Cholinesterase (ChE) Inhibitor

Trimethylammonium chloride (Hegzadesil) is a non-competitive Acetylcholinesterase inhibitor. Trimethylammonium chloride reversibly blocks the deacetylation of acetylcholinesterase.

Dimethyl sulfoxide (Standard) is the analytical standard of Dimethyl sulfoxide. This product is intended for research and analytical applications. Dimethyl sulfoxide (DMSO) is an aprotic solvent that dissolves both polar and nonpolar compounds. Dimethyl sulfoxide has anti-freezing and bacteriostatic properties.

Lactupicrin (Lactucopicrin) exhibits analgesic, sedative, antimalarial activities and atheroprotective effect. Lactupicrin inhibits acetylcholinesterase (AChE) with an IC₅₀ of 150.3 μM. Lactupicrin is an orally active characteristic bitter sesquiterpene lactone.

Lecithins, egg (Lecithins, egg yolk; Belovo PL 85) is an orally active natural phospholipid mixture extracted from egg yolks. Lecithins, egg inhibits the activities of acetylcholinesterase (AChE) and angiotensin-converting enzyme (ACE). Lecithins, egg exhibits antibacterial, antioxidant and anti-inflammatory activities, and helps delay cellular senescence. Lecithins, egg enhances nerve conduction, improves memory and cognitive function, and exerts positive effects on delaying neurodegenerative diseases. Lecithins, egg promotes lipid absorption and alleviates diarrhea. Lecithins, egg acts as a high-efficiency drug carrier for the preparation of targeted drug delivery systems such as liposomes.

Flavonol is a cholinesterase (ChE) inhibitor, with an IC₅₀ value of 120 μM and a K_i 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.

Dimethoate is an organophosphate insecticide and acaricide. Dimethoate is an orally active acetylcholinesterase inhibitor. Dimethoate induces reactive oxygen species (ROS). Dimethoate induces DNA damage and cell apoptosis in vivo. Dimethoate affect immune system in mice.

Sinapine thiocyanate is an alkaloid isolated from seeds of the cruciferous species. Sinapine thiocyanate exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine thiocyanate is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.

Chavicol (p-Hydroxyallylbenzene) is a phenylpropane compound. Chavicol can be isolated from the bark of Sassafras tzumu. Chavicol exhibits Acetylcholinesterase inhibitory activity (IC₅₀ = 7.42 μM). Chavicol produces a 3% inhibitory effect on antigen-IgE-mediated degranulation in mast cells.

Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC₅₀ of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α₃β₄, α₄β₂, α₆β₄ nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD).

Methyl rosmarinate is an orally active hydroxycinnamic acid. Methyl rosmarinate exhibits an IC₅₀ of 24.70 μM and a K_i of 15.29 μM against PTP1B, an IC₅₀ of 41.46 μg/mL against BChE, a K_i of 0.61 mM against mushroom tyrosinase, and an IC₅₀ of 2.50 μM against SARS-CoV-2 3CLpro. Methyl rosmarinate downregulates the phosphorylation levels of ERK, JNK, p38, Smad2 and Smad3. Methyl rosmarinate activates erythrocyte BPGM and promotes the production of 2,3-BPG. Methyl rosmarinate induces apoptosis of fibroblasts. Methyl rosmarinate prolongs the survival time of hypoxic mice. Methyl rosmarinate improves insulin sensitivity. Methyl rosmarinate binds to SARS-CoV-2 3CLpro and inhibits viral replication. Methyl rosmarinate induces glioblastoma cell death. Methyl rosmarinate activates the TGR5/AMPK axis and reduces the levels of ROS and MDA. Methyl rosmarinate shows inhibitory activity against MMP-1. Methyl rosmarinate can be used in research related to pulmonary fibrosis, hypoxia-induced injury, type 2 diabetes, Alzheimer's disease, hyperpigmentation disorders, COVID-19, glioblastoma and myocardial ischemia-reperfusion injury.

Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) is a potent amyloid β (Aβ) inhibitor. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases the expression of acetylcholine (ACh) levels, choline acetyltransferase (ChAT) activity, and ChAT gene induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) decreases in acetyl cholinesterase (AChE) activity and AChE gene expression induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases muscarinic M1 receptor gene expression and muscarinic M1 receptor binding activity. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) can be used for Alzheimer's disease research.

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

Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α₁-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC₅₀ of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity.

N-p-trans-Coumaroyltyramine is a natural phenolic amide compound and an inhibitor of AChE (IC₅₀: 122 μM) and α-glucosidase (IC₅₀: 2.7 μM). N-p-trans-Coumaroyltyramine also has anti-trypanosomal activity, with an IC₅₀ of 13.3 µM against T. brucei rhodesiense. N-p-trans-Coumaroyltyramine can be used in the research of diseases such as Alzheimer's disease.

Neostigmine methyl sulfate is an AchE inhibitor. Neostigmine methyl sulfate increases endogenous acetylcholine levels, mediates antinociceptive effects, and alleviates heat-induced pain. Neostigmine methyl sulfate can be used in studies related to postoperative pain and sepsis.

Physostigmine hemisulfate (Eserine hemisulfate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine hemisulfate can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine hemisulfate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine hemisulfate is also an antidote for anticholinergic poisoning.

Skimmianine is an orally active furoquiniline alkaloid present mainly in the Rutaceae family. Skimmianine has analgesic, antispastic, sedative, and anti-inflammatory properties. Skimmianine inhibits acetylcholinesterase (AChE) (IC₅₀ = 8.6 μg/mL). Skimmianine exhibits cytotoxicity against a variety of cancer cell lines and genotoxicity. Skimmianine has antioxidant and anti-inflammatory effects on ischemia-reperfusion (IR) injury. Skimmianine exerts anti-inflammatory effects through activation of the phosphatidylinositol-3-kinase (PI3K)-protein kinase B (AKT) pathway. Skimmianine is neuroprotective by targeting the NF-κB activation pathway to prevent neuroinflammation. Skimmianine inhibits the release of histamine, intracellular Ca²⁺ signaling and protein kinase C signaling.

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.

Itopride (HSR803) hydrochloride is a potent dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride hydrochloride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD).

Fenitrothion is a broad-spectrum and orally active insecticide/acaricide. Fenitrothion inhibits cholinesterase, AMPKα and IRS1/PI3K/AKT. Fenitrothion causes Apoptosis, reduces SOD activity. Fenitrothion shows insecticidal effect against Rhyzopertha dominica and Tribolium castaneum adults. Fenitrothion is widely used in cotton crops, vegetable crops, fruit crops and field crops, especially rice. Fenitrothion can be used for brain and spleen toxicology studies.