
Acetylcholine-d4 chloride is a deuterium-labeled form of the neurotransmitter acetylcholine. It functions as a potent cholinergic agonist and effectively crosses the blood-brain barrier (BBB). This reagent modulates dopaminergic neuronal activity by stimulating nicotinic acetylcholine receptors (nAChRs) and has also been shown to inhibit the aggregation of p53 mutant peptides in vitro. Its unique isotopic labeling makes it a valuable tool for chemical and biological research applications. -
P2X4 Receptor Antagonist
BX430 is a potent noncompetitive allosteric antagonist of the human P2X4 receptor, exhibiting an IC50 value of 0.54 μM. This compound demonstrates selectivity and species specificity, making it a valuable tool for investigating the role of P2X4 receptors in various biological processes. BX430 is primarily utilized in research applications related to chronic pain and cardiovascular diseases, providing insight into therapeutic potential in these areas. -
Stable Isotope
Acetylcholine-d9 chloride is a deuterium-labeled form of acetylcholine chloride, a potent cholinergic agonist that effectively crosses the blood-brain barrier. This compound modulates dopaminergic neuronal activity by stimulating nicotinic acetylcholine receptors (nAChRs). Additionally, it has been shown to inhibit p53 mutant peptide aggregation in vitro, making it valuable for research focused on neurobiology, receptor pharmacology, and protein aggregation studies. -
Neuroprotective Compound
REM127 is a neuroprotective small molecule that modulates calcium homeostasis in cells. It effectively restores calcium balance in cellular models affected by the pathological accumulation of tau protein, demonstrating potential to mitigate synaptic and cognitive deficits in Alzheimer's disease models. REM127 is capable of crossing the blood-brain barrier and may slow the progression of amyloid-beta and tau protein pathologies. This compound is suitable for research applications in neurodegenerative diseases. -
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. -
Calcium Channel
2-Chloro-ATP sodium is an analog of ATP that acts as an antagonist of the purinergic P2Y1 receptor, inhibiting intracellular calcium mobilization induced by ADP in Jurkat cells with a Ki of 2.3 μM. Additionally, it serves as an agonist for the purinergic P2X receptor, generating inward currents in HEK293 cells with varying affinities (EC50 of 0.5 and 2.5 μM). This compound also induces concentration-dependent relaxation of precontracted guinea pig cecal strips. Furthermore, 2-Chloro-ATP sodium is utilized to investigate substrate specificity among cyclic nucleotide-dependent protein kinases, including protein kinase A (PKA) and PKG. -
α7 nAChR Allosteric Modulator
PAM-2 is a selective positive allosteric modulator of the α7 nicotinic acetylcholine receptor (nAChR). Exhibiting potent anti-nociceptive and anti-inflammatory properties, PAM-2 enhances receptor activity, demonstrating efficacy in animal models of neuropathic pain induced by Streptozotocin and Oxaliplatin. It shows selectivity for α7 nAChR over α9α10 nAChR and CaV2.2 channels, making it a valuable tool for research into pain mechanisms and potential therapeutic applications in neuropathic pain. -
Calcium Antagonist
Phenchlobenpyrrone is a selective neuronal calcium antagonist that effectively crosses the blood-brain barrier. This compound demonstrates the capability to mildly inhibit acetylcholinesterase (AChE) activity, along with inhibiting amyloid-beta (Aβ) aggregation and promoting the clearance of Aβ oligomers. Additionally, Phenchlobenpyrrone reduces abnormal phosphorylation of Tau protein. This agent is valuable for research applications focused on Alzheimer's disease and related neurodegenerative conditions. -
α9α10 nAChR/CaV2.2 Antagonist
GeX-2 is a truncated analogue of αO-conotoxin that serves as an antagonist of the α9α10 nicotinic acetylcholine receptor (nAChR) and CaV2.2 channels. This compound demonstrates significant analgesic properties, effectively alleviating pain in rat models exhibiting chronic constriction injury. GeX-2 is valuable in research focusing on pain mechanisms and the modulation of excitatory neurotransmission through its interactions with nAChR and calcium channels. -
CaMKK2 Inhibitor
CaMKK2-IN-1 is a selective inhibitor of calcium/calmodulin-dependent protein kinase kinase 2 (CaMKK2) with an IC50 of 7 nM. This compound displays high ligand efficiency, making it a valuable tool for investigating the role of CaMKK2 in cellular signaling pathways. Its application in research includes studies on metabolism, cancer, and neurological disorders where the modulation of CaMKK2 activity may provide insights into therapeutic interventions. -
CAMKK2 Inhibitor
SGC-CAMKK2-1 is a selective inhibitor of calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2), exhibiting an IC50 of 30 nM. This compound effectively inhibits AMPK phosphorylation in C4-2 cells with an IC50 of 1.6 μM. SGC-CAMKK2-1 serves as a valuable chemical probe for investigating the role of CAMKK2 in various biological processes and pathways related to cellular energy regulation and metabolism. -
AChE/BChE Inhibitor
1,2-Didehydrotanshinone IIA is an inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), demonstrating an IC50 value of 5.98 μM for BChE. Additionally, this compound acts as an indoleamine 2,3-dioxygenase (IDO) inhibitor, with an IC50 value of 4.68 µM. Its dual inhibitory activity positions 1,2-Didehydrotanshinone IIA as a valuable reagent for research into neurodegenerative diseases and immune modulation. -
α-amylase/α-glucosidase/Acetylcholinesterase Inhibitor
Kaempferol-3,7-di-O-β-glucoside is a flavonol that acts as an inhibitor of α-amylase, α-glucosidase, and acetylcholinesterase. This compound has demonstrated protective effects on differentiating neuronal cells, specifically SH-SY5Y, against injury induced by Amyloid β peptide. Its enzyme inhibitory properties and neuroprotective effects indicate potential applications in Alzheimer's disease research and therapeutics. -
AChE/BChE Ligand
Luteolin 5,3'-dimethyl ether is a flavonoid compound that serves as a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). This compound demonstrates significant biological activities, including free radical scavenging and enzyme inhibitory effects. It is particularly useful in research focused on neurodegenerative diseases, diabetes, and disorders related to skin pigmentation. Additionally, it can be isolated from the dried roots of Alhagi maurorum, further emphasizing its natural origin and therapeutic potential. -
α-glucosidase/Acetylcholinesterase Inhibitor
7β-Hydroxybufalin is a bufadienolide that acts as a potent inhibitor of α-glucosidase and acetylcholinesterase. Isolated from the venom of Bufo bufo gargarizans, this compound demonstrates significant biological activity relevant to the modulation of carbohydrate and neurotransmitter metabolism. 7β-Hydroxybufalin is utilized in research applications focused on metabolic disorders and neurodegenerative diseases. -
Insecticide
Metolcarb is an N-methylcarbamate insecticide that functions by inhibiting acetylcholinesterase, leading to the accumulation of acetylcholine and consequent disruption of neural transmission in pest organisms. This compound is utilized in agricultural practices to effectively manage various insect populations, enhancing crop protection. Its efficacy in targeting insects makes it a valuable tool in integrated pest management strategies. -
Racemate of Anabasine
(±) Anabasine hydrochloride is a racemic mixture of the alkaloid Anabasine, functioning primarily as an agonist of the alpha-7 nicotinic acetylcholine receptor (α7nAChR). This compound demonstrates notable anti-inflammatory properties, making it useful in studies related to inflammation and neuropathology. Additionally, it exhibits insecticidal activity, proving beneficial in entomological research. -
sEH/AChE Inhibitor
sEH/AChE-IN-3 is a potent dual inhibitor of soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE), demonstrating IC50 values of 0.4 nM for human sEH and 1.94 nM for human AChE. This compound also exhibits inhibitory activity against human butyrylcholinesterase with an IC50 of 615 nM, and shows strong inhibition in both mouse sEH and AChE with IC50 values of 4.3 nM and 2.61 nM, respectively. Due to its ability to penetrate the blood-brain barrier, sEH/AChE-IN-3 is suitable for research applications in neuropharmacology and the study of neurological disorders. -
sEH/AChE Inhibitor
sEH/AChE-IN-4 is a potent dual inhibitor targeting soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE). It demonstrates impressive inhibitory activity with IC50 values of 3.1 nM against human sEH, 1660 nM against human AChE, 179 nM against human butyrylcholinesterase (hBChE), 14.5 nM against murine sEH, and 102 nM against murine AChE. This compound has potential applications in research areas related to neurodegenerative diseases and pain modulation, effectively crossing the blood-brain barrier. -
Drug Derivative
Fenthion sulfone is a drug derivative primarily recognized for its potential as a pesticide metabolite. It exhibits significant biological activity by interacting with cholinesterase enzymes, leading to the inhibition of acetylcholine breakdown. This compound is utilized in research applications related to toxicology and environmental studies, particularly in assessing the effects of organophosphate compounds on biological systems.
