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]
-
AChE Related Products (455)
Related Products (455)
-
AChE-IN-106
0 ImagesCat. No.: HY-181119AChE-IN-106 is an AChE inhibitor. AChE-IN-106 shows no obvious cytotoxicity at low concentrations. AChE-IN-106 can be used for the research of Alzheimer's disease.
-
Magnotriol B
0 ImagesCat. No.: HY-N15710CAS No.: 92829-71-5Magnotriol B is a cholinesterase inhibitor with IC50 values of 12.63 nM and 14.5 nM against AChE and BChE, respectively. Magnotriol B also exhibits significant NO inhibitory activity with an IC50 of 2.02 μM. Magnotriol B can be used in the research of neurodegenerative and inflammatory diseases.
-
AChE-IN-75
0 ImagesCat. No.: HY-162915AChE-IN-75 (N-(2′-methyl)allylnorgalanthamine) is an AChE inhibitor. AChE-IN-75 can be used in Alzheimer's disease research.
-
Picfeltarraegenin X
0 ImagesCat. No.: HY-N2219CAS No.: 1391826-61-1Picfeltarraenin X, a triterpenoid isolated, is an AChE inhibitor.
-
CAI/II-IN-5
0 ImagesCat. No.: HY-147955CAS No.: 2428389-67-5CAI/II-IN-5 (compound MZ8) is a potent hCA I and hCA II (human carbonic anhydrase isoenzymes I and II) inhibitor, with IC50 values of 37.88 and 45.23 nM, respectively. CAI/II-IN-5 also shows inhibition profile against α-Glycosidase and AChE, with IC50 values of 48.98 and 420.14 nM, respectively. CAI/II-IN-5 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy.
-
H3R antagonist 4
0 ImagesCat. No.: HY-162812H3R antagonist 4 (compound 11L) was a dual inhibitor of cholinesterase and histamine receptor (H3R), with corresponding IC50 of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible) and 1.09 nM (H3R) , respectively. H3R antagonist 4 inhibited the aggregation of Aβ1-42 induced by itself and Cu2+ (95.48% and 88.63%) , and degraded the Aβ1-42 fibrils induced by itself and Cu2+ (80.16% and 89.30%) . H3R antagonist 4 chelate biometals such as Cu2+, Zn2+, Al3+, and Fe2+. H3R antagonist 4 significantly reduced tau protein hyperphosphorylation induced by Aβ1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimer's disease induced by scopolamine (HY-N0296) .
-
Multitarget AD inhibitor-2
0 ImagesCat. No.: HY-158978Multitarget AD inhibitor-2 (Compound VN-19) is a multitargeting inhibitor acetylcholinesterase (AChE, IC50=0.14 μM), butyrylcholinesterase (BChE, IC50=11.6 μM), monoamine oxidase B (MAO B, IC50=0.45 μM). Multitarget AD inhibitor-2 inhibits self-induced aggregation of amyloid beta protein Aβ1-42 (inhibition rate is 47.3% at 20 μM), and downregulates the level of ROS in SH-SY5Y (80 inhibition rate at 25 μM). Multitarget AD inhibitor-2 ameliorates the cognitive decline in Scopolamine (HY-N0296)-induced Alzheimer’s Disease zebrafish models.
-
hAChE/hBACE-1-IN-1
0 ImagesCat. No.: HY-149287hAChE/hBACE-1-IN-1 (compounds 5d) is an orally active inhibitor of hAChE with blood-brain permeability. hAChE/hBACE-1-IN-1 inhibits hAChE and hBACE-1 with IC50 values of 0.076 and 0.23 μM, respectively. hAChE/hBACE-1-IN-1 inhibits Aβ1-42 aggregation and improves mouse learning and memory ability. hAChE/hBACE-1-IN-1 can be used to research in Alzheimer's disease.
-
AChE-IN-98
0 ImagesCat. No.: HY-177798CAS No.: 307535-32-6AChE-IN-98 (Compound 26) is an AChE inhitibor, with an IC50 value of 7.3 μM for ee AChE. AChE-IN-98 is also a Coumarin (HY-N0709) derivative. AChE-IN-98 can be used in the research of Alzheimer's disease.
-
Desoxypeganine
0 ImagesDesoxypeganine (Deoxypeganine), 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 can be used for alcohol abuse research.
-
Trimyristin--d15
0 ImagesCat. No.: HY-N2511SCAS No.: 1219804-94-0Trimyristin--d15 is the d15-labeled Trimyristin (HY-N2511). Trimyristin is an orally active compound. Trimyristin can be isolated from the seeds of nutmeg (Myristica fragrans). Trimyristin inhibits the activities of acetylcholinesterase (AChE), ACP and ALP, with IC50 values of 0.11, 0.16 and 0.18 mM, respectively. Trimyristin exerts competitive-noncompetitive inhibition on acetylcholinesterase, uncompetitive inhibition on ACP, and competitive/noncompetitive inhibition on ALP. Trimyristin restores the downregulated acetylcholinesterase concentration in the cerebral cortex of rats exposed to sodium arsenite. Trimyristin can be used in studies related to fascioliasis and neurotoxicity.
-
Multitarget AD-IN-5
0 ImagesCat. No.: HY-181041Multitarget AD-IN-5 (Compound 20), 9-Aminoacridine (HY-B1422) derivative, is a neuroprotective agent. Multitarget AD-IN-5 shows IC50 values of 0.614, 0.448, 3.73 and 1.55 μM for hAChE, hBChE, hMAO-A and hMAO-B. Multitarget AD-IN-5 can reduce length and diameter of Aβ42 fibers, and decrease the number of fibers per unit area. Multitarget AD-IN-5 can be used for research of Alzheimer's disease.
-
BChE-IN-48
0 ImagesCat. No.: HY-180146BChE-IN-48 (Compound 12a) is a BChE inhibitor that can cross the blood-brain barrier with IC50 values for eqBChE and huBChE of 1.3 and 0.95 μM respectively. BChE-IN-48 exhibits an IC50 value for eeAChE of 8.6 μM. BChE-IN-48 exhibits significant neuroprotective activity in cell damage and significantly improves cognitive impairment in mouse models. BChE-IN-48 can be used for research on Alzheimer's disease.
-
AJ-4
0 ImagesCat. No.: HY-184742AJ-4 is an orally active, blood-brain barrier-permeable GSK-3β/AChE inhibitor, with an IC50 of 4.7 nM against GSK-3β and 2.97 μM against AChE. AJ-4 increases the level of phosphorylated GSK-3β and reduces the expression of Amyloid-β and phosphorylated Tau. AJ-4 improves scopolamine-induced learning and memory impairment and alleviates hippocampal neuron damage in AD mice. AJ-4 can be used for the research of Alzheimer's disease.
-
AChE/BChE-IN-12
0 ImagesCat. No.: HY-149211AChE/BChE-IN-12 (compound 10b), a 3,5-dimethoxy analogue, is a potent AChE, BChE, and β-secretase-1 (BACE-1) inhibitor, with IC50 values of 2.57, 3.26, and 10.65 μM, respectively. AChE/BChE-IN-12 crosses the blood-brain barrier via passive diffusion and inhibits the self-aggregation of amyloid-β monomers. AChE/BChE-IN-12 can be used for Alzheimer’s disease (AD) research.
