AChE Inhibitor

Kuwanon U is a potent cholinesterase inhibitor with IC₅₀s of 19.69, 10.11 µM and K_is of 6.48, 9.59 µM for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), respectively. Kuwanon U has the potential for the research of Alzheimer’s disease (AD).

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.

Galanthamine N-Oxide is an alkaloid obtained from the bulbs of Zephyranthes concolor. Galanthamine N-Oxide inhibits electric eel acetylcholinesterase (AChE) with an EC₅₀ of 26.2 μM. Galanthamine N-Oxide is a prominent inhibitor of substrate accommodation in the active site of the Torpedo californica AChE (TcAChE), hAChE and hBChE enzymes.

Pitofenone hydrochloride, a spasmolytic compound, inhibits the acetylcholinesterase (AChE) activity from bovine erythrocytes and from electric eel with K_is of 36 and 45 μM, respectively.

Minaprine is a brain-penetrant monoamine oxidase inhibitor. Minaprine also weakly inhibits acetylcholinesterase (AChE) activity. Minaprine reduces intraneuronal dopamine metabolism, lowers striatal homovanillic acid and dihydroxyphenylacetic acid levels, and raises striatal 3-methoxytyramine and 5-hydroxytryptamine levels. Minaprine exhibits convulsant, antidepressant properties.

Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC₅₀s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO^- scavenging effect (IC₅₀, 16.83 μM), and can be used for the research of Alzheimer disease. Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Epiberberinecan be used for the research of diabetic disease.

Norneostigmine is a potent inhibitor of AChE that can penetrate the blood-brain barrier. Norneostigmine can achieve a 50% inhibition rate of mouse brain AChE after 10 min treatment, which is close to the inhibitory effect of tetrahydroaminoacridine (57% at 10 min). Norneostigmine can be used to study memory disorders related to Alzheimer's disease and other memory disorders.

Zanapezil (TAK-147) is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC₅₀=51.2 nM). Zanapezil shows a moderate inhibition of muscarinic M1 and M2 receptor binding with K_i values of 234 and 340 nM, respectively. Zanapezil can be used for the research of early stages of Alzheimer's disease (AD).

Kokusaginine is a furoquinoline alkaloids, which exhibits inhibitory efficacy for acetylcholinesterase (AChE) with an IC₅₀ of 28.2 μM. Kokusaginine exhibits anti-proliferative and apoptotic inducing effects in MCF-7/ADR cells.

Zanapezil (TAK-147) free base is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC₅₀=51.2 nM). Zanapezil free base shows a moderate inhibition of muscarinic M1 and M2 receptor binding with K_i values of 234 and 340 nM, respectively. Zanapezil free base can be used for the research of early stages of Alzheimer's disease (AD).

SD-6 is an orally active inhibitor of hAChE and hBChE with IC₅₀ values of 0.907 µM and 1.579 µM, respectively. SD-6 has excellent blood-brain barrier (BBB) permeability and no neurotoxicity, which can be used for research on Alzheimer's disease.

BChE-IN-11 (compound 10) is a potent, selective and non-competitive BChE (butyrylcholinesterase) inhibitor, with an IC₅₀ of 2.1 μM. BChE-IN-11 can be used for Alzheimer's disease (AD) research.

Isoprocarb-d₃ is deuterium labeled Isoprocarb. Isoprocarb is carbamate insecticide that widely used to control rice paddy lice and leafhopper. Isoprocarb is also an AChE inhibitor.

PE154 is a fluorescent probe that binds to Aβ plaques, as well as a potent fluorescent inhibitor of AChE and BChE, with an IC₅₀ of 280 pM against hAChE and 16 nM against hBChE. PE154 is applicable for histochemical detection of Aβ plaques in mouse and human brain tissues. PE154 can be used in research related to Alzheimer's disease.

Velnacrine (HP 029 free base) is an inhibitor for acetylcholinesterase (AChE), with an IC₅₀ of 3.27 μM. Velnacrine reverses the Scopolamine (HY-N0296)-induced amnesia in rat models, and exhibits acute toxicity with LD₅₀ of 65 mg/kg.

AChE/BChE-IN-10 (Compound 7b) is a potent dual AChE and BChE inhibitor with IC₅₀ values of 0.176, and 0.47 μM, respectively. AChE/BChE-IN-10 shows good blood brain barrier permeability. AChE/BChE-IN-10 can inhibit Aβ-aggregation and be used in Alzheimer’s disease (AD) research.

Donepezil N-oxide, a metabolite of Donepezil (HY-14566), is human erythrocyte acetylcholinesterase (AChE) inhibitor.

Lucidadiol is a natural compound isolated from Ganoderma lucidum. Lucidadiol exhibits acetylcholinesterase-inhibitory activity, with IC₅₀ values of 31 μM. Lucidadiol shows antiviral activity against influenza virus type A and HSV type 1.

Methyl tridecanoate is a fatty acid methyl ester. Methyl tridecanoate exhibits an IC₅₀ of 3.26 μM and a K_i of 2.30 μM against AsOBP21f in Anopheles sinensis. Methyl tridecanoate induces electroantennographic responses in female Anopheles sinensis. Methyl tridecanoate shows a dose-dependent attractive effect on Anopheles sinensis. Methyl tridecanoate weakly inhibits β-amyloid aggregation and AChE activity. Methyl tridecanoate can be used in the research of malaria and Alzheimer's disease.

Coroxon (Coumaphos oxon) is an oxidative metabolite of the organophosphate insecticide Coumaphos (HY-W653717) and an active AChE inhibitor with insecticidal and acaricidal properties. Coroxon can be hydrolyzed by phosphotriesterases of microorganisms such as Nocardia asteroides to produce the fluorescent product Chlorferon.