AChE
Acetylcholinesterase (AChE) is the principal cholinergic enzyme that rapidly hydrolyzes acetylcholine at cholinergic synapses and neuromuscular junctions, thereby terminating neurotransmission and maintaining synaptic signaling fidelity[1]. Mechanistically, AChE regulates cholinergic pathway activity through efficient acetylcholine clearance, a process that is essential for normal neuronal communication and neuromuscular function[1]. Beyond its catalytic role, AChE displays multiple molecular forms and has been implicated in cellular interactions, neuronal activity modulation, and pathological states, supporting broader biological functions outside classical neurotransmission[1]. In neurodegenerative disease models, particularly Alzheimer’s disease (AD), altered cholinergic signaling is closely associated with cognitive impairment, and cholinesterase inhibition remains a major symptomatic therapeutic strategy[2][3]. Compared with the related isoform butyrylcholinesterase (BChE), AChE is the predominant cholinesterase in the brain and plays a primary role in synaptic acetylcholine hydrolysis, whereas BChE may compensate when AChE activity is reduced and exhibits distinct pathological changes during AD progression[3][4]. For experimental and translational applications, reversible and dual AChE/BChE inhibitors, including rivastigmine, are widely used to enhance cholinergic neurotransmission and investigate mechanisms underlying neurodegeneration and cognitive dysfunction[2][3].
References:
- [1]. Massoulié J, et al. Structure and functions of acetylcholinesterase and butyrylcholinesterase. Prog Brain Res. 1993;98:139-46. [Content Brief]
- [2]. Walczak-Nowicka ŁJ, et al. Acetylcholinesterase Inhibitors in the Treatment of Neurodegenerative Diseases and the Role of Acetylcholinesterase in their Pathogenesis. Int J Mol Sci. 2021 Aug 27;22(17):9290. [Content Brief]
- [3]. Nordberg A, et al. A review of butyrylcholinesterase as a therapeutic target in the treatment of Alzheimer's disease. Prim Care Companion CNS Disord. 2013;15(2):PCC.12r01412. [Content Brief]
- [4]. Geula C, et al. Butyrylcholinesterase, cholinergic neurotransmission and the pathology of Alzheimer's disease. Drugs of Today (Barcelona, Spain : 1998). 2004 Aug;40(8):711-721. [Content Brief]
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AChE Related Products (445)
Related Products (445)
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SCR1693
0 ImagesCat. No.: HY-165341CAS No.: 1442559-20-7SCR1693 is a selective, reversible, orally active and noncompetitive inhibitor of AChE (IC50 = 0.68 μM) as well as a calcium channel blocker. SCR1693 reduces tau phosphorylation levels, and inhibits the generation and release of Aβ. SCR1693 restores insulin signaling and improves cognitive deficits. SCR1693 can be used for the study of Alzheimer's disease, especially which complicated with type 2 diabetes mellitus.
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MAO-A/B-IN-3
0 ImagesCat. No.: HY-162606CAS No.: 315210-31-2MAO-A/B-IN-3 (Compound 12) stands out as a key dual MAO-AChE inhibitor, displaying excellent multi-target efficacy against MAO-A, MAO-B, and AChE with IC50 values of 67 nM, 29 nM, and 1370 nM respectively. MAO-A/B-IN-3 is adept at altering the A site (hydrophobic ring) and C site (semicarbazone chain) within ketone amine-based MTDLs to bolster the inhibitory potential against MAO-A/B while notably diminishing activity against AChE. MAO-A/B-IN-3 is poised for research applications in the field of neurodegenerative diseases.
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TZ3O
0 ImagesCat. No.: HY-155822Purity: 98.17%TZ3O is an anticholinergic agent with neuroprotective effects. TZ3O inhibits acetylcholinesterase (AChE) activity in human plasma with an IC50 of 304.5 μM. TZ3O can improve memory impairment and cognitive decline in rats in the Scopolamine (HY-N0296)-induced Alzheimer-type model. TZ3O could be used in Alzheimer’s research.
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AChE-IN-52
0 ImagesCat. No.: HY-163126CAS No.: 2214210-63-4AChE-IN-52 (compound A6) is an acetylcholinesterase (AChE) inhibitor. AChE-IN-52 shows antitumor efficacy, especially against breast cancer MCF-7 cells. AChE-IN-52 significantly disrupts the amino acid metabolism and inhibits migration of MCF-7. AChE-IN-52 plays anticancer role by regulating Best1 and HIST1H2BJ.
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BChE-IN-15
0 ImagesCat. No.: HY-152232CAS No.: 3060336-91-3BChE-IN-15 (Compound 6) is a pseudo-irreversible and covalent BChE inhibitor with an IC50 of 1.76 nM against hBChE .
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1,10-Bis(pyridinium)decane
0 ImagesSynonyms: Decamethylenebispyridinium dibromide1,10-Bis(pyridinium)decane (Decamethylenebispyridinium dibromide) is an acetylcholinesterase (AChE) inhibitor with an IC50 of 25.8 nM. 1,10-Bis(pyridinium)decane acts as a bis-quaternary ligand that bridges the enzyme's catalytic site and peripheral site via its two pyridinium groups. 1,10-Bis(pyridinium)decane can be used for the research of alzheimer's disease.
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LINS05414
0 ImagesCat. No.: HY-181597LINS05414 is a histamine H3 receptor ligand with antiCholinesterase and metal chelating activities. LINS05414 exhibits inhibitory activity against acetylcholinesterase (pIC50 = 4.03) and butyrylcholinesterase (pIC50 = 3.83), with a pKi of 6.37 for human histamine H3 receptors. LINS05414 chelates copper ions, ferrous ions and ferric ions. LINS05414 regulates the release of neurotransmitters. LINS05414 can be used in the research of neurodegenerative diseases.
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AChE-IN-102
0 ImagesCat. No.: HY-180243AChE-IN-102 (compound C8) is a potent, selective and competitive AChE inhibitor with a Ki of 7.55 nM and an IC50 of 15.25 nM. AChE-IN-102 shows selectivity over BuChE (IC50 = 21.15 nM, b>Ki = 6.17 nM). AChE-IN-102 can be used for Alzheimer’s disease research.
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(+)-(3S)-ψ-Ribalinine
0 ImagesCat. No.: HY-N21824CAS No.: 155158-70-6(+)-(3S)-ψ-Ribalinine is an inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with an IC50 of 62.46 μM against electric eel acetylcholinesterase and an IC50 of 150.04 μM against equine butyrylcholinesterase. (+)-(3S)-ψ-Ribalinine can be used for the research of neurological disorders.
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p38α-IN-13
0 ImagesCat. No.: HY-114422CAS No.: 3077831-12-7p38α-IN-13 is p38α MAPK, BChE and AChE inhibitor with IC50 values of 5.79, 16.24, 51.8 µM for p38α MAP, hBChE, hAChE, respectively. p38α-IN-13 has the potential for the research of Alzheimer’s disease.
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AChE-IN-59
0 ImagesCat. No.: HY-157978CAS No.: 2957916-86-6AChE-IN-59 (compounds 3b) is an AChE inhibitor, with an IC50 value of 0.05 μM. AChE-IN-59 can inhibit the aggregation of Aβ1-42, protect nerve cells and penetrate the blood-brain barrier well. AChE-IN-59 can be used for the research of Alzheimer's disease (AD).
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Desoxypeganine hydrochloride
0 ImagesCat. No.: HY-108048ACAS No.: 61939-05-7Synonyms: Deoxypeganine hydrochloride; Deoxyvasicine hydrochlorideDesoxypeganine (Deoxypeganine) hydrochloride, an alkaloid, is a potent and orally active cholinesterase (BChE and AChE) and selective MAO-A inhibitor, with IC50 values of 2, 17, and 2 μM, respectively. Desoxypeganine hydrochloride can be used for alcohol abuse research.
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AChE/BChE-IN-3 hydrochloride
0 ImagesCat. No.: HY-146663ACAS No.: 2410992-69-5
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MR2938
0 ImagesCat. No.: HY-149087CAS No.: 1044870-65-6
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Icopezil
0 ImagesCat. No.: HY-105157CAS No.: 145508-78-7Synonyms: CP-118954Icopezil (CP-118954) is an orally active, selective AchE inhibitor with an IC50 of 0.33 nM. Icopezil increases acetylcholine levels in the brain and striatum of mammals, induces centrally mediated tremors and peripherally mediated salivation, and improves working memory performance in aged dogs. Icopezil serves as a parent compound for radioiodine-labeled acetylcholinesterase imaging agents. Icopezil is applicable to research related to Alzheimer's disease.
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Pitofenone
0 ImagesCat. No.: HY-105853CAS No.: 54063-52-4Pitofenone, a spasmolytic compound, inhibits the acetylcholinesterase (AChE) activity from bovine erythrocytes and from electric eel with Kis of 36 and 45 μM, respectively.
