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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
AChE Inhibitor/GABAA Receptor Antagonist
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. -
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. -
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. -
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. -
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. -
CerS6 Inhibitor, Ceramide Synthesis Inhibitor, Acetylcholinesterase Inhibitor
FF-C1 is a non-competitive inhibitor of Ceramide Synthase 6 (CerS6), exhibiting an IC50 of 7.89 μM. By inhibiting intestinal CerS6, FF-C1 effectively lowers serum ceramide levels, offering protective effects against metabolic dysfunction-associated steatohepatitis. This compound is also reported to inhibit acetylcholinesterase, highlighting its potential applications in studying metabolic disorders and neurodegenerative diseases. -
Cholinesterase (ChE) Inhibitor
Vomifoliol is a cholinesterase (ChE) inhibitor that exhibits significant antiacetylcholinesterase activity, comparable to that of abscisic acid (ABA). Additionally, this compound shows moderate antileishmanial activity, making it a valuable tool for research into neurodegenerative disorders and parasitic infections. Its unique structure, featuring a modified 2,4-pentadiene side chain, further contributes to its biological activity, offering potential applications in pharmacological studies. -
Acetylcholinesterase Inhibitor
Trimethylammonium chloride is a non-competitive inhibitor of acetylcholinesterase, targeting the enzymatic activity responsible for the hydrolysis of the neurotransmitter acetylcholine. By reversibly blocking the deacetylation process of acetylcholinesterase, this reagent plays a critical role in studies related to neurobiology and the modulation of synaptic transmission. Its application extends to research investigating cholinergic signaling pathways and potential therapeutic strategies for neurological disorders. -
Monoamine Oxidase Inhibitor
MAO-B-IN-2 is a selective and competitive inhibitor of monoamine oxidase B (MAO-B) with an IC50 value of 0.51 μM, and it also inhibits butyrylcholinesterase (BChE) with an IC50 of 7.00 μM. This compound plays a significant role in studying neurodegenerative disorders by modulating monoamine metabolism, making it valuable for research into conditions such as Parkinson's disease and Alzheimer's disease. Its specificity for MAO-B makes it an important tool for exploring therapeutic pathways involving neurotransmitter regulation. -
NF-κB Inhibitor
6-O-p-Hydroxybenzoylglutinoside is a selective NF-κB inhibitor that effectively suppresses TNF-α-activated NF-κB transcriptional activity, with an IC50 of 52.78 μM. This compound demonstrates targeted biological activity without significantly inhibiting soluble epoxide hydrolase (sEH), acetylcholinesterase (AChE), or butyrylcholinesterase (BChE). Isolated from the seeds of Catalpa bungei (Manchurian catalpa), 6-O-p-Hydroxybenzoylglutinoside is valuable for research applications focused on inflammation and signal transduction pathways. -
Aβ Aggregation Inhibitor
Aβ-IN-5 is a potent Aβ aggregation inhibitor, demonstrating oral bioavailability. It effectively inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) with IC50 values of 21.29 μM and 1.32 μM, respectively. This compound exhibits significant neuroprotective effects while maintaining low neurotoxicity, making it a valuable tool for research on neurodegenerative diseases, particularly Alzheimer’s disease. -
Cholinesterase (ChE) Inhibitor
hAChE/Aβ1-42-IN-1 is a potent cholinesterase (ChE) inhibitor that effectively inhibits human acetylcholinesterase (hAChE) and prevents the aggregation of Aβ1-42 peptides. This compound demonstrates favorable relative safety in HepG2 cell lines and exhibits excellent blood-brain barrier (BBB) penetration, exhibiting a wide safety margin. hAChE/Aβ1-42-IN-1 is a valuable tool for research focusing on Alzheimer's disease (AD) and related neurodegenerative conditions. -
BuChE Inhibitor
BuChE-IN-6 is a potent and selective inhibitor of butyrylcholinesterase (BuChE), exhibiting IC50 values of 0.46 μM and 0.51 μM for equine and human BuChE, respectively. This compound also demonstrates the ability to inhibit self-aggregation of amyloid-beta 42 (Aβ42), making it a valuable tool for research related to neurodegenerative diseases. Its unique properties support investigations into cholinergic dysfunction and the pathogenesis of Alzheimer's disease. -
hAChE/hBACE Inhibitor
hAChE/hBACE-1-IN-4 is a quinazoline derivative that functions as a dual inhibitor of human acetylcholinesterase (hAChE) and human β-site amyloid precursor protein cleaving enzyme 1 (hBACE-1). It exhibits potent inhibitory activity with IC50 values of 0.283 μM for hAChE and 0.231 μM for hBACE-1. This compound demonstrates the ability to inhibit amyloid-beta (Aβ) aggregation and shows favorable properties such as non-neurotoxicity, blood-brain barrier permeability, and oral bioavailability. hAChE/hBACE-1-IN-4 is suitable for research applications related to Alzheimer's disease. -
AChE Inhibitor
AChE-IN-19 is a potent inhibitor of acetylcholinesterase (AChE), exhibiting an IC50 value of 0.56 μM. This compound also demonstrates the ability to inhibit amyloid beta (Aβ) aggregation, contributing to its neuroprotective properties. AChE-IN-19 has been shown to exert minimal toxicity on SH-SY5Y neuronal cells, making it a valuable tool for research applications related to Alzheimer's disease. -
Amyloid-β Inhibitor
AChE/Aβ-IN-5 is a bifunctional inhibitor that targets acetylcholinesterase (AChE) and reduces the auto-induced aggregation of amyloid-β (Aβ) peptides. This compound has demonstrated the ability to significantly ameliorate cognitive deficits induced by scopolamine and Aβ in murine models. It serves as a valuable tool for research into neurodegenerative diseases, particularly Alzheimer's disease, by providing insights into the mechanisms underlying cognitive impairment. -
AChE Inhibitor
Memoquin is an AChE inhibitor with significant anti-amyloid and antioxidant properties. It exhibits oral bioavailability and selectively inhibits BACE-1 and AChE, with IC50 values of 108 nM and 1.55 nM, respectively. Memoquin is noted for its ability to enhance cognitive function while preventing Aβ-induced neurotoxicity associated with oxidative stress. This compound is valuable for research into Alzheimer's disease and related neurodegenerative disorders. -
AChE Inhibitor
Phenserine tartrate is a selective, noncompetitive inhibitor of acetylcholinesterase (AChE) derived from Physostigmine. This compound has been shown to reduce the formation of β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ), key factors involved in Alzheimer's disease pathology. Phenserine tartrate has demonstrated potential in improving cognitive performance and may help slow the progression of Alzheimer's disease, making it a valuable tool for research in neurodegenerative disorders. -
ChE/Aβ1-42 Aggregation Inhibitor
ChE/Aβ1-42-IN-1 is a potent inhibitor of acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), and amyloid-beta peptide (Aβ1-42) aggregation, exhibiting IC50 values of 0.062 µM, 0.767 µM, and 1.227 µM, respectively. This compound demonstrates significant blood-brain barrier (BBB) penetration, making it a promising candidate for research into Alzheimer's disease. ChE/Aβ1-42-IN-1's multi-targeted mechanism positions it as a valuable tool for studying therapeutic strategies in neurodegenerative disorders. -
AChE Inhibitor
hAChE-IN-10 is a potent inhibitor of human acetylcholinesterase (AChE), demonstrating an IC50 of 6.34 nM. This compound exhibits significant antioxidant properties and effectively scavenges free radicals. Additionally, hAChE-IN-10 has been shown to inhibit Cu2+-induced aggregation of Aβ1-42, reduce amyloid plaque formation, and provide neuroprotective effects. It has also been linked to the improvement of cognitive deficits in mouse models induced by scopolamine, making it a valuable tool for studying neurodegenerative diseases and cognitive impairment. -
MAO-B Inhibitor
MAO-B-IN-50 is a selective inhibitor of monoamine oxidase B (MAO-B), demonstrating an IC50 value of 0.06 μM. This compound is effective in inhibiting the aggregation of amyloid-beta (Aβ40/42) and Tau proteins, with overall IC50 values near 1 μM. Additionally, MAO-B-IN-50 shows potent selective inhibition of acetylcholinesterase (AChE) with an IC50 of 1.78 μM. It is suitable for use in research related to Alzheimer's disease. -
AChE Inhibitor
AChE-IN-12 is a selective acetylcholinesterase (AChE) inhibitor that effectively penetrates the blood-brain barrier, exhibiting IC50 values of 0.41 μM for rat AChE and 1.88 μM for electric eel AChE. This compound also demonstrates antioxidant properties (ORAC = 3.3 eq), selectively chelates metals, and inhibits human monoamine oxidase B (MAO-B) with an IC50 of 8.8 μM. AChE-IN-12 significantly inhibits both self- and Cu2+-induced aggregation of Aβ1-42 and displays neuroprotective effects, making it a valuable tool for research related to Alzheimer’s disease. -
AChE/BuChE Inhibitor
AChE/BuChE-IN-3 is a dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), exhibiting IC50 values of 0.65 μM and 5.77 μM, respectively. This compound effectively inhibits the aggregation of amyloid beta peptide Aβ1-42 and demonstrates neuroprotective properties with minimal toxicity in SH-SY5Y cells. AChE/BuChE-IN-3 is suitable for research applications related to Alzheimer's disease, providing insight into cholinergic system modulation and potential therapeutic strategies. -
Aβ1-42/AChE Inhibitor
AChE-IN-59 is a potent acetylcholinesterase (AChE) inhibitor, displaying an IC50 value of 0.05 μM. This compound effectively inhibits the aggregation of amyloid-beta peptide Aβ1-42, offering protective effects on neuronal cells and demonstrating favorable penetration of the blood-brain barrier. AChE-IN-59 is a valuable tool for research focused on Alzheimer's disease and related neurodegenerative disorders. -
AChE Inhibitor
AP2238 is a dual-function acetylcholinesterase (AChE) inhibitor that demonstrates Ki values of 21.7 μM for human AChE and 48.9 μM for butyrylcholinesterase (BuChE). This compound effectively inhibits the pro-fibrotic interaction between the peripheral site of AChE and amyloid-beta (Aβ), as well as Aβ aggregation. AP2238 is primarily utilized in Alzheimer's disease research, contributing to studies focused on neurodegeneration and cholinergic dysfunction. -
AChE/BuChE Inhibitor
AChE/BuChE-IN-2 is a selective inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), demonstrating IC50 values of 0.72 μM and 0.16 μM, respectively. This compound exhibits non-competitive inhibition of AChE and effectively inhibits β-amyloid (Aβ) aggregation, with an IC50 of 62.52 μM. Notably, AChE/BuChE-IN-2 is capable of crossing the blood-brain barrier, making it a valuable tool for studying neurodegenerative conditions, such as Alzheimer's disease. -
BuChE Inhibitor
Multitarget AD inhibitor-1 is a selective and reversible inhibitor of butyrylcholinesterase (BuChE), exhibiting IC50 values of 7.22 μM for human BuChE and 1.55 μM for equine BuChE. This compound also inhibits β-secretase activity (IC50 = 41.60 μM) and demonstrates a strong capacity to inhibit amyloid β aggregation (IC50 = 3.09 μM) as well as tau aggregation. As a diphenylpropylamine derivative, it holds promise for multifunctional disease-modifying applications in Alzheimer’s research. -
AChE Inhibitor
hAChE-IN-3 is a potent acetylcholinesterase (AChE) inhibitor with demonstrated blood-brain barrier permeability. It exhibits significant inhibitory effects against butyrylcholinesterase (BuChE), monoamine oxidase B (MAO-B), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1), with IC50 values of 0.44, 0.08, 5.15, and 0.38 μM, respectively. Additionally, hAChE-IN-3 possesses antioxidant properties and metal chelating ability, enabling it to interact with peripheral anion sites and influence β-amyloid accumulation. This compound holds promise for advancing research in Alzheimer's disease and related neurodegenerative disorders. -
Multi-target Inhibitor
AChE-IN-63 is a multi-target inhibitor with a primary action as a selective inhibitor of human acetylcholinesterase (hAChE), exhibiting an IC50 of 0.103 μM. This compound also demonstrates inhibitory activity against human butyrylcholinesterase (hBChE) and human beta-site amyloid precursor protein cleaving enzyme 1 (hBACE-1) with IC50 values of 10 μM and 1.342 μM, respectively. AChE-IN-63 effectively inhibits Aβ aggregation, thereby preventing the formation and deposition of Aβ1-42. Due to its ability to penetrate the blood-brain barrier and oral bioavailability, it is primarily utilized in research related to Alzheimer's disease.
