Cholinesterase (ChE) Inhibitor

Dimethyl sulfoxide (DMSO), meets analytical specification of Ch.P. is an aprotic solvent that dissolves polar and non-polar compounds, including water-insoluble therapeutic and toxic agents. Dimethyl sulfoxide (DMSO) has a strong affinity for water and can rapidly penetrate or enhance the penetration of other substances into 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. Dimethyl sulfoxide also exhibits antifreeze and antibacterial properties.
MCE provides Dimethyl sulfoxide that complies with the inspection standards (Ch.P) of Part 4 of the Chinese Pharmacopoeia (2020 Edition). Amicrobic, low endotoxin, can be used in various biochemical experiments such as drug dissolution.

Dimethyl sulfoxide (DMSO) is an aprotic solvent that can dissolve water-insoluble therapeutic and toxic agents. Dimethyl sulfoxide (DMSO) 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.
Low endotoxin, can be used in various biochemical experiments such as drug dissolution.

Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC₅₀ of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity.

Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC₅₀s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively.

TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand. TMPyP4 tosylate inhibits the interaction between G-quadruplexes and IGF-1. TMPyP4 tosylate is a telomerase inhibitor and inhibits cancer cells proliferation. TMPyP4 tosylate is also a stabilizer of nucleic acid secondary structure and an acetylcholinesterase inhibitor. Besides, TMPyP4 tosylate has antiviral activity against SARS-CoV-2.

COX-2-IN-67 is an orally active, blood-brain barrier permeable multi-target inhibitor that potently targets COX-2 (IC₅₀=0.07 μM), hCA IX (K_i=62.7 nM) and hBuChE (IC₅₀=0.47 μM). COX-2-IN-67 alleviates oxidative stress and liver stress, improves glucose homeostasis and insulin sensitivity, and optimizes lipid profiles. Meanwhile, COX-2-IN-67 effectively reduces the levels of neuroinflammatory markers and improves hippocampus-dependent cognitive function in a high-fat diet-induced rat model. COX-2-IN-67 can be used for the research of metabolic dysfunction-associated mild cognitive impairment.

Imperatorin is an effective of NO synthesis inhibitor (IC₅₀=9.2 μmol), which also is a BChE inhibitor (IC₅₀=31.4 μmol). Imperatorin is a weak agonist of TRPV1 with EC₅₀ of 12.6±3.2 μM.

Phosphatidylcholines, egg are a type of phosphatidylcholine that can be isolated and extracted from eggs, primarily present in egg yolks. As a major phospholipid component of cell membranes, Phosphatidylcholines, egg play a key role in providing nutrition and protection to the body. Phosphatidylcholines, egg can inhibit oxidative stress and neurotoxicity, exerting neuroprotective effects. Additionally, Phosphatidylcholines, egg can suppress the lymphatic absorption of cholesterol in the intestine and are also used in research on intestinal lipid absorption.

Garcinol, a polyisoprenylated benzophenone harvested from Garcinia indica, exerts anti-cholinesterase properties towards acetyl cholinesterase (AChE) and butyrylcholinesterase (BChE) with IC₅₀s of 0.66 μM and 7.39 μM, respectively. Garcinol also inhibits histone acetyltransferases (HATs, IC₅₀= 7 μM) and p300/CPB-associated factor (PCAF, IC₅₀ = 5 μM). Garcinol has anti-inflammatory and anti-cancer activity.

Dimethyl sulfoxide, cryoprotectant vitrification agent (DMSO, cryoprotectant vitrification agent) is a biochemical reagent that can be used as a biological material or organic compound for life science related research. This product has been sterilized and has no endotoxin. It can be used for long-term cell cryopreservation and will not affect the normal growth of cells.

α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC₅₀ of 9 μM. α-NETA is a potent ALDH1A1 (IC₅₀=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC₅₀=84 µM) and acetylcholinesterase (AChE; IC₅₀=300 µM). α-NETA has anti-cancer activity.

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.

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.

Linarin (Buddleoside) is an orally active and selective inhibitor of acetylcholinesterase (AChE). Linarin has many activities, such as anti-inflammatory, antioxidant, sleep aid and sedation, bone differentiation, anti-tumor, antibacterial and antiviral. Linarin can be used to study diseases such as the nervous system, osteoporosis and cancer.

Scopoletin is an inhibitor of acetylcholinesterase (AChE).

Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with an IC₅₀ of 500 nM.

Hemicholinium 3 is a competitive inhibitor of the high affinity choline transporter (HACU) with a K_i value of 25 nM. Hemicholinium 3, a neuromuscular blocking agent which inhibits the synthesis and the release of acetylcholine (ACh). Hemicholinium 3 inhibits the Epibatidine-evoked contraction and [³H]acetylcholine release with IC50s of 897 nM and 693 nM, respectively.

Iso-OMPA (Tetraisopropyl pyrophosphoramide) is a selective inhibitor of the irreversible butyrylcholinesterase (BuChE). Iso-OMPA enhances soman toxicity in rats associated with the inhibition of plasma carboxylesterase (CarbE).

Chlorpyrifos-oxon, an active metabolite of Chlorpyrifos, is a potent phosphorylating agent that potently inhibits AChE. Chlorpyrifos-oxon can induce cross-linking between subunits of tubulin and disrupt microtubule function.

Epiberberine chloride 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 chloride has antioxidant activity, with peroxynitrite ONOO^- scavenging effect (IC₅₀, 16.83 μM), and may protect against Alzheimer disease. Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Epiberberine has the potential effect in the research of diabetic disease.