1. Signaling Pathways
  2. Neuronal Signaling
  3. Cholinesterase (ChE)

Cholinesterase (ChE)

Cholinesterase (ChE) is a family of enzymes present in the central nervous system, particularly in nervous tissue, muscle and red cells, which catalyze the hydrolysis of the neurotransmitter acetylcholine into choline and acetic acid, a reaction necessary to allow a cholinergic neuron to return to its resting state after activation. It is one of many important enzymes needed for the proper functioning of the nervous systems of humans.

There are two types: acetylcholinesterase (AChE, acetylcholine hydrolase) and butyrylcholinesterase (BChE, acylcholine acylhydrolase), also known as nonspecific cholinesterase or pseudocholinesterase. AChE is primarily found in the blood on red blood cell membranes, in neuromuscular junctions, and in neural synapses, while BChE is produced in the liver and found primarily in plasma. The difference between the two types of cholinesterase is their relative preferences for substrates: AChE hydrolyzes acetylcholine faster while BChE hydrolyzes butyrylcholine faster.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N13902
    Arisugacin B
    Inhibitor
    Arisugacin B is a potent, orally active and selective acetylcholinesterase (AChE) inhibitor.
    Arisugacin B
  • HY-17368S1
    (Rac)-Rivastigmine-d6
    Inhibitor
    (Rac)-Rivastigmine-d6 is a labelled racemic Rivastigmine. Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease.
    (Rac)-Rivastigmine-d<sub>6</sub>
  • HY-163662
    AE027
    Inhibitor
    AE027 is a potent inhibitor against both WT and resistant mutation F348Y AChE with the IC50 values of 10 and 43 μM, respectively.
    AE027
  • HY-W027553R
    Ipidacrine (Standard)
    Inhibitor
    Ipidacrine (Standard) is the analytical reference standard of Ipidacrine. This product is used for research and analytical applications. Ipidacrine is orally active and blood-brain-barrier-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K+ and Na+-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases.
    Ipidacrine (Standard)
  • HY-105327R
    P11149 (Standard)
    Inhibitor
    P11149 (Standard) is the analytical standard of P11149 (HY-105327). This product is intended for research and analytical applications. P11149 is a competitive, BBB-penetarated weakly, orally active and selective inhibitor of AChE. P11149 exhibits an IC50 of 1.3 μM for rat BChE/AChE. P11149, a Galanthamine derivative, demonstrates central cholinergic activity, behavioral efficacy and safety. P11149 is used in the study for Alzheimer's disease.
    P11149 (Standard)
  • HY-N15450
    Undulatine
    Inhibitor
    Undulatine is a potent AChE inhibitor with an IC50 of 7.4 μM. Undulatine is able to cross the BBB by passive permeation and can be used in the study of Alzheimer’s disease.
    Undulatine
  • HY-N3185
    N-Methylcalycinine
    Inhibitor
    N-Methylcalycinine is a nature product with AChE inhibitory activity. N-Methylcalycinine can be isolated from the roots of Stephania epigaea. N-Methylcalycinine can be used for the research of asthma, cancer, dysentery, fever, hyperglycemia, intestinal complaints, inflammation, sleep disturbances, tuberculosis and so on.
    N-Methylcalycinine
  • HY-107825R
    Flavonol (Standard)
    Inhibitor
    Flavonol (Standard) is the analytical standard of Flavonol. This product is intended for research and analytical applications. Flavonol is a cholinesterase (ChE) inhibitor, with an IC50 value of 120 μM and a Ki value of 74 μM. Flavonol has antioxidant, free radical-scavenging, antibacterial properties, and immune modulation functions. Flavonol inhibits the PriA helicase of Staphylococcus aureus. Flavonol can suppress the production of NO in LPS-activated RAW 264.7 cells by inhibiting the expression of the iNOS enzyme. Flavonol shows protective and analgesic effects in mice through various neuronal pathways. Flavonol can be used in research related to tumors and atherosclerosis diseases.
    Flavonol (Standard)
  • HY-100919R
    Ambenonium chloride (Standard)
    Inhibitor
    Ambenonium (chloride) (Standard) is the analytical standard of Ambenonium (chloride). This product is intended for research and analytical applications. Ambenonium (WIN 8077) chloride is an orally active and reversible inhibitor of Acetyicholinesterase (AChE) with high affinity. Ambenonium chloride inhibits human AChE with an IC50 value of 0.7 nM (hAChE).
    Ambenonium chloride (Standard)
  • HY-N15323
    Samioside
    Inhibitor
    Samioside is an effective acetylcholinesterase inhibitor that can be isolated from Phlomis nissolii and P. capitata. Samioside possesses free-radical scavenging and antimicrobial activities. Samioside can be used in research on its anti-Alzheimer’s potency.
    Samioside
  • HY-W020785R
    Fosthiazate (Standard)
    Inhibitor
    Fosthiazate (Standard) is the analytical standard of Fosthiazate. This product is intended for research and analytical applications. Fosthiazate is a broad-spectrum nematicide against various plant parasitic nematodes, including Meloidogyne spp., Globodera spp., and Pratylenchus spp., through inhibiting the synthesis of acetylcholinesterase.
    Fosthiazate (Standard)
  • HY-118275
    FK960
    Activator
    FK960 is a potential anti-dementia agent that reverses the reduction in cerebral blood flow (rCBF) caused by sensory stimulation by enhancing cholinergic neurotransmission. In macaque experiments, physostigmine (AChE inhibitor; HY-N6608) was able to completely eliminate the rCBF in the sensory cortex increased by vibrotactile stimulation. FK960 (1-1000 μg/kg) can restore the eliminated rCBF response, and the action time can last for 1 hour. However, FK960 cannot restore the rCBF response eliminated by HA-966 (NMDA modulator; HY-100822), indicating that its function is not dependent on non-glutamatergic neurotransmission.
    FK960
  • HY-124920
    Methiocarb
    Inhibitor
    Methiocarb (Mercaptodimethur) is an orally active carbamate insecticide. Methiocarb exerts dose-dependent toxic effects on onions. In addition to inhibiting acetylcholinesterase to induce cholinergic excitation, Methiocarb can induce lipid peroxidation in liver, kidney, brain and testicular tissues and alter reduced glutathione levels by generating ROS. Methiocarb can be used for agricultural pest control and research on oxidative stress-related cellular damage in mammals.
    Methiocarb
  • HY-119419S
    Pirimicarb-d6
    Pirimicarb-d6 is the deuterium labeled Pirimicarb (HY-119419). Pirimicarb is a fast-acting selective carbamate insecticide on a wide range of crops including cereals, sugar beet, potatoes, fruits and vegetables. Pirimicarb is an AChE inhibitor and an acaricide.
    Pirimicarb-d<sub>6</sub>
  • HY-N4142R
    Cyanidin-3-O-galactoside chloride (Standard)
    Inhibitor
    Cyanidin-3-O-galactoside (chloride) (Standard) is the analytical standard of Cyanidin-3-O-galactoside (chloride). This product is intended for research and analytical applications. Cyanidin-3-O-galactoside chloride (Ideain chloride) is a component from extract peel of hawthorn fruit (EPHF) with the value of 179.4 mg/g. EPHF exhibits strong AChE inhibitory activity.
    Cyanidin-3-O-galactoside chloride (Standard)
  • HY-N4261R
    Dehydronuciferine (Standard)
    Inhibitor
    Dehydronuciferine is isolated from the leaves of Nelumbo nucifera Gaertn, a acetylcholinesterase (AChE) inhibitor with an IC50 of 25 μg/mL.
    Dehydronuciferine (Standard)
  • HY-10400R
    Ladostigil hemitartrate (Standard)
    Inhibitor
    Ladostigil hemitartrate (Standard) is the analytical standard of Ladostigil hemitartrate (HY-10400). This product is intended for research and analytical applications. Ladostigil (TV-3326) hemitartrate is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hemitartrate exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil hemitartrate can be used for the research of depression and Alzheimer's disease. Ladostigil hemitartrate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Ladostigil hemitartrate (Standard)
  • HY-165600
    Trimedoxime dichloride
    Activator
    Trimedoxime dichloride (TMB-4 dichloride) is a blood-brain barrier-permeable cholinesterase reactivator. Trimedoxime dichloride reactivates cholinesterase inhibited by paraoxon, sarin, tabun and other agents, restricts the breakdown of acetylcholine and alleviates excessive cholinergic stimulation. Trimedoxime dichloride reduces mortality and prolongs survival time. Trimedoxime dichloride exhibits reactivation efficacy against AChE in rat tissues. Trimedoxime dichloride can be used in research related to organophosphate (paraoxon) poisoning and tabun poisoning.
    Trimedoxime dichloride
  • HY-18039
    WAY-361789
    Agonist
    WAY-361789 (SEN15924) is an orally active agonist for α7 nicotinic acetylcholine receptor (α7 nAChR) with an EC50 of 0.18 μM. WAY-361789 improves the cognitive function, exhibits potential in ameliorating Alzheimer’s Disease and schizophrenia.
    WAY-361789
  • HY-N0631R
    Cornuside (Standard)
    Inhibitor
    Cornuside (Standard) is the analytical standard of Cornuside (HY-N0631). This product is intended for research and analytical applications. Cornuside is an iridoid glycoside with anti-allergic, anti-inflammatory, and neuroprotective activities. Cornuside exerts anti-allergic activity by downregulating the p38 MAPK, JNK, and NF-κB signaling pathways, and inhibits IgE-mediated histamine release from mast cells. Cornuside improves cognitive impairment in mice by inhibiting BACE1 activity (IC50 = 55.84 μg/mL) and enhancing ChAT activity. Cornuside inhibits LPS (HY-D1056)-induced inflammatory mediators, including iNOS, COX-2, PGE2, TNF-α, IL-6, and IL-1β, by suppressing NF-κB activation.
    Cornuside (Standard)
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