AChE

Cat. No.

A61276

CAS No.

20725-03-5

Fustin

Synonyms: (±)-Fustin; 3,7,3'; 4'-Tetrahydroxyflavanone

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.

Cat. No.

A61280

CAS No.

83654-05-1

RHC 80267

Synonyms: U-57908

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.

Cat. No.

A61499

CAS No.

23513-72-6

Deanol pidolate

Synonyms: V0191; DMAE pidolate; DMAE PCA

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.

Cat. No.

A62550

CAS No.

469-22-7

Eseroline

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.

Cat. No.

A64460

CAS No.

2447589-08-2

COX-2-IN-22

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.

Cat. No.

A65846

CAS No.

36001-47-5

Vescalagin

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.

Cat. No.

A66712

CAS No.

224445-12-9

Bis(7)-tacrine dihydrochloride

Bis(7)-tacrine dihydrochloride is a dimeric inhibitor of acetylcholinesterase (AChE) and a potent antagonist of GABAA receptors. This compound exhibits neuroprotective properties by preventing glutamate-induced neuronal apoptosis through NMDA receptor blockade. Bis(7)-tacrine dihydrochloride is valuable for research applications related to Alzheimer's disease and other neurological disorders.

Cat. No.

A67334

CAS No.

1402938-19-5

Memagal

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.

Cat. No.

A67576

CAS No.

34433-31-3

Asoxime dichloride

Synonyms: HI-6

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.

Cat. No.

A67664

CAS No.

144252-71-1

Asoxime dimesylate

Synonyms: HI-6 dimesylate

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.

Cat. No.

A67675

CAS No.

61012-31-5

Ferulamide

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.

Cat. No.

A67753

CAS No.

59417-09-3

AChE/nAChR-IN-1

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.

Cat. No.

A67789

CAS No.

18696-26-9

Sinapine

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.

Cat. No.

A67834

CAS No.

122-30-5

Sinapine hydroxide

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.

Cat. No.

A68030

CAS No.

62732-44-9

Ipidacrine

Synonyms: NIK-247 free base; Amiridine free base

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.

Cat. No.

A68221

CAS No.

90043-86-0

Ipidacrine hydrochloride

Synonyms: NIK-247; Amiridine

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.

Cat. No.

A68429

CAS No.

61-12-1

Dibucaine hydrochloride

Synonyms: Cinchocaine hydrochloride

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.

Cat. No.

A69482

CAS No.

93944-58-2

α-Amylase-IN-3

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.

Cat. No.

A69505

CAS No.

1038094-94-8

α-Amylase/α-Glucosidase-IN-7

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.

Cat. No.

A69568

CAS No.

523-88-6

Dibromsalicil

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.

Cat. No.

A69587

CAS No.

23560-59-0

Heptenophos

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.

Cat. No.

A70157

CAS No.

41303-74-6

N-Desmethyl Galanthamine

Synonyms: Norgalanthamine

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.

Cat. No.

A70611

CAS No.

16655-82-6

3-Hydroxycarbofuran

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.

Cat. No.

A70655

CAS No.

3735-33-9

Phosmet oxon

Synonyms: Imidoxon; Oxoimidan

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.

Cat. No.

A70830

CAS No.

120013-84-5

Donepezil N-oxide

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.