AChE

Cat. No.

A78367

CAS No.

156910-61-1

Phenserine tartrate

Synonyms: (-)-Eseroline phenylcarbamate tartrate; (-)-Phenserine (+)-tartrate

Phenserine tartrate is a selective, noncompetitive inhibitor of acetylcholinesterase (AChE) derived from Physostigmine. This compound has been shown to reduce the formation of β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ), key factors involved in Alzheimer's disease pathology. Phenserine tartrate has demonstrated potential in improving cognitive performance and may help slow the progression of Alzheimer's disease, making it a valuable tool for research in neurodegenerative disorders.

Cat. No.

A78369

CAS No.

2761149-22-6

ChE/Aβ1-42-IN-1

ChE/Aβ1-42-IN-1 is a potent inhibitor of acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), and amyloid-beta peptide (Aβ1-42) aggregation, exhibiting IC50 values of 0.062 µM, 0.767 µM, and 1.227 µM, respectively. This compound demonstrates significant blood-brain barrier (BBB) penetration, making it a promising candidate for research into Alzheimer's disease. ChE/Aβ1-42-IN-1's multi-targeted mechanism positions it as a valuable tool for studying therapeutic strategies in neurodegenerative disorders.

Cat. No.

A78375

CAS No.

3058182-98-9

hAChE-IN-10

hAChE-IN-10 is a potent inhibitor of human acetylcholinesterase (AChE), demonstrating an IC50 of 6.34 nM. This compound exhibits significant antioxidant properties and effectively scavenges free radicals. Additionally, hAChE-IN-10 has been shown to inhibit Cu2+-induced aggregation of Aβ1-42, reduce amyloid plaque formation, and provide neuroprotective effects. It has also been linked to the improvement of cognitive deficits in mouse models induced by scopolamine, making it a valuable tool for studying neurodegenerative diseases and cognitive impairment.

Cat. No.

A78384

CAS No.

3105860-84-9

MAO-B-IN-50

MAO-B-IN-50 is a selective inhibitor of monoamine oxidase B (MAO-B), demonstrating an IC50 value of 0.06 μM. This compound is effective in inhibiting the aggregation of amyloid-beta (Aβ40/42) and Tau proteins, with overall IC50 values near 1 μM. Additionally, MAO-B-IN-50 shows potent selective inhibition of acetylcholinesterase (AChE) with an IC50 of 1.78 μM. It is suitable for use in research related to Alzheimer's disease.

Cat. No.

A78386

CAS No.

2764664-52-8

AChE-IN-12

AChE-IN-12 is a selective acetylcholinesterase (AChE) inhibitor that effectively penetrates the blood-brain barrier, exhibiting IC50 values of 0.41 μM for rat AChE and 1.88 μM for electric eel AChE. This compound also demonstrates antioxidant properties (ORAC = 3.3 eq), selectively chelates metals, and inhibits human monoamine oxidase B (MAO-B) with an IC50 of 8.8 μM. AChE-IN-12 significantly inhibits both self- and Cu2+-induced aggregation of Aβ1-42 and displays neuroprotective effects, making it a valuable tool for research related to Alzheimer’s disease.

Cat. No.

A78387

CAS No.

2742707-47-5

AChE/BuChE-IN-3

AChE/BuChE-IN-3 is a dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), exhibiting IC50 values of 0.65 μM and 5.77 μM, respectively. This compound effectively inhibits the aggregation of amyloid beta peptide Aβ1-42 and demonstrates neuroprotective properties with minimal toxicity in SH-SY5Y cells. AChE/BuChE-IN-3 is suitable for research applications related to Alzheimer's disease, providing insight into cholinergic system modulation and potential therapeutic strategies.

Cat. No.

A78400

CAS No.

2957916-86-6

AChE-IN-59

AChE-IN-59 is a potent acetylcholinesterase (AChE) inhibitor, displaying an IC50 value of 0.05 μM. This compound effectively inhibits the aggregation of amyloid-beta peptide Aβ1-42, offering protective effects on neuronal cells and demonstrating favorable penetration of the blood-brain barrier. AChE-IN-59 is a valuable tool for research focused on Alzheimer's disease and related neurodegenerative disorders.

Cat. No.

A78403

CAS No.

553681-56-4

AP2238

AP2238 is a dual-function acetylcholinesterase (AChE) inhibitor that demonstrates Ki values of 21.7 μM for human AChE and 48.9 μM for butyrylcholinesterase (BuChE). This compound effectively inhibits the pro-fibrotic interaction between the peripheral site of AChE and amyloid-beta (Aβ), as well as Aβ aggregation. AP2238 is primarily utilized in Alzheimer's disease research, contributing to studies focused on neurodegeneration and cholinergic dysfunction.

Cat. No.

A78410

CAS No.

1946008-31-6

AChE/BuChE-IN-2

AChE/BuChE-IN-2 is a selective inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), demonstrating IC50 values of 0.72 μM and 0.16 μM, respectively. This compound exhibits non-competitive inhibition of AChE and effectively inhibits β-amyloid (Aβ) aggregation, with an IC50 of 62.52 μM. Notably, AChE/BuChE-IN-2 is capable of crossing the blood-brain barrier, making it a valuable tool for studying neurodegenerative conditions, such as Alzheimer's disease.

Cat. No.

A78412

CAS No.

2205015-77-4

Multitarget AD inhibitor-1

Multitarget AD inhibitor-1 is a selective and reversible inhibitor of butyrylcholinesterase (BuChE), exhibiting IC50 values of 7.22 μM for human BuChE and 1.55 μM for equine BuChE. This compound also inhibits β-secretase activity (IC50 = 41.60 μM) and demonstrates a strong capacity to inhibit amyloid β aggregation (IC50 = 3.09 μM) as well as tau aggregation. As a diphenylpropylamine derivative, it holds promise for multifunctional disease-modifying applications in Alzheimer’s research.

Cat. No.

A78417

CAS No.

2983723-56-2

hAChE-IN-3

hAChE-IN-3 is a potent acetylcholinesterase (AChE) inhibitor with demonstrated blood-brain barrier permeability. It exhibits significant inhibitory effects against butyrylcholinesterase (BuChE), monoamine oxidase B (MAO-B), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1), with IC50 values of 0.44, 0.08, 5.15, and 0.38 μM, respectively. Additionally, hAChE-IN-3 possesses antioxidant properties and metal chelating ability, enabling it to interact with peripheral anion sites and influence β-amyloid accumulation. This compound holds promise for advancing research in Alzheimer's disease and related neurodegenerative disorders.

Cat. No.

A78418

CAS No.

876685-78-8

AChE-IN-63

AChE-IN-63 is a multi-target inhibitor with a primary action as a selective inhibitor of human acetylcholinesterase (hAChE), exhibiting an IC50 of 0.103 μM. This compound also demonstrates inhibitory activity against human butyrylcholinesterase (hBChE) and human beta-site amyloid precursor protein cleaving enzyme 1 (hBACE-1) with IC50 values of 10 μM and 1.342 μM, respectively. AChE-IN-63 effectively inhibits Aβ aggregation, thereby preventing the formation and deposition of Aβ1-42. Due to its ability to penetrate the blood-brain barrier and oral bioavailability, it is primarily utilized in research related to Alzheimer's disease.

Cat. No.

A78426

CAS No.

2653349-78-9

BChE-IN-8

BChE-IN-8 is a potent and orally active inhibitor of butyrylcholinesterase (BChE), demonstrating IC50 values of 0.15 nM against equine serum BChE and 45.2 nM against human BChE. Its high stability ensures enhanced blood concentration and tissue exposure. BChE-IN-8 exhibits neuroprotective and cognitive-enhancing effects through modulation of the cholinergic system, amyloid beta (Aβ) aggregation, and neuropeptide levels. This compound is particularly relevant for research into Alzheimer's disease.

Cat. No.

A78427

CAS No.

2341935-88-2

AChE/MAO-B-IN-9

AChE/MAO-B-IN-9 is a selective, reversible, non-competitive inhibitor of acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B), exhibiting an IC50 of 0.156 μM against electric eel AChE. This compound effectively inhibits the formation of Aβ40/42 fibrils, promotes the depolymerization of Aβ fibrils, and suppresses Tau protein fibril formation. Additionally, AChE/MAO-B-IN-9 demonstrates antioxidant and neuroprotective properties, while alleviating memory deficits induced by scopolamine in murine models. This reagent is valuable for research related to Alzheimer’s disease.

Cat. No.

A78428

CAS No.

2758789-03-4

AChE-IN-88

AChE-IN-88 is a novel pyridazine derivative that functions as an acetylcholinesterase (AChE) inhibitor. It exhibits potent inhibitory activity against AChE and additionally targets amyloid β protein (Aβ) aggregation, making it relevant for Alzheimer's disease research. With a pIC50 value of 7.16, AChE-IN-88 is a promising candidate for studying multi-target approaches in neurodegenerative conditions.

Cat. No.

A78429

CAS No.

2745118-93-6

BuChE-IN-2

BuChE-IN-2 is a potent inhibitor of butyrylcholinesterase (BuChE), exhibiting IC50 values of 1.28 μM and 0.67 μM against BuChE and nitric oxide production, respectively. This compound has demonstrated the ability to inhibit amyloid-beta aggregation, reduce reactive oxygen species formation, and chelate copper ions, all while effectively crossing the blood-brain barrier. BuChE-IN-2 is a valuable tool for research focused on Alzheimer's disease and related neurodegenerative disorders.

Cat. No.

A78441

CAS No.

32527-84-7

Aβ1–42 aggregation inhibitor 3

Aβ1–42 aggregation inhibitor 3 is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), with IC50 values of 1.634 μM and 0.0285 μM, respectively. This compound effectively inhibits the aggregation of Aβ1-42, making it a valuable tool in Alzheimer's disease research. Its dual inhibitory action on cholinesterases positions it as a promising candidate for studies aimed at understanding and mitigating neurodegenerative processes associated with AD.

Cat. No.

A78442

CAS No.

1776948-12-9

hBChE-IN-1

hBChE-IN-1 is a potent inhibitor of human butyrylcholinesterase (hBChE) with an IC50 value of 7 nM, demonstrating high selectivity over human acetylcholinesterase (hAChE). This compound also exhibits inhibitory activity against tau and Aβ40 protein aggregation, with IC50 values of 20 μM and 4.3 μM, respectively. hBChE-IN-1 is valuable in Alzheimer's disease research, aiding in the exploration of therapeutic strategies targeting protein aggregation associated with neurodegeneration.

Cat. No.

A78446

CAS No.

159652-53-6

(±)-Phenserine ((±)-Eseroline phenylcarbamate)

Synonyms: (±)-Eseroline phenylcarbamate

(±)Phenserine is a racemic form of the acetylcholinesterase (AChE) inhibitor Phenserine, derived from Physostigmine. This compound exhibits non-competitive and long-lasting inhibition of AChE, leading to a decrease in the formation of β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ). (±)Phenserine has been shown to enhance cognitive abilities and may help to slow the progression of Alzheimer's disease, making it a valuable agent in neurodegenerative research.

Cat. No.

A78447

CAS No.

2402753-39-1

BuChE-IN-5

BuChE-IN-5 is a potent butyrylcholinesterase (BuChE) inhibitor, exhibiting an IC50 value of 1.94 μM. This compound effectively inhibits the aggregation of amyloid-beta (Aβ) and tau proteins in Escherichia coli, demonstrating significant potential in Alzheimer's disease research. Additionally, BuChE-IN-5 possesses free radical scavenging capabilities and antioxidant activity, making it a valuable tool for studying neurodegenerative processes and related therapeutic approaches.

Cat. No.

A78477

CAS No.

2978613-03-3

hAChE-IN-7

hAChE-IN-7 is a mixed inhibitor targeting both the catalytic active site and peripheral anionic site of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBuChE). It exhibits potent inhibitory activity with IC50 values of 69.8 nM for hAChE and 68.0 nM for hBuChE, along with a notable inhibitory effect on β-secretase-1 (BACE-1) at an IC50 of 3.6 μM. This compound is valuable for research related to Alzheimer's disease, facilitating studies on cholinergic system modulation and potential therapeutic strategies.

Cat. No.

A78489

CAS No.

185154-95-4

2-Acetoxyacorenone

2-Acetoxyacorenone is a sesquiterpenoid that functions as a potent inhibitor of acetylcholinesterase (AChE) and β-secretase 1 (BACE1). Isolated from the rhizome of Acorus tatarinowii, this compound exhibits significant biological activity relevant to the modulation of cholinergic signaling and amyloid precursor protein processing. It serves as a valuable tool in Alzheimer's disease research, allowing for investigations into therapeutic strategies targeting these key enzymes.

Cat. No.

A78490

CAS No.

2479315-19-8

BACE1-IN-12

BACE1-IN-12 is a potent inhibitor of Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1), exhibiting an IC50 of 8.9 µM. This compound demonstrates selective inhibition of butyrylcholinesterase (BuChE) with an IC50 of 3.2 µM and possesses antioxidant activity with an IC50 of 10.2 μM, as assessed by the DPPH assay. BACE1-IN-12 may serve as a potentially valuable agent in Alzheimer's disease research.

Cat. No.

A78531

CAS No.

263248-16-4

TAK-802

TAK-802 is a potent orally active inhibitor of acetylcholinesterase, a key enzyme in neurotransmitter regulation. This compound demonstrates significant nonlinear pharmacokinetics, with its distribution in red blood cells showing concentration-dependent behavior. TAK-802 is primarily utilized in research applications focused on neurodegenerative disorders and cognitive function enhancement.

Cat. No.

A78533

CAS No.

312-45-8

Hemicholinium 3

Synonyms: Hemicholinium dibromide

Hemicholinium 3 is a competitive inhibitor of the high affinity choline transporter (HACU), exhibiting a Ki value of 25 nM. It acts as a neuromuscular blocking agent by inhibiting both the synthesis and release of acetylcholine (ACh). Hemicholinium 3 demonstrates key biological activities, including the inhibition of Epibatidine-induced contraction and [3H]acetylcholine release, with IC50 values of 897 nM and 693 nM, respectively. This compound is useful in research applications focused on neurotransmitter modulation and neuromuscular transmission studies.