AChE Inhibitor

Pirimiphos-methyl is an organophosphorus insecticide and acaricide that can inhibit AChE in target organisms. Pirimiphos-methyl is often used for prevention and control of beetles, snout beetles, moths and Ephestia cautella during storage of agricultural grains.

(±)-Huperzine A is the racemate of (-)-Huperzine A (HY-17387). (-)-Huperzine A is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC₅₀ of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease.

Galanthaminone (Narwedin) is a competitive and reversible cholinesterase (AChE) inhibitor; is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments.

Neoeriocitrin is a Naringin (HY-N0153) analogue found in Drynaria Rhizome. Neoeriocitrin induces cells proliferation, differentiation, up-regulates type I collagen, osteocalcin, and key osteogenic markers, and increases ALP activity. Neoeriocitrin increases expression of Runx2, COL I, OCN and Beclin1. Neoeriocitrin inhibits phosphorylation of P38 mitogen-activated protein kinase, reduces acetylcholinesterase (AChE) activity, and increases choline acetyltransferase (ChAT) activity. Neoeriocitrin reduces apoptosis and induces autophagy. Neoeriocitrin can be used for the researches of osteoporosis and Alzheimer's disease.

Jatrorrhizine hydroxide is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine hydroxide is a potent and orally active inhibitor of AChE (IC₅₀=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine hydroxide reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.

β-NETA is a potent and noncompetitive choline acetyltransferase (ChA; IC₅₀=76 μM) and cholinesterase (ChE; IC₅₀=40 μM) inhibitor. β-NETA weakly inhibits acetylcholinesterase (AChE; IC₅₀=1 mM).

Phenthoate is an organophosphorus pesticide having low toxicity in animals. Phenthoate is also a AChE inhibitor.

Edrophonium chloride is a short-acting acetylcholinesterase (AChE) inhibitor. Edrophonium chloride has K_i values of 0.2, 0.2, and 0.4 μM and IC₅₀ values of 0.2, 0.05, and 0.5 μM for AChE in human erythrocytes, purified calf forebrain, and purified octopus brain, respectively. Edrophonium chloride can be used to detect early digitalis toxicity and in the study of myasthenia gravis.

N-Desmethyl Galanthamine (N-Norgalanthamine) is a metabolite of Galanthamine (HY-76299). N-Desmethyl Galanthamine is an EeAChE inhibitor with an IC₅₀ of 2.76 μM. N-Desmethyl Galanthamine can be used in the research of Alzheimer's disease.

Pteryxin ((+)-Pteryxin) is an orally active multi-target inhibitor that targets NF-κB, MAPK, NLRP3 inflammasome, and Nrf2/ARE pathways. Pteryxin is also a BChE inhibitor (IC₅₀=12.96 μg/mL) with a low inhibitory efficiency on AChE. Pteryxin inhibits the Ca²⁺-calcineurin-NFATc1 pathway by blocking NF-κB/MAPK signaling, inhibiting NLRP3 inflammasome activation, and reducing ROS generation, and activates Nrf2-mediated antioxidant enzyme expression. Pteryxin has anti-inflammatory, antioxidant, and osteoclastogenesis inhibitory activities. Pteryxin can be used in the study of inflammatory diseases, osteoporosis, diabetes, and Alzheimer's disease.

Methyl orsellinate acts as an antiviral agent and insecticide. Methyl orsellinate exhibits enzyme inhibitory activity, with an IC₅₀ of 59.6 µM against porcine leukocyte 5-lipoxygenase (5-LOX); it inhibits soybean 15-lipoxygenase (15-LOX), and shows weak inhibitory activity against acetylcholinesterase (AChE) and glutathione S-transferase (GST). Methyl orsellinate displays contact toxicity against adult Drosophila suzukii. Methyl orsellinate shows anti-HSV-1 activity. Methyl orsellinate can be used in studies related to *Drosophila suzukii* infestation and HSV-1 infection.

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).

PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC₅₀ of 18.1 nM and a K_d of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [³H]-NMS binding to the M4 receptor with a K_i of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC₅₀ s of 22 nM and 120 nM for electric eel and human AChE, respectively.

Manghaslin is a flavonoid glycoside with anti-inflammatory activities. Manghaslin shows inhibitory activity against AChE with an IC₅₀ of 94.92 μM.

Trimethylammonium chloride (Standard) (Hegzadesil (Standard)) is the analytical standard of Trimethylammonium chloride (HY-Y0504). This product is intended for research and analytical applications. Trimethylammonium chloride (Hegzadesil) is a non-competitive Acetylcholinesterase inhibitor. Trimethylammonium chloride reversibly blocks the deacetylation of acetylcholinesterase.

Fenobucarb is a carbamate insecticide. Fenobucarb induces zebrafish developmental neurotoxicity through pathways involved in inflammation, oxidative stress, degeneration and apoptosis. Fenobucarb is a possible risk factor to cardiovascular and cerebrovascular systems in animals.

Polygalacic acid, is a triterpene, isolated from the root of Polygala tenuifolia Willd. Polygalacic acid inhibits MMP expression. Polygalacic acid may have a therapeutic effect in Osteoarthritis (OA) treatment . Polygalacic acid exerts a significant neuroprotective effect on cognitive impairment, PA improves cholinergic system reactivity by inhibiting acetylcholinesterase (AChE) activity, increasing choline acetyltransferase (ChAT) activity, and elevating levels of acetylcholine (Ach) in the hippocampus and frontal cortex.

Dehydroevodiamine is a blood-brain barrier-permeable, orally effective AChE and BACE1 inhibitor (IC₅₀ = 40.96 μM). Dehydroevodiamine is isolated and extracted from Evodia rutaecarpa. Dehydroevodiamine attenuates neurotoxicity through multiple targets by inhibiting BACE1 to block Aβ production, inhibiting AChE activity, scavenging ROS, and suppressing calcium influx. Dehydroevodiamine can be used for research on Alzheimer's disease, cerebral ischemia, vascular dementia, and other cognitive disorder-related diseases.

2,2'-Dihydroxy-1,1'-binaphthyl is an acetylcholinesterase (AChE) inhibitor with an IC₅₀ value of 21.9 μM against human AChE. 2,2'-Dihydroxy-1,1'-binaphthyl exhibits cytotoxicity against Artemia nauplii.

Tacrine hydrochloride (hydrate) is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC₅₀s of 31 nM and 25.6 nM, respectively.