Cholinesterase Inhibitors

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D0879 Diisopropylfluorophosphate Potent inhibitor of serine proteases such as trypsin and chymotrypsin, and of acetylcholinesterase; also inhibits cathepsin G, cholinesterase, coagulation factor Xa, leucocyte elastase, pancreatic elastase, tissue kallikrein, plasmin, subtilisin, and thrombin. Inhibition of acetylcholinesterase makes this compound especially toxic. Inhibits apoptosis induced by ricin and bacterial toxins.
human ... PTGS1(5742), PTGS2(5743)
E8375 Eserine Acetylcholinesterase inhibitor that crosses the blood-brain barrier and forms a carbamylated enzyme complex with acetyl cholinesterase that degrades slowly.
human ... ACHE(43), APP(351), BCHE(590)
mouse ... Ache(11423), Bche(12038), Chrm1(12669)
rat ... Ache(83817), Bche(65036), Chrm2(81645)
E8625 Eserine hemisulfate salt Acetylcholinesterase inhibitor that crosses the blood-brain barrier and forms a carbamylated enzyme complex with acetyl cholinesterase that degrades slowly.
 
45720 Eserine salicylate salt ≥97.0% (N) Acetylcholinesterase inhibitor that crosses the blood-brain barrier and forms a carbamylated enzyme complex with acetyl cholinesterase that degrades slowly.
 
E5406 Ethopropazine hydrochloride ≥98% (HPLC), powder Ethoproprazine hydrochloride is an inhibitor of butyrylcholinesterase; antiparkinsonian. It reduces extrapyramidal motor effects, characteristic of Parkinson′s disease; also alleviates thermal hyperalgesia in rats.
 
G1660 Galanthamine hydrobromide from Lycoris sp. ≥94% (TLC) Cholinesterase inhibitor; reverses scopolamine-induced amnesia; antimyasthenic.
 
H5902 (−)-Huperzine A Acetylcholinesterase inhibitor; active enantiomer.
human ... ACHE(43), BCHE(590)
rat ... Ache(83817)
T90301 3-(2-Hydroxyethyl)indole 97%    
SML0033 Itopride hydrochloride ≥98% (HPLC) Itopride is an acetylcholinesterase (AChE) inhibitor and D2 dopamine receptor antagonist. Itopride is used as a gastroprokinetic agent.
 
M2824 Meptazinol hydrochloride Meptazinol entered the human pharmaceutical market as a racemic mixture in the 1980s for use as an analgesic. Its pharmacology is not completely understood; however, its analgesic properties are mostly due to its partial agonism at the mu1 opioid receptor. Due to its partial agonism, Meptazinol antagonizes morphine dependence in vivo. Its advantage over other opiates is its reduced capacity to cause addition and respiratory depression, also due to its intrinsic activity as a partial agonist. Meptazinol has been found to have additional activity as an acetylcholinesterase (AChE) inhibitor, particularly in its (-) enantiomeric form, which may partially explain its analgesic properties. AChE inhibitors are used to treat Alzheimer′s disease, providing additional interest in this compound.
 
M2939 Methyl arachidonyl fluorophosphonate ≥98%, methyl acetate solution (10 mg/mL) MAFP is a selective, irreversible inhibitor of both calcium-dependent and calcium-independent cytosolic phospholipase A2, but not secretory phospholipase A2. MAFP is also a potent acetylcholinesterase inhibitor.
 
N2001 Neostigmine bromide ≥98% (HPLC and titration), powder Reversible inhibitor of acetylcholinesterase that is similar to eserine, but does not cross the blood-brain barrier.
human ... ACHE(43)
N2126 Neostigmine methyl sulfate Reversible inhibitor of acetylcholinesterase that is similar to eserine, but does not cross the blood-brain barrier.
 
565520 2-Nitro-N-methylbenzylamine    
SML0624   PE 154 ≥97% (HPLC) Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are known to associate with β-amyloid plaques, and histological co-localization of AChE and Ab peptides is well established in Alzheimer’s disease. PE-154 is a fluorescent inhibitor of both AChE and BChE with IC50 values of 280 pM and 16 nM. PE-154 stains Aβ plaques in both rodent and human tissue samples, and does not cross react with phospho-tau.
 
P0111 Phenserine ≥98% (HPLC), solid (-)-Phenserine, a phenylcarbamate derivative, is a selective, non-competitive inhibitor of acetylcholinesterase (AChE). (-)-Phenserine produces rapid, potent, and long-lasting AChE inhibition, in vivo. It is significantly less toxic than (-)-physostigmine. (-)-Phenserine improves cognitive performance in both young learning-impaired and elderly rats. Reduced secretion of β-amyloid (Abeta) has been observed in cell lines exposed to (-)-phenserine, occurring through translational regulation of β-amyloid precursor protein (beta-APP) mRNA via a non-cholinergic mechanism. These in vitro findings appear to translate in vivo into animal models and humans.