Catalog No.
Product Name
Application
Product Information
Citations
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Parasite
Triazophos is a potent non-systemic insecticide and acaricide that functions as an acetylcholinesterase (AChE) inhibitor. By covalently and irreversibly binding to the acetylcholine binding site, Triazophos effectively disrupts the hydrolysis of acetylcholine, resulting in increased neuroexcitability. This compound demonstrates efficacy against a broad spectrum of soil insects and mites, including aphids, thrips, and spider mites, making it valuable for crop protection in various agricultural settings, such as ornamentals, cotton, rice, maize, soybeans, oil palms, olives, and coffee. -
Parasite Inhibitor
Phosalone is an organophosphate insecticide that primarily targets acetylcholinesterase, leading to the inhibition of neurotransmission in parasites. Its potent biological activity makes it effective in controlling a wide range of insect pests. Phosalone is utilized in entomological research and in studies focusing on pest management strategies and the biochemical pathways of insecticide resistance. -
ChE Inhibitor
Isogarcinol is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), exhibiting IC50 values of 1.13 μM and 8.30 μM, respectively. This compound also demonstrates significant leishmanicidal activity, with an IC50 of 0.33 μM against Leishmania donovani. Isogarcinol's dual action makes it a valuable tool for research in neurodegenerative disorders and parasitic diseases. -
Stable Isotope
Temephos-d12 is a deuterated form of Temephos, an organophosphate larvicide. It targets the central nervous system of aquatic larvae, including those of mosquitoes, midges, and black flies, by inhibiting cholinesterase activity. This mechanism leads to larval mortality prior to reaching the adult stage, making Temephos-d12 valuable for research on pesticide efficacy and environmental impact studies. -
AChE Inhibitor
Temephos is an organophosphate insecticide that functions as an irreversible inhibitor of acetylcholinesterase (AChE). This inhibition leads to cholinergic overactivation, effectively disrupting the larval development of Aedes aegypti and Aedes albopictus, making it a valuable tool in research concerning Dengue Virus, Zika Virus, and other mosquito-borne pathogens. While exhibiting important biological activity, Temephos has been shown to cause genotoxicity, neurodevelopmental toxicity, and potential liver and reproductive system effects in mammals. Additionally, it can accumulate in adipose tissues and aquatic organisms, with its metabolism primarily occurring through oxidation and hydrolysis. Temephos serves as a critical reagent in studies of vector control and viral transmission dynamics. -
SMase Inhibitor
SMase-IN-1 is a specific inhibitor of bacterial sphingomyelinase (SMase), exhibiting an IC50 value of 6.43 µM against B. cereus SMase. In addition to its primary activity, SMase-IN-1 also demonstrates a significant inhibition rate of 59.50% for equine butyrylcholinesterase (eqBuChE) at a concentration of 50 µM. This compound forms a complex with Cu2+ in biometal interactions and effectively reduces hemolysis induced by B. cereus in sheep erythrocytes. SMase-IN-1 is valuable for research in microbial pathogenesis and enzyme inhibition studies. -
Stable Isotope
Itopride-d6 is a deuterated form of Itopride, a potent dopamine D2 receptor antagonist and acetylcholinesterase (AChE) inhibitor. Its unique stable isotope labeling allows for advanced metabolic and pharmacokinetic studies. Itopride enhances gastric motility through its combined antidopaminergic and anti-AChE actions, making it valuable in research applications focused on gastrointestinal prokinetics and conditions such as gastro-esophageal reflux disease (GERD). -
Babesicidal Agent
Quinuronium disulfate is a potent babesicidal agent with demonstrated anticholinesterase activity. It is primarily utilized in the study of protozoan infections, particularly those caused by Babesia species. This compound serves as a valuable tool in researching therapeutic interventions for babesiosis and related parasitic diseases. -
AChE/Dopamine 2 Inhibitor
Itopride is a potent dopamine D2 receptor antagonist and an acetylcholinesterase (AChE) inhibitor. Itopride enhances gastric motility through its dual mechanisms of action, promoting both antidopaminergic and anti-acetylcholinesterase effects. This compound is primarily utilized in research related to gastrointestinal disorders, particularly gastroesophageal reflux disease (GERD), offering insights into prokinetic therapies. -
BChE Inhibitor/CB2R Agonist
hBChE-IN-2 is a potent butyrylcholinesterase (BChE) inhibitor with an IC50 of 0.62 μM and functions as an agonist for cannabinoid receptor 2 (CB2R). This compound exhibits significant neuroprotective activities, making it a valuable tool in the study of neurodegenerative diseases and cannabinoid signaling pathways. Its dual action positions hBChE-IN-2 as an important reagent for research applications targeting cholinergic regulation and endocannabinoid modulation. -
Alkaloid
Aposcopolamine is an alkaloid isolated from Datura ferox, known for its ability to bind closely with acetylcholinesterase (ACHE), adrenergic receptor alpha-2A (ADRA2A), and muscarinic receptor subtype 2 (CHRM2). This compound is of significant interest in Alzheimer's disease research due to its potential effects on cholinergic signaling pathways. Aposcopolamine serves as a valuable tool in investigating neurodegenerative mechanisms and developing therapeutic strategies. -
Topoisomerase I Inhibitor
RPR121056 is a topoisomerase I inhibitor that functions as a metabolite of the chemotherapy agent Irinotecan (CPT-11), produced by the enzyme CYP3A4. This compound induces cell death by disrupting DNA replication, making it relevant for cancer research, particularly in the context of colorectal cancer treatment. Additionally, RPR121056 demonstrates direct inhibition of acetylcholinesterase (AChE), further expanding its potential applications in pharmacological studies. -
Stable Isotope
RPR121056-d3 is a deuterated analog of RPR121056, a metabolite of the anticancer drug Irinotecan. It primarily targets and inhibits topoisomerase type I, leading to apoptosis in cancer cells. RPR121056-d3 is utilized in research applications focused on understanding the metabolic pathways and pharmacokinetics of Irinotecan, particularly in the context of colorectal cancer therapy. Additionally, it may also provide insights into the inhibition of acetylcholinesterase (AChE). -
Alkaloid
Circumdatin C is an alkaloid that demonstrates inhibitory effects on lipopolysaccharide (LPS)-stimulated nitric oxide production. Additionally, it inhibits acetylcholinesterase (AChE) activity with an IC50 value of 13.9 μM. This compound is valuable for research into neurodegenerative diseases, particularly Alzheimer's disease, by exploring mechanisms related to neurotransmitter regulation and neuroinflammation. -
Antioxidant Agent
4-Hydroxyisophthalic acid functions primarily as an antioxidant agent, activating crucial antioxidant enzymes such as catalase (CAT) and superoxide dismutase (SOD). Its ability to scavenge free radicals contributes to its protective effects on neuronal function, as it enhances the activity of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). In research applications, 4-Hydroxyisophthalic acid has demonstrated potential in improving cognitive defects and alleviating circadian rhythm disorders in model organisms, such as fruit flies. -
Stable Isotope
Imidazole-15N2 is a stable isotope-labeled derivative of imidazole, a heterocyclic aromatic compound. It serves as a valuable tool in metabolic studies and tracing experiments due to its nitrogen-15 labeling. Imidazole and its derivatives exhibit a wide range of biological activities, including inhibition of acetylcholinesterase and xanthine oxidase, as well as properties such as antifungal, antituberculosis, anti-inflammatory, and antioxidant effects. Additionally, imidazole derivatives have shown promise in the inhibition of SARS-CoV-2 3CLPro enzyme, highlighting their potential applications in research related to Alzheimer's disease, gout, COVID-19, and thromboembolic disorders. -
COX-2 Inhibitor
COX-2-IN-22 is a selective inhibitor of Cyclooxygenase-2 (COX-2) with an IC50 of 8.6 µM. In addition to its primary activity, COX-2-IN-22 also exhibits inhibitory effects on Acetylcholinesterase (AChE), Butyrylcholinesterase (BChE), β-Secretase, Lipoxygenase-5 (LOX-5), and DPPH, with IC50 values of 2.8 µM, 6.3 µM, 15.3 µM, 13.9 µM, and 6.8 µM, respectively. This compound is capable of crossing the blood-brain barrier, making it a valuable tool for research in neuroinflammatory and neurodegenerative disease models. -
μ-Opioid Receptor Agoinst/AChE Inhibitor
Eseroline is a potent μ-opioid receptor agonist and a selective, competitive inhibitor of acetylcholinesterase (AChE), with Ki values of 0.1 μM for AChE and 200 μM for butyrylcholinesterase (BuChE). This compound also acts as a nicotinic acetylcholine receptor allosteric enhancing ligand, enhancing acetylcholine signal transduction without directly activating the receptor. Eseroline's neurotoxic effects include cell membrane damage and energy metabolism disruption, making it a valuable tool for investigating Alzheimer's disease pathology and cholinergic signaling. -
BChE/NMDA/mAChR Antagonist
Ethopropazine hydrochloride is a potent and selective inhibitor of butyrylcholinesterase (BChE) and acts as a non-selective antagonist at muscarinic acetylcholine receptors (mAChR) and N-methyl-D-aspartate receptors (NMDA). This compound exhibits anticholinergic, antihistamine, and antiadrenergic activities, making it valuable in studying its effects on neuropathic pain conditions such as thermal hyperalgesia. Ethopropazine hydrochloride is particularly relevant in research related to Parkinson's disease, providing insights into cholinergic system modulation and receptor interactions. -
Aβ Inhibitor
Fustin (3,7,3',4'-Tetrahydroxyflavanone) is a potent inhibitor of amyloid β (Aβ), demonstrating significant effects on neurochemical markers associated with Alzheimer's disease. It enhances acetylcholine (ACh) levels and stimulates choline acetyltransferase (ChAT) activity while decreasing acetylcholinesterase (AChE) activity and expression. Additionally, Fustin promotes the expression of muscarinic M1 receptor genes and enhances receptor binding activity. This compound is valuable for research in Alzheimer's disease and neurodegenerative processes involving Aβ toxicity. -
Diacylglycerol Lipase Inhibitor
RHC 80267 is a potent and selective inhibitor of diacylglycerol lipase (DAGL), exhibiting an IC50 of 4 μM in canine platelets. This compound is valuable for research applications focusing on the modulation of lipid signaling pathways, particularly in the context of acetylcholine-induced relaxation. Additionally, RHC 80267 demonstrates inhibitory effects on cholinesterase with an IC50 of 4 μM and also inhibits cyclooxygenase (COX) and the hydrolysis of phosphatidylcholine (PC), making it a versatile tool for exploring lipid metabolism and neuronal signaling. -
M4 Receptor Antagonist
PCS1055 dihydrochloride is a selective and competitive antagonist of the muscarinic M4 receptor, with an IC50 value of 18.1 nM and a Kd of 5.72 nM. This compound effectively inhibits the binding of the radioligand [3H]-NMS to the M4 receptor, displaying a Ki of 6.5 nM. PCS1055 dihydrochloride demonstrates over 100-fold selectivity against M1, M3, and M5 receptors, and 30-fold selectivity at the M2 receptor. Additionally, it serves as a potent acetylcholinesterase inhibitor, with IC50 values of 22 nM and 120 nM for electric eel and human AChE, respectively, highlighting its potential for various neurological research applications. -
mAChR 4 Antagonist
PCS1055 is a selective competitive antagonist of the muscarinic M4 receptor, exhibiting an IC50 of 18.1 nM and a Kd of 5.72 nM. It effectively inhibits radioligand [3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. Additionally, PCS1055 demonstrates inhibitory activity against acetylcholinesterase (AChE), with IC50 values of 22 nM for electric eel AChE and 120 nM for human AChE. This compound is valuable for research focused on muscarinic receptor signaling and cholinergic modulation. -
AChE/mAChR Antagonist
CI-1002, a potent antagonist of acetylcholinesterase (AChE) and muscarinic acetylcholine receptors (mAChR), is utilized in neuroscience research. Its ability to inhibit AChE activity makes it particularly valuable for investigating the underlying mechanisms of cognitive dysfunction associated with Alzheimer’s disease. CI-1002 serves as a crucial tool for studying neurodegenerative processes and potential therapeutic strategies. -
Muscarinic M2 Acetylcholine Receptor Antagonist
Gallamine is a selective allosteric antagonist of the muscarinic M2 acetylcholine receptor, exhibiting an EC50 value of 130 nM in promoting the dissociation of [3H]NMS from porcine muscarinic M2 receptors. Additionally, it serves as an acetylcholinesterase inhibitor with varying IC50 values against different isoforms: 1070 μM for EeAChE, 1480 μM for hAChE, and 235 μM for hBChE. Gallamine is known to elevate levels of free norepinephrine and is utilized in research exploring muscle relaxation and pharmacological modulation of cholinergic signaling. -
Pro-cholinergic Agent
Deanol pidolate is an orally active pro-cholinergic agent that enhances cognitive function by promoting the release of acetylcholine (ACh), while minimizing the side effects commonly associated with cholinesterase inhibitors. It has demonstrated the ability to mitigate the negative impacts of scopolamine on long-term memory, facilitating a quicker recovery to baseline memory performance. Deanol pidolate is particularly useful in research applications related to Alzheimer's disease and other cognitive disorders. -
Stable Isotope
Itopride-d6 hydrochloride is a deuterium-labeled derivative of Itopride hydrochloride that serves as a stable isotope. Itopride functions as a gastroprokinetic agent by inhibiting acetylcholinesterase (AChE) and antagonizing dopamine D2 receptors. This compound is valuable for studies investigating gastrointestinal motility and neurotransmitter interactions, as well as for tracing and quantifying its metabolic pathways in biological research. -
Phosmet Metabolite
Phosmet oxon is a potent metabolite of phosmet, functioning primarily as a cholinesterase inhibitor. This compound exhibits significant neurotoxic activity, making it relevant in studies investigating insecticidal mechanisms and their effects on cholinergic signaling pathways. Phosmet oxon's utility extends to research on pesticide metabolism and its implications for environmental toxicology and safety assessments. -
Corydaline Metabolite
Isocorybulbine is a primary metabolite of Corydaline, produced in human liver microsomes and liver cells. It exhibits significant biological activities, including anti-acetylcholinesterase and anti-allergic effects. This compound is valuable for metabolic studies of Corydaline, contributing to research in pharmacology and potential therapeutic applications. -
AChE Inhibitor
Donepezil N-oxide is an acetylcholinesterase (AChE) inhibitor derived from Donepezil. It exhibits significant biological activity by inhibiting AChE in human erythrocytes, which is crucial for regulating acetylcholine levels in neurological pathways. This reagent is utilized in research focused on Alzheimer's disease and other cognitive disorders where modulation of cholinergic transmission is a key area of investigation. -
Disulfoton Oxidation Metabolite
Demeton-S sulfone is the oxidative metabolite of the organophosphorus insecticide Disulfoton, primarily targeting acetylcholinesterase. This compound exhibits significant acetylcholinesterase inhibition, which is essential for studying neurotoxic effects related to organophosphate exposure. It serves as a crucial reagent for evaluating the biochemical pathways of organophosphate metabolism and understanding their environmental and health impacts. -
Pesticide Metabolite
Malaoxon is a pesticide metabolite that serves as an inhibitor of acetylcholinesterase, impacting neurotransmitter regulation. This compound has been shown to induce cellular death in cultured human pulmonary cells, making it relevant for studies on pulmonary toxicity and its underlying mechanisms. Its application extends to research focused on the toxicological effects of pesticide exposure in human respiratory systems. -
Cholinesterase (ChE) Inhibitor
N-Desmethyl Galanthamine is a potent cholinesterase inhibitor, specifically targeting acetylcholinesterase (AChE) with an IC50 value of 2.76 μM. As a metabolite of Galanthamine, it holds significant relevance in neuropharmacological research. This compound is utilized in studies related to Alzheimer's disease, providing insights into therapeutic strategies aimed at enhancing cholinergic transmission. -
Aldicarb Metabolite
Aldicarb sulfoxide is a metabolite of aldicarb that primarily interacts with glutathione-linked enzymes in CHO-K1 cells. This compound exhibits inhibitory activity against cholinesterase (ChE) and carboxylesterase (CaE), with an IC50 of 10 μM in zebrafish models. Its mechanism of action and biological activity make it a valuable tool for research on neurotoxicology and enzymatic regulation. -
AChE Inhibitor
3-Hydroxycarbofuran is a reversible inhibitor of acetylcholinesterase (AChE), acting primarily by competing with acetylcholine at the enzyme's active site. This compound serves as a significant metabolite of Carbofuran and exhibits notable biological activity in the modulation of cholinergic signaling. It is utilized in research related to neurobiology, toxicology, and pesticide biochemistry, providing insights into the effects of AChE inhibition on synaptic transmission and potential neurotoxic mechanisms. -
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. -
Stable Isotope
Dibucaine-d9 hydrochloride is a deuterium-labeled derivative of Dibucaine hydrochloride, primarily functioning as a sodium channel inhibitor. This compound exhibits strong inhibition of serum cholinesterase (SChE) activity, making it valuable in pharmacological studies related to analgesia and local anesthesia. Its stable isotope labeling facilitates advanced metabolic research and provides insights into drug metabolism and distribution. -
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. -
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. -
AChE/BuChE Inhibitor
Ipidacrine hydrochloride is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), with IC50 values of 1 μM and 1.9 μM, respectively. This compound also acts as a partial agonist at M2-cholinergic receptors and exhibits reversible cholinesterase inhibition. Ipidacrine hydrochloride facilitates neuromuscular transmission and demonstrates moderate analgesic properties. It shows promise in preclinical models for various conditions, including Alzheimer’s disease, ischemic stroke, facial nerve neuropathy, and diabetes-associated erectile dysfunction, highlighting its potential in investigating cholinergic system-related disorders. -
Sodium Channel Inhibitor
Dibucaine hydrochloride is a sodium channel inhibitor that effectively blocks the influx of sodium ions, thereby preventing the propagation of action potentials in excitable tissues. This compound exhibits potent activity as an anesthetic and is utilized in various research applications, including studies of nerve conduction and muscle excitability. Additionally, it serves as a significant inhibitor of serum cholinesterase, contributing to its utility in pharmacological investigations and the development of anesthetic protocols. -
AchE Inhibitor/NMDAR Antagonist
Memagal is a potent acetylcholinesterase (AChE) inhibitor with an IC50 of 1.16 nM and acts as an N-methyl-D-aspartate receptor (NMDAR) antagonist with a Ki of 4.6 μM. This compound effectively inhibits neurotoxicity triggered by NMDA, demonstrating an IC50 value of 0.28 nM. Memagal serves as a valuable tool for research focused on Alzheimer's disease, providing insights into mechanisms and potential therapeutic approaches. -
AChE Reversible Inhibitor
Asoxime dichloride is a reversible inhibitor of acetylcholinesterase (AChE) that functions as a thiosemicarbazone-based antidote. Its primary mechanism involves reactivating AChE that has been inhibited by nerve agents, thus restoring cholinergic nerve function. Additionally, Asoxime dichloride enhances muscle function in the presence of poisoning without reactivating AChE and acts as an antagonist to acetylcholine receptors, including nicotinic and α7 nAChRs. Due to its immunomodulatory properties, Asoxime dichloride can also enhance the immune response of the nervous system, making it valuable in neuropharmacological research. -
AChE Reversible Inhibitor
Asoxime dimesylate is a reversible inhibitor of acetylcholinesterase (AChE) that serves as a thiosemicarbazone-based antidote. Its primary mechanism of action involves reactivating AChE inhibited by nerve agents, thus restoring cholinergic nerve function. Additionally, Asoxime dimesylate has been shown to significantly restore muscle function compromised by poisoning without the reactivation of AChE. It also acts as an antagonist at acetylcholine receptors, including nicotinic receptors and α7 nAChR, and demonstrates potential as an immunomodulator, enhancing immune responses in the nervous system. This compound is valuable for research in neuropharmacology and toxicology. -
nAChR Inhibitor
Ferulamide is a derivative of ferulic acid that acts as a competitive inhibitor of nicotinic acetylcholine receptors (nAChRs). It exhibits significant anticholinesterase activity, making it a valuable tool for studying cholinergic signaling pathways. This compound is useful in research related to neurodegenerative diseases and the modulation of synaptic transmission. -
AChE/nAChR Inhibitor
AChE/nAChR-IN-1 is a dual inhibitor targeting acetylcholinesterase (AChE) and nicotinic acetylcholine receptors (nAChR). This compound exhibits potent toxicity and larvicidal activity against Culex pipiens larvae, with an LC50 of 4 ng/mL. AChE/nAChR-IN-1 is utilized in research focused on controlling mosquito populations and studying mosquito-borne diseases. -
AChE Inhibitor
Sinapine is an acetylcholinesterase (AChE) inhibitor derived from cruciferous seeds. This compound demonstrates a range of biological activities, including anti-inflammatory, antioxidant, anti-tumor, anti-angiogenic, and radio-protective effects. Sinapine is instrumental in research targeting neurodegenerative disorders such as Alzheimer's disease, myasthenia gravis, ataxia, and Parkinson’s disease, making it a valuable tool for advancing scientific understanding in these areas.
