Cholinesterase (ChE) Inhibitor

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

Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine (HY-N6608) and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease.

Pyridostigmine-d₆ (bromide) is the deuterium labeled Pyridostigmine, which is a parasympathomimetic and a reversible cholinesterase inhibitor.

Fosthiazate is an inhibitor of acetylcholinesterase (Acetylcholinesterase, AChE). Fosthiazate exhibits significant nematicidal activity and systemic insecticidal activity. Fosthiazate is applicable to studies on plant-parasitic nematodes, root-knot diseases, agricultural pests, as well as the ecotoxicology and environmental behavior of organophosphorus compounds.

Penconazole is a typical triazole fungicide, and mainly applied on apples, grapes, and vegetables to control powdery mildew. Penconazole inhibits sterol biosynthesis in fungi. Penconazole decrease AChE activity in the cerebrum and cerebellum of rats.

MAPK-IN-1 (Compound 2) is a MAPK signaling pathway inhibitor. MAPK-IN-1 exhibits AChE inhibitory activity with an IC₅₀ of 23.84 μM. MAPK-IN-1 shows anti-neuroinflammatory and neuroprotective activity and can be used for Alzheimer's disease research.

L-Citronellol ((S)-3,7-Dimethyloct-6-en-1-ol) is a natural product with anti-allergic and neuroprotective effects. L-Citronellol inhibits mast cell activation and the release of inflammatory factors by inhibiting the ERK pathway. L-Citronellol inhibits BACE1/PSEN1 and AChE, reduces TNF-α expression and lipid peroxidation, demonstrating the potential of multi-target anti-Alzheimer's disease (AD).

Carbosulfan is an orally active AChE inhibitor that hydrolyzes to Carbofuran in organisms to exert insecticidal effects. Carbosulfan exhibits broad-spectrum insecticidal activity, and it also induces severe oxidative stress by enhancing lipid peroxidation and impairing the antioxidant defense system. Carbosulfan causes reproductive toxicity in male rats and developmental disorders in their offspring. Carbosulfan shows persistence in paddy field environments and potential hazards to non-target organisms, and it is commonly used in studies related to reproductive toxicity and environmental risk assessment.

Dihydroactinidiolide, existing in plant leaves and fruits, is a potent plant growth inhibitor, a regulator of gene expression and is responsible for photo acclimation in Arabidopsis. Dihydroactinidiolide has antioxidant activity, antibacterial activity, anticancer activity and neuroprotective effect. Dihydroactinidiolide is also an inhibitor of AChE (IC50=34.03 nM) and has scavenging activities for DPPH and (.NO). Dihydroactinidiolide is present in plant leaves and fruits and is a potent plant growth inhibitor, regulator of gene expression, and responsible for light adaptation in Arabidopsis.

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).

Dimethyl sulfoxide (DMSO) (GMP Like) is the GMP Like class Dimethyl sulfoxide (HY-Y0320C). Dimethyl sulfoxide is an aprotic solvent that can dissolve water-insoluble therapeutic and toxic agents. Dimethyl sulfoxide has a strong affinity for water and has the ability to rapidly penetrate or enhance the penetration of other substances through biological membranes. Dimethyl sulfoxide also has potential free radical scavenging and anticholinesterase effects and may affect coagulation activity. Dimethyl sulfoxide also induces histamine release from mast cells but is thought to have low systemic toxicity.

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

Chlorpyrifos (Standard) is the analytical standard of Chlorpyrifos. This product is intended for research and analytical applications. Chlorpyrifos is a neurotoxic insecticide that belongs to the class of thionite esters. Chlorpyrifos is also a AChE inhibitor that affects neurological function in insects, humans and other animals. Chlorpyrifos interferes with cell replication and differentiation, ultimately altering synaptic transmission in neurons.

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.

Demecarium Bromide (BC-48) is a potent cholinesterase inhibitor, with an apparent affinity (K_iapp) of 0.15 μM. Demecarium Bromide (BC-48) is used as a glaucoma agent.