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Catalog No.
Product Name
Application
Product Information
Citations
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GABAAR Inhibitor
Org 21465 is a selective inhibitor of the GABA A receptor (GABA A R). It exhibits significant analgesic properties without inducing cardiovascular or respiratory depression, making it a valuable compound for pain research. This compound can be utilized in studies concerning the modulation of GABAergic neurotransmission and its effects on pain mechanisms in vivo. -
GABA-AT Inhibitor
GABA-AT-IN-2 is an inhibitor of GABA aminotransferase (GABA-AT) with an IC50 of 19.8 μM. This compound has demonstrated significant antianxiety effects in preclinical models, making it a valuable tool for investigating anxiety-related neurotic disorders. Its application in research may provide insights into therapeutic strategies for managing anxiety. -
GABA Uptake Inhibitor
CI-966 is a highly selective, orally active inhibitor of the GABA transporter GAT-1, with exceptional brain penetration. It displays IC50 values of 0.26 μM for human GAT-1 and 1.2 μM for rat GAT-1, demonstrating over 200-fold selectivity against GAT-2, GAT-3, and BGT-3. CI-966 is recognized for its anticonvulsant and neuroprotective properties, making it a valuable tool for neuropharmacological research. -
GABAA Inhibitor
AA29504 is an ethyl carbamate that functions as a GABAA receptor inhibitor. It effectively blocks the transmission of gamma-aminobutyric acid (GABA), a key neurotransmitter in the central nervous system, leading to its potential applications in the study of anxiety, insomnia, and other neuropsychiatric disorders. This compound serves as an important tool for researchers investigating GABAA receptor-mediated pathways and their role in various neurological conditions. -
GABA Receptor Inhibitor
CP-457920 is a potent GABA receptor inhibitor with a Ki value of approximately 1 ng/mL. This compound is primarily utilized in neurological research, particularly for studying pathways and mechanisms underlying diseases such as Alzheimer's disease. Its inhibitory action on GABA receptors makes it a valuable tool for investigating neuropharmacological processes and potential therapeutic interventions. -
GABA Receptor Inhibitor
DPNI-GABA is a nitroindoline derivative that selectively inhibits GABA(A) receptors, significantly decreasing GABA-evoked peak responses with an IC50 value of 0.5 mM. This compound serves as a valuable tool for researching the role of GABAergic signaling in various physiological and pathological processes, contributing to studies of neuronal excitability and synaptic transmission. Its inhibition of GABA(A) receptors makes it essential for elucidating mechanisms of action in neuropharmacology and related fields. -
GABA Receptor Inhibitor
SKF 89976A is a selective GABA transporter (GAT-1) inhibitor, displaying an IC50 of 0.28 μM for GAT-1 and significantly higher IC50 values of 137.34 μM and 202.8 μM for GAT-2 and GAT-3, respectively, in CHO cells. This compound is primarily utilized in neurological research focusing on the modulation of GABA neurotransmission. Its specificity for GAT-1 makes it a valuable tool for studying GABAergic signaling and related disorders. -
GABA-T Inhibitor
D-DABA is an enantiomeric form of L-DABA that acts as a weak inhibitor of GABA transaminase (GABA-T). Its inhibitory potency is approximately one-twentieth that of the L-isomer in reducing GABA uptake. This compound is useful in research applications involving GABA metabolism and neurotransmitter modulation. -
GABA/nACh Receptor Inhibitor
APS3 is a potent inhibitor of GABA and nicotinic acetylcholine (nACh) receptors, showcasing a lethal concentration (LC50) of 7.2423 μg/mL against the pest Plutella xylostella. This compound is useful for studying neuropharmacological pathways and assessing the impact of receptor inhibition on insect behavior and survival. Applications include research in insect physiology and the development of pest management strategies. -
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. -
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. -
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. -
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. -
α-Amylase Inhibitor
α-Amylase-IN-3 is a potent inhibitor of α-Amylase, exhibiting an IC50 of 18.04 μM, and also targets acetylcholinesterase (AChE) with IC50s of 21.04 μM and 22.2 μM, respectively. This compound demonstrates antioxidant activity, making it valuable for studies related to diabetes and diseases associated with oxidative stress. Its biochemical properties make α-Amylase-IN-3 a useful tool for researchers investigating metabolic disorders and neuroprotective mechanisms. -
α-glucosidase/α-amylase enzyme Dual Inhibitor
α-Amylase/α-Glucosidase-IN-7 is a competitive dual inhibitor targeting α-glucosidase and α-amylase, demonstrating IC50 values of 18.52 µM and 20.25 µM, respectively. Additionally, this compound effectively inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 values of 9.25 µM and 10.06 µM. α-Amylase/α-Glucosidase-IN-7 is valuable for research applications related to diabetes and Alzheimer’s disease. -
CES Inhibitor
Dibromsalicil is a selective inhibitor of carboxylesterases (CES), exhibiting inhibitory activity with IC50 values of 72.7 nM against human intestinal carboxylesterase (hiCE) and 53.5 nM against rabbit liver carboxylesterase (rCE). This compound demonstrates minimal activity against human liver carboxylesterase (hCE1) and cholinesterase, making it a valuable tool for research applications focused on drug metabolism and enzymatic activity modulation. Its specificity for hiCE and rCE positions Dibromsalicil as an important reagent for studying carboxylesterase-related pathways. -
AChE/CES Inhibitor
Heptenophos is a potent inhibitor of acetylcholinesterase (AChE) and plasma carboxylesterase (CES). By obstructing AChE activity, Heptenophos leads to the accumulation of acetylcholine at cholinergic synapses, which can result in symptoms characteristic of organophosphate poisoning. Its rapid toxicity in animal models, such as male albino mice, allows for the investigation of detoxification strategies, particularly in conjunction with agents like obidoxime and Memantine. This compound is widely utilized in research exploring the mechanisms underlying organophosphate effects and potential antidotal treatments. -
COMT Inhibitor
Neluxicapone is a potent inhibitor of catechol-O-methyltransferase (COMT), primarily utilized in the research of Parkinson's disease (PD). By inhibiting COMT, this compound enhances dopamine levels in the brain, which may alleviate motor symptoms associated with PD. Researchers can use neluxicapone to investigate its pharmacological effects and potential therapeutic benefits in neurodegenerative conditions. -
COMT Inhibitor
Ro 41-0960 is a selective inhibitor of catechol-O-methyltransferase (COMT), which plays a crucial role in the metabolism of catecholamines. By inhibiting COMT, this compound enhances the levels of neurotransmitters such as dopamine, norepinephrine, and epinephrine. It is widely used in research to investigate the biochemical pathways of neurotransmission and to explore potential therapeutic applications in conditions such as Parkinson's disease and other neuropsychiatric disorders. -
COMT Inhibitor
Nitecapone is an orally active and short-acting catechol-O-methyltransferase (COMT) inhibitor. It exhibits notable gastroprotective and antioxidant properties by scavenging reactive oxygen and nitrogen species, thereby preventing lipid peroxidation. Nitecapone is valuable in research applications focusing on neurodegenerative diseases and other conditions where COMT modulation may play a therapeutic role. -
hMAO-B/MB-COMT Inhibitor
hMAO-B/MB-COMT-IN-1 is a dual inhibitor of human monoamine oxidase B (hMAO-B) and membrane-bound catechol-O-methyltransferase (MB-COMT), exhibiting IC50 values of 2.5 µM and 3.84 µM, respectively. This compound is effective in protecting cells from oxidative damage, making it a valuable tool for studying neurodegenerative diseases, including Parkinson's Disease. Its dual inhibition profile provides insights into the molecular mechanisms underlying these conditions and aids in the development of potential therapeutic strategies. -
COMT Inhibitor
S-Adenosylhomocysteine sulfoxide is a potent inhibitor of catechol-O-methyltransferase (COMT) with an IC50 value of 860 μM. This compound is utilized in research to investigate the modulation of methylation reactions, providing valuable insights into biochemical pathways involving methyltransferases. Its inhibitory properties make it a significant tool for studies related to neurotransmitter metabolism and epigenetic regulation. -
COMT Inhibitor
U-0521 is a selective inhibitor of catechol-O-methyltransferase (COMT), an enzyme involved in the metabolism of catecholamines. This compound exhibits significant biological activity by modulating neurotransmitter levels, which is crucial for investigations into Parkinson's disease and related disorders. U-0521 is valuable for research focused on understanding the role of COMT in neurodegenerative conditions and for exploring potential therapeutic strategies targeting this pathway. -
COMT Inhibitor
(Z)-Entacapone is a selective inhibitor of catechol-O-methyltransferase (COMT), crucial for catecholamine metabolism. This compound serves as a valuable tool in studying COMT's role in neurological disorders and drug metabolism. Additionally, it may appear as a potential impurity in commercial Entacapone preparations or as a degradation product due to UV light exposure, providing further relevance in quality control and biological research applications. -
hMAO-B/MB-COMT Inhibitor
hMAO-B/MB-COMT-IN-2 is a potent dual inhibitor of hMAO-B and MB-COMT, exhibiting IC50 values of 4.27 μM and 2.69 μM, respectively. This compound effectively protects cells from oxidative damage, making it valuable for studies related to neurodegenerative diseases. hMAO-B/MB-COMT-IN-2 is particularly relevant in the research of conditions such as Parkinson’s Disease, offering insights into potential therapeutic strategies. -
COMT Inhibitor
COMT-IN-1 is a potent catechol-O-methyltransferase (COMT) inhibitor, demonstrating an IC50 of 0.37 μM for COMT activity. This nitrophenolic analogue effectively inhibits monoamine oxidase A (MAO-A) and MAO-B with IC50 values of 95.58 μM and 58.82 μM, respectively. With good blood-brain barrier permeability, COMT-IN-1 enhances dopamine levels and alleviates symptoms associated with MPTP-induced Parkinson's disease in murine models, making it a valuable tool for research into Parkinson's disease and dopamine metabolism. -
COMT Inhibitor
CGP 28014 is a potent inhibitor of catechol-O-methyltransferase (COMT), an enzyme involved in the metabolism of catecholamines. This compound has been shown to lower homovanillic acid (HVA) levels and increase dihydroxyphenylacetic acid (DOPAC) levels in the striatum of rat models. CGP 28014 is valuable in research focused on the pathophysiology and potential treatment strategies for Parkinson's disease, providing insights into dopaminergic signaling and neurotransmitter dynamics. -
COMT Inhibitor
BIA 3-335 is a potent inhibitor of catechol-O-methyltransferase (COMT), an enzyme involved in the metabolism of catecholamines. Its primary mechanism disrupts the methylation of catechols, leading to increased levels of dopamine, which may be beneficial in the study of Parkinson's disease and related neurological disorders. This compound is widely used in research settings to explore therapeutic strategies aimed at enhancing dopaminergic signaling. -
COMT Inhibitor
Methylspinazarin is a potent inhibitor of catechol O-methyltransferase (COMT), exhibiting an IC50 of 0.8 μg/ml. Isolated from the actinobacterium Streptomyces, Methylspinazarin demonstrates selectivity for COMT compared to tyrosine hydroxylase. This compound is valuable for research applications focused on neurotransmitter metabolism and the pharmacological modulation of catecholamine pathways. -
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. -
ACOX1 Inhibitor
10,12-Tricosadiynoic acid is a selective and potent inhibitor of acyl-CoA oxidase-1 (ACOX1). It demonstrates significant potential in addressing metabolic disorders induced by high-fat diets or obesity by enhancing mitochondrial lipid metabolism and modulating reactive oxygen species (ROS) levels. Additionally, this compound serves as a versatile click chemistry reagent, featuring an alkyne group that facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, making it valuable for various biochemical applications. -
OGT Inhibitor
ST045849 is a small-molecule inhibitor targeting O-GlcNAc transferase (OGT) with an IC50 of 30 μM against the soluble form of OGT (sOGT) and 53 μM against the nuclear/cytoplasmic form (ncOGT). This compound is valuable for studying the role of OGT in metabolism-related diseases, providing insights into regulatory mechanisms involving O-GlcNAcylation. Its application aids in understanding the biological implications of OGT inhibition in various pathological conditions. -
OGT Inhibitor
OSMI-2 is a selective inhibitor of O-linked N-acetylglucosamine transferase (OGT), designed for cellular permeability. This compound has been shown to enhance the splicing of retained introns in various cell types, making it a valuable tool for studying the regulation of alternative splicing and OGT's role in cellular processes. OSMI-2 is applicable in various research fields, including cancer biology and neurodegenerative disorders, where OGT activity is implicated. -
OGT Inhibitor
OSMI-3 is a selective inhibitor of O-linked N-acetylglucosamine transferase (OGT), characterized by its potent and cell-permeable properties. This compound effectively modulates OGT activity, leading to the enhancement of retained intron splicing in cellular contexts. OSMI-3 is valuable in research investigating the role of OGT in cellular processes and its implications in various disease states. -
Cholinesterase (ChE) Inhibitor
Sinapine hydroxide is an acetylcholinesterase (AChE) inhibitor with significant potential in the investigation of neurodegenerative disorders such as Alzheimer's disease, myasthenia gravis, ataxia, and Parkinson's disease. This alkaloid, derived from cruciferous seeds, exhibits a range of biological activities including anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic, and radioprotective effects. Its ability to modulate cholinergic pathways makes it a valuable tool for studying cholinergic dysfunction and related therapeutic strategies. -
P2X Receptor Inhibitor
PSFL2915 is a selective inhibitor of the P2X receptor family, exhibiting an IC50 of 0.319 μM for human P2X3 and 0.261 μM for rat P2X2/3, with approximately 42-fold selectivity for human P2X3 over human P2X2. This compound inhibits human P2X3 activation by disrupting the allosteric tightening of the inner pocket necessary for channel opening, with dependency on magnesium for its inhibitory effect. Additionally, PSFL2915 demonstrates inhibitory activity against rat P2X2/3 and human P2X2 receptors, while showing minimal effects on human P2X1, P2X4, and P2X7 receptors. It is applicable in chronic cough research. -
P2X Receptor Inhibitor
AZD9056 hydrochloride is a selective oral inhibitor of the P2X7 receptor, which is implicated in various inflammatory and pain-related conditions. By blocking P2X7 activity, this compound demonstrates potential in modulating inflammatory responses, making it a valuable tool for research in pain management and inflammatory disease pathways. Its application in preclinical studies may help elucidate the role of purinergic signaling in various biological processes. -
P2X4 Inhibitor
NP-1815-PX sodium is a selective inhibitor targeting the P2X4 receptor, exhibiting an IC50 of 0.26 μM against human P2X4 receptors. This compound effectively inhibits ATP-mediated prostaglandin production and attenuates TP receptor-induced calcium elevation, as well as NLRP3 inflammasome signaling. Notably, NP-1815-PX sodium demonstrates anti-allodynic effects in vivo and alleviates DNBS-induced colitis symptoms, including weight loss and tissue damage, through the downregulation of IL-1β levels and Caspase-1 activity. This reagent is applicable in research areas such as asthma and inflammatory bowel disease. -
P2X4 Receptor Inhibitor
Taspine is a natural product that functionally inhibits the P2X4 receptor, primarily through the inhibition of the PI3K signaling pathway. This compound exhibits notable anti-inflammatory activity by suppressing pro-inflammatory signaling in macrophages. Taspine is valuable for research applications focused on inflammation and immune responses, as well as studying the role of purinergic receptors in various pathological conditions. -
P2X3 Receptor Inhibitor
P2X3-IN-1 is a selective inhibitor of the P2X3 receptor, which plays a crucial role in mediating pain and other neurogenic responses. This compound demonstrates significant biological activity in modulating P2X3 receptor signaling, making it valuable for research into neurogenic diseases and pain pathways. Researchers can utilize P2X3-IN-1 to explore therapeutic strategies for conditions associated with P2X3 receptor dysfunction. -
P2X4 Inhibitor
P2X4 antagonist-1 is a potent inhibitor of the P2X4 receptor, exhibiting an IC50 of 15 nM. This compound effectively modulates P2X4 signaling, making it valuable for research involving pain modulation, neuroinflammation, and cardiovascular regulation. Its specificity towards P2X4 supports studies aimed at understanding its role in various pathophysiological conditions. -
P2X3 Receptor Inhibitor
Purotoxin 1 is a selective P2X3 receptor inhibitor. It exhibits significant antinociceptive effects in animal models of inflammatory pain, making it a valuable tool for pain research. Isolated from the venom of the wolf spider Geolycosa sp., Purotoxin 1 can be utilized in studies aimed at understanding pain mechanisms and developing new analgesic therapies. -
P2X1 Receptor Inhibitor
NF864 is a selective inhibitor of the P2X1 receptor, primarily expressed in human platelets. This compound effectively disrupts ATP-mediated signaling cascades involved in platelet activation and aggregation. NF864 is useful in research applications focused on cardiovascular disease, thrombosis, and platelet-related disorders, allowing scientists to investigate the role of P2X1 in vascular biology. -
P2X4 Inhibitor
P2X4-IN-1 is a potent inhibitor of the P2X4 receptor, which is involved in various physiological processes including pain perception and inflammation. This compound demonstrates significant biological activity by selectively blocking P2X4 receptor signaling. Its application in research allows for the investigation of therapeutic strategies for diseases associated with P2X4 receptor dysregulation. -
P2X7 Receptor Inhibitor
GSK1370319A is a selective inhibitor of the human P2X7 receptor, demonstrating an IC50 of 474 nM and a Ki of 176 nM. This compound effectively inhibits the production of interleukin-1 beta (IL-1β), decreases the generation of reactive oxygen species (ROS), and enhances macrophage survival rates. GSK1370319A is applicable in research related to inflammatory bowel disease and the broader study of inflammatory processes. -
P2X Receptor Inhibitor
P2X receptor-1 is a selective inhibitor of P2X receptors, which play a critical role in mediating pain and inflammatory responses. This compound has potential applications in research focused on understanding nociception and addressing inflammatory conditions. Its ability to modulate P2X receptor activity makes it an important tool for exploring therapeutic strategies in pain management and inflammation research. -
P2X3 Inhibitor
TC-P 262 is a highly effective inhibitor of the P2X3 receptor, a key player in pain and inflammatory responses. By binding to the human P2X3 receptor, TC-P 262 demonstrates significant inhibitory effects, making it a valuable tool for studying conditions such as rheumatoid arthritis, chronic cough, and pain management. This reagent facilitates the exploration of P2X3's role in these biological processes, contributing to the understanding of potential therapeutic interventions. -
AChE/BuChE Inhibitor
Ipidacrine is a potent and selective inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), exhibiting IC50 values of 1 μM and 1.9 μM, respectively. This compound also acts as a partial agonist on M2-cholinergic receptors, promoting neuromuscular transmission and providing a moderate anti-pain effect. Ipidacrine is relevant for research into Alzheimer's disease, ischemic stroke, and diabetic complications, enhancing erectile function and exhibiting effects on ionic channels in neuronal membranes. Its applications extend to studying various deficits in central and peripheral cholinergic disorders.
