AChE Inhibitor

Ganstigmine (CHF 2819 free base) is a potent, orally active, blood-brain barrier-permeable acetylcholinesterase (AChE) inhibitor, with an IC₅₀ value of 65 nM against human AChE, 310 nM against human butyrylcholinesterase (BChE), and 5.12 μM against Torpedo californica AChE. Ganstigmine increases extracellular acetylcholine levels in the brain of rodents without altering the concentrations of other neurotransmitters, stimulates cholinergic transmission, and induces the release of soluble non-amyloidogenic amyloid precursor protein. Ganstigmine exhibits neuroprotective activity independent of cholinesterase inhibition, prevents neuronal death, alleviates β-amyloid-induced neurodegeneration, rescues cholinergic neuron loss, and reverses Scopolamine (HY-N0296)-induced amnesia and memory deficits. Ganstigmine shows cholinesterase inhibition-independent neuroprotective effects against growth factor deprivation and Aβ_25-35 toxicity. Ganstigmine can be used in research on Alzheimer's disease, cholinergic dysfunction, and neuroprotection.

AD-35 free base is an orally active, blood-brain barrier-permeable acetylcholinesterase inhibitor with an IC₅₀ of 793 nM. AD-35 free base inhibits metal-induced amyloid-β aggregation and disassembles preformed amyloid-β aggregates. In rat models of cognitive impairment, AD-35 free base attenuates Aβ_25-35-induced astrocyte activation, TNF-α and IL-1β release, inhibits ERK phosphorylation, and alleviates learning and memory deficits. AD-35 free base can be used for research on Alzheimer's disease.

Methyl ganoderate A acetonide, a lanostane triterpene, is a natural product that could be isolated from the fruiting bodies of Ganoderma lucidum. Methyl ganoderate A acetonide is a potent AChE inhibitor with an IC₅₀ value of 18.35 μM. Methyl ganoderate A acetonide can be used in research of Alzheimer’s disease (AD).

AChE-IN-115 is an acetylcholinesterase (AChE) inhibitor. AChE-IN-115 forms stable complexes with AChE from Spodoptera litura (tobacco cutworm) and Tribolium castaneum (red flour beetle). AChE-IN-115 exhibits insecticidal activity.

TAE-1 is a potent inhibitor of AChE and BuChE. TAE-1 also inhibits Aβ fibril formation and aggregation. TAE-1 can be used for the researches of Alzheimer's disease.