Catalog No.
Product Name
Application
Product Information
Citations
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AChE inhibitor
Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with an IC50 of 500 nM. -
AChE inhibitor
Rivastigmine tartrate is a dual cholinesterase inhibitor (ChEI). It inhibits both butyrylcholinesterase (BChE) and acetylcholinesterase (AChE). -
AChE inhibitor
Acotiamide is a drug approved in Japan for the treatment of postprandial fullness, upper abdominal bloating, and early satiation due to functional dyspepsia. -
AChE and BChE inhibitor
Tacrine hydrochloride hydrate is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively. -
BuChE inhibitor
BuChE-IN-TM-10 (TM-10) is a potent butyrylcholinesterase (BuChE) inhibitor, with an IC50 of 8.9 nM. -
AChE inhibitor
Acetyllovastatin, a acetate of Lovastatin, presentes a moderate inhibitory effect against the enzyme acetylcholinesterase with an IC50 of 79 μg/mL. Lovastatin has been found to display antifungal activity, and suppresses proliferation of a number of transformed cell lines. - (+)-Corynoline is an acetylcholinesterase inhibitor isolated from Corydalis incisa.
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acetylcholinesterase inhibitor
Pitofenone hydrochloride is an antispasmodic agent. It acts as a potent inhibitor of acetylcholinesterase activity. -
AChE & butyrylcholinesterase inhibitor
Tacrine is a derivative of aminoacridine that functions as an inhibitor of both acetylcholinesterase (AChE) and butyrylcholinesterase (IC50s = 31 and 26.5 nM, respectively). -
insecticide
Azamethiphos is an organothiophosphate insecticide. It is a veterinary drug used in Atlantic salmon fish farming to control parasites. -
Cholinesterase Reactivator
Pralidoxime iodide is a Cholinesterase Reactivator. -
BChE inhibitor
Drofenine hydrochloride is a potent competitive inhibitor of BChE, and the ki values of Drofenine is calculated to be 3 uM. -
acetylcholinesterase inhibitor
Edrophonium Chloride, also known as Tensilon, is an acetylcholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. Edrophonium Chloride has also been used as an antidote to curare principles. -
AChE inhibitor
Desoxypeganine hydrochloride is an AChE (acetylcholinesterase) inhibitor that has been used in the treatment of Alzheimer's dementia. -
AChE and BChE inhibitor
Rivastigmine, an cholinesterase inhibitor(IC50= 5.5 uM), inhibits both butyrylcholinesterase and acetylcholinesterase. -
Polygalacic acid (Virgaureagenin G) is a triterpenoid isolated from the root of Polygala tenuifolia Willd that inhibits MMP expression. Polygalacic acid (Virgaureagenin G) can significantly improve the responsiveness of the cholinergic system, such as decreased acetylcholinesterase (AChE) activity, increased choline acetyltransferase (ChAT) activity, and increased acetylcholine (ACh) levels in the hippocampus and frontal cortex. Polygalacic acid (Virgaureagenin G) can also inhibit IL-1β-induced Wnt/β-catenin activation and mitogen-activated protein kinase (MAPK) signaling pathways in chondrocytes, and is used in osteoarthritis (OA) related research
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Stable Isotope
Galanthamine-d6 is a deuterium-labeled derivative of Galanthamine, a potent inhibitor of acetylcholinesterase (AChE) with an IC50 value of 500 nM. This stable isotope compound is valuable in pharmacokinetic studies and metabolic research, particularly in exploring the mechanisms of cholinergic modulation. Its isotopic labeling helps in the precise tracking of metabolite pathways in biological assays. -
Phenolic Compound
Cardanol monoene is a phenolic compound derived from cashew nut shell liquid, primarily targeting cellular mechanisms involved in cancer progression. It exhibits significant anti-cancer activities, including the inhibition of cell proliferation and migration, S phase arrest, and induction of apoptosis via reactive oxygen species (ROS) production and mitochondrial depolarization. Cardanol monoene modulates key signaling pathways by downregulating MMP-2 and MMP-9 expressions and regulating the expression of CDK2, p53, and Bax, among others. Additionally, it demonstrates weak DPPH radical scavenging and acetylcholinesterase inhibition activities, making it suitable for research in cancer, infection, and inflammation. -
AChE Inhibitor
Kokusaginine is a furoquinoline alkaloid that acts as an acetylcholinesterase (AChE) inhibitor, exhibiting an IC50 value of 28.2 μM. This compound has demonstrated anti-proliferative and apoptotic effects in MCF-7/ADR cancer cell lines, making it a valuable reagent for research in neurobiology and cancer biology. Its ability to modulate cholinergic signaling and induce cell death highlights its potential for further investigation in therapeutic applications. -
CDK2/9 Inhibitor
ZLMT-12 is a potent CDK2/9 inhibitor, demonstrating IC50 values of 0.002 μM and 0.011 μM against CDK9 and CDK2, respectively. This compound is derived from tacrine and exhibits weak inhibition of acetylcholinesterase (IC50 = 19.023 μM) and butyrylcholinesterase (IC50 = 2.768 μM). ZLMT-12 is characterized by low toxicity and notable antiproliferative activity, effectively inducing apoptosis and facilitating cell cycle arrest in the S and G2/M phases. This compound serves as a valuable tool for research in cell cycle regulation and therapeutic development in cancer biology. -
ChA Inhibitor
α-NETA is a potent noncompetitive inhibitor of choline acetyltransferase (ChA), exhibiting an IC50 value of 9 μM. Additionally, it displays strong antagonistic activity against aldehyde dehydrogenase 1A1 (ALDH1A1) with an IC50 of 0.04 µM and also targets chemokine-like receptor-1 (CMKLR1). While it shows some inhibitory effects on cholinesterase (ChE) and acetylcholinesterase (AChE) with higher IC50 values, α-NETA is notable for its anti-cancer properties, making it a valuable tool for research in cancer biology and neuropharmacology. -
Stable Isotope
Propoxur-d3 is the deuterated form of Propoxur, a reversible and competitive acetylcholinesterase (AChE) inhibitor. It crosses the blood-brain barrier and exerts neurotoxic effects by inhibiting AChE activity, leading to increased acetylcholine levels and resultant neurological dysfunction. Additionally, Propoxur-d3 promotes the expression of matrix metalloproteinase-2 (MMP-2) and enhances tumor cell migration and invasion through the generation of intracellular reactive oxygen species (ROS) and the activation of the ERK/Nrf2 signaling pathway. This compound has applications in neurotoxicity studies and cancer research, as well as in assessing pesticide effects in ecological studies. -
Stable Isotope
Propoxur-d7 is the deuterium-labeled analog of Propoxur, a reversible and competitive inhibitor of acetylcholinesterase (AChE). This compound exhibits significant neurotoxic effects by inhibiting AChE activity, leading to increased levels of acetylcholine and subsequent neurological dysfunction. Propoxur-d7 also enhances tumor cell migration and invasion through the promotion of matrix metalloproteinase-2 (MMP-2) expression, driven by reactive oxygen species (ROS) generation and activation of the ERK/Nrf2 signaling pathway. Additionally, Propoxur serves as a carbamate insecticide effective against a variety of pests in turf, forestry, and household settings. -
5-HT Receptor Antagonist
T 82 is a potent 5-HT3 receptor antagonist that also functions as an acetylcholinesterase (AChE) inhibitor. This compound exhibits significant biological activity relevant for modulating neurotransmitter signaling in the central nervous system. T 82 is primarily utilized in research related to neurodegenerative diseases, including Alzheimer's Disease, making it a valuable tool in understanding the pathophysiology and treatment approaches for related conditions. -
AChE/SERT Inhibitor
BGC-201259 is a potent and orally active inhibitor of acetylcholinesterase (AChE) and serotonin transporter (SERT), with IC50 values of 101 nM and 42 nM, respectively. Additionally, it inhibits the 5-HT receptor with an IC50 of 90 nM. BGC-201259 exhibits varying activity against several targets, including the norepinephrine transporter (IC50 = 7.7 μM), L-type calcium channel (IC50 = 3.6 μM), σ receptor (IC50 = 2 μM), and sodium channel (IC50 = 5.1 μM). This compound shows promise in research related to Alzheimer's disease by potentially enhancing cognitive and emotional functions through its dual-targeting mechanism. -
AChE Inhibitor
Flucopride is an AChE inhibitor with an IC50 of 24 nM, demonstrating significant potency in acetylcholinesterase modulation. Additionally, it acts as a partial agonist at the 5-HT4 receptor with a binding affinity (Ki) of 9.6 nM. Flucopride facilitates non-amyloidogenic processing of amyloid precursor protein (APP) in COS-7 cells expressing the human 5-HT4 receptor, with an EC50 of 23.0 nM. Its properties suggest effective gastrointestinal tract penetration and the capability to cross the blood-brain barrier, as indicated by PAMPA assay results, making it relevant for neuropharmacology research. -
Stable Isotope
Dimethoate-d6 is a deuterium-labeled analogue of Dimethoate, an organophosphate insecticide and acaricide. It functions primarily as an acetylcholinesterase inhibitor, leading to enhanced neurotransmitter activity. This compound demonstrates significant biological activities, including the induction of reactive oxygen species (ROS), DNA damage, and cell apoptosis in vivo. Additionally, Dimethoate-d6 has been shown to affect immune system responses in murine models, making it a valuable tool for research in toxicology and environmental sciences. -
Stable Isotope
Galanthamine-O-methyl-d3 is a deuterium-labeled derivative of Galanthamine, a potent inhibitor of acetylcholinesterase (AChE) with an IC50 value of 500 nM. This stable isotope-labeled compound is primarily utilized in pharmacokinetic and metabolic studies. It serves as a valuable tool for investigating the pharmacological dynamics and biochemical pathways associated with cholinergic activity. -
Stable Isotope
Carbaryl-d7 is a deuterium-labeled derivative of Carbaryl, which functions as an acetylcholinesterase inhibitor. By suppressing the breakdown of acetylcholine in the synaptic cleft, Carbaryl-d7 leads to an accumulation of acetylcholine, potentially resulting in neurotoxic effects. This stable isotope is primarily utilized in chemical research to study the enzymatic action and biological effects of Carbaryl and its derivatives. -
Stable Isotope
Galanthamine-d3 hydrochloride is a deuterium-labeled derivative of Galanthamine, primarily used as a stable isotope. This compound serves as a useful tool in pharmacokinetic studies and metabolic research, enabling the investigation of drug metabolism and distribution. Galanthamine-d3 hydrochloride plays a significant role in understanding the mechanisms of action of acetylcholinesterase inhibitors and their effects on neurological processes. -
Anticancer Agent
Lanuginosine is an alkaloid with demonstrated anticancer activity. It induces apoptosis and inhibits acetylcholinesterase (AChE) with an IC50 of 10.9 μM, in addition to preventing amyloid-beta (Aβ) aggregation. This compound exhibits potent anticancer effects against various malignancies, including hepatocellular carcinoma, human promyelocytic leukemia, chronic myeloid leukemia, melanoma, and brain tumors. Lanuginosine is also valuable for research related to Alzheimer's disease and its therapeutic strategies. -
Stable Isotope
Carbaryl-d3 is a deuterium-labeled variant of Carbaryl, characterized as an acetylcholinesterase inhibitor. This compound prevents the breakdown of acetylcholine in the synaptic cleft, resulting in its accumulation and subsequent neurotoxic effects. Carbaryl-d3 is employed in research related to neurotoxicity mechanisms and may serve as a tool for studying the pharmacokinetics and metabolic pathways of Carbaryl. Its stable isotope labeling enhances analytical precision in experimental applications. -
Apoptosi
Pamiparib maleate is a highly potent and selective inhibitor of poly (ADP-ribose) polymerase (PARP), targeting apoptotic pathways. This compound effectively penetrates the blood-brain barrier, inducing neurotoxicity manifesting as cerebral hemorrhage, brain atrophy, and movement disorders in zebrafish embryos. It regulates critical enzymes such as acetylcholinesterase (AChE) and adenosine triphosphatase (ATPase), leading to increased oxidative stress that triggers apoptosis and affects the expression of neurodevelopment-related genes. Additionally, pamiparib maleate downregulates the Notch signaling pathway, providing insights into its potential neurotoxic effects during embryonic development and its relevance in neuropharmacology research. -
MAO-B/Acetylcholinesterase Inhibitor
MAO-B-IN-26 is a selective inhibitor of monoamine oxidase B (MAO-B) and acetylcholinesterase, demonstrating neuroprotective properties against β-amyloid (Aβ) induced cytotoxicity in SH-SY5Y cells. This compound effectively mitigates morphological alterations, reactive oxygen species (ROS) generation, and membrane damage associated with neurodegeneration. Additionally, MAO-B-IN-26 suppresses Aβ-induced autophagy and apoptosis, making it a valuable tool for research focused on therapeutic strategies for Alzheimer's disease. -
BChE Inhibitor
Pteryxin is a potent butyrylcholinesterase (BChE) inhibitor (IC50 = 12.96 μg/mL) with additional multi-target mechanisms including inhibition of NF-κB, MAPK, NLRP3 inflammasome activation, and modulation of the Nrf2/ARE pathways. This compound demonstrates significant anti-inflammatory, antioxidant, and osteoclastogenesis inhibitory activities. Pteryxin is suitable for research applications related to inflammatory diseases, osteoporosis, diabetes, and neurodegenerative disorders such as Alzheimer's disease. -
AChE/BChE/BACE-1 Inhibitor
AChE/BChE/BACE-1-IN-1 is a potent inhibitor of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and beta-secretase 1 (BACE-1), exhibiting IC50 values of 0.058 μM, 0.082 μM, and 0.115 μM, respectively. This compound demonstrates significant binding affinity for the peripheral anionic site of AChE, facilitates brain penetration, and shows potential in disrupting amyloid-beta (Aβ) aggregates. Additionally, AChE/BChE/BACE-1-IN-1 exhibits neuroprotective properties against Aβ-induced stress and possesses promising antioxidant activity, making it a valuable tool for Alzheimer's disease research and related neurodegenerative studies. -
AChE/BChE Inhibitor
AChE/BChE-IN-9 is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), exhibiting IC50 values of 5.74 μM and 14.05 μM, respectively. In addition to its enzymatic inhibition, AChE/BChE-IN-9 demonstrates antioxidant properties with an IC50 of 57.35 μM and has the ability to chelate iron, potentially mitigating oxidative stress. This compound also influences the aggregation of amyloid β1-42, making it relevant for research in neurodegenerative diseases and gerontology. Its capacity to cross the blood-brain barrier further enhances its suitability for studies focused on central nervous system disorders. -
AChE/GSK-3β Inhibitor
AChE/GSK-3β-IN-1 is a dual inhibitor targeting acetylcholinesterase (AChE) and glycogen synthase kinase 3 beta (GSK-3β), demonstrating potent inhibition with IC50 values of 1.2 nM for hAChE, 149.8 nM for hBChE, and 22.4 nM for hGSK-3β. This compound effectively penetrates the blood-brain barrier and displays high selectivity for the CMGC kinase family, particularly binding to the ATP site of DYRK1A. Additionally, AChE/GSK-3β-IN-1 has been shown to inhibit reactive oxygen species (ROS) expression, thereby reducing oxidative stress. It is a valuable tool for research into Alzheimer's disease and related neurodegenerative conditions. -
AChE/BChE/BACE-1 Inhibitor
AChE/BChE/BACE-1-IN-2 is a potent oral inhibitor of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1), exhibiting IC50 values of 0.069 μM, 0.127 μM, and 0.097 μM, respectively. This compound demonstrates significant binding affinity to the peripheral anionic site of AChE, high brain permeability, and the ability to disassemble amyloid-beta (Aβ) aggregates. Additionally, AChE/BChE/BACE-1-IN-2 provides neuroprotective effects against Aβ-induced stress and possesses noteworthy antioxidant properties, making it suitable for research in neurodegenerative disease models. -
AChE/BChE Inhibitor
AChE-IN-14 is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), displaying IC50 values of 0.46 μM for electric eel AChE, 0.48 μM for human recombinant AChE, and 0.44 μM for equine serum BChE. In addition to its cholinesterase inhibition, AChE-IN-14 has a high affinity for the human H3 receptor (H3R) with a Ki value of 159.8 nM. This compound is particularly relevant for research focused on neurodegenerative diseases such as Alzheimer’s disease, where the modulation of cholinergic signaling is critical. -
Antihistamine Agent
Difeterol is an antihistamine agent that functions primarily as a histamine-1 receptor antagonist. It also inhibits butyrylcholinesterase (BChE), making it a valuable tool for studying cholinergic pathways. This compound is particularly relevant for research related to Alzheimer's disease, where modulation of histamine and cholinergic systems may provide insights into therapeutic strategies. -
Antioxidant
Contilisant is a potent antioxidant and neuroprotective agent that targets histamine H3 receptors. It effectively inhibits monoamine oxidases and cholinesterases, contributing to its neuroprotective profile. With a binding affinity of 65.23 nM towards human sigma-1 receptor, Contilisant demonstrates significant therapeutic potential. In preclinical studies, it has been shown to restore cognitive deficits induced by Aβ1-42 in the radial maze assay, making it a valuable tool for Alzheimer's disease research. -
Histamine H3 Receptor Antagonist
AChE/BChE-IN-21 is a histamine H3 receptor antagonist that also functions as a calcium channel blocker and acetylcholinesterase inhibitor. This compound demonstrates neuroprotective properties against oxidative stress induced by H2O2 and amyloid-beta peptide Aβ1-40. Additionally, AChE/BChE-IN-21 has been shown to improve cognitive function in mouse models of Alzheimer's disease, making it a valuable tool for research into neurodegenerative disorders. -
H3R Antagonist
H3R Antagonist 2 is a selective antagonist of the histamine H3 receptor (H3R) with a Ki value of 170 nM for human H3R. This compound demonstrates inhibitory activity against acetylcholinesterase, butyrylcholinesterase, and human monoamine oxidase B (hMAO B), with IC50 values of 180 nM, 880 nM, and 775 nM, respectively. Additionally, H3R Antagonist 2 exhibits promising anti-neuropathic pain and memory-enhancing effects, effectively crossing the blood-brain barrier (BBB). This makes it a valuable tool for research in neuropharmacology and cognitive enhancement studies.
