Catalog No.
Product Name
Application
Product Information
Citations
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AChE/GSK-3β Inhibitor
AChE/GSK-3β-IN-1 is a dual inhibitor targeting acetylcholinesterase (AChE) and glycogen synthase kinase 3 beta (GSK-3β), demonstrating potent inhibition with IC50 values of 1.2 nM for hAChE, 149.8 nM for hBChE, and 22.4 nM for hGSK-3β. This compound effectively penetrates the blood-brain barrier and displays high selectivity for the CMGC kinase family, particularly binding to the ATP site of DYRK1A. Additionally, AChE/GSK-3β-IN-1 has been shown to inhibit reactive oxygen species (ROS) expression, thereby reducing oxidative stress. It is a valuable tool for research into Alzheimer's disease and related neurodegenerative conditions. -
AChE/BChE/BACE-1 Inhibitor
AChE/BChE/BACE-1-IN-2 is a potent oral inhibitor of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1), exhibiting IC50 values of 0.069 μM, 0.127 μM, and 0.097 μM, respectively. This compound demonstrates significant binding affinity to the peripheral anionic site of AChE, high brain permeability, and the ability to disassemble amyloid-beta (Aβ) aggregates. Additionally, AChE/BChE/BACE-1-IN-2 provides neuroprotective effects against Aβ-induced stress and possesses noteworthy antioxidant properties, making it suitable for research in neurodegenerative disease models. -
nAChR Antagonist
Mecamylamine is a nonselective, noncompetitive antagonist of nicotinic acetylcholine receptors (nAChR). It functions as a ganglionic blocker and is capable of crossing the blood-brain barrier. Mecamylamine is utilized in research focused on neuropsychiatric disorders, hypertension, and the development of antidepressant therapies. -
AChE/BChE Inhibitor
AChE-IN-14 is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), displaying IC50 values of 0.46 μM for electric eel AChE, 0.48 μM for human recombinant AChE, and 0.44 μM for equine serum BChE. In addition to its cholinesterase inhibition, AChE-IN-14 has a high affinity for the human H3 receptor (H3R) with a Ki value of 159.8 nM. This compound is particularly relevant for research focused on neurodegenerative diseases such as Alzheimer’s disease, where the modulation of cholinergic signaling is critical. -
Antihistamine Agent
Difeterol is an antihistamine agent that functions primarily as a histamine-1 receptor antagonist. It also inhibits butyrylcholinesterase (BChE), making it a valuable tool for studying cholinergic pathways. This compound is particularly relevant for research related to Alzheimer's disease, where modulation of histamine and cholinergic systems may provide insights into therapeutic strategies. -
Antioxidant
Contilisant is a potent antioxidant and neuroprotective agent that targets histamine H3 receptors. It effectively inhibits monoamine oxidases and cholinesterases, contributing to its neuroprotective profile. With a binding affinity of 65.23 nM towards human sigma-1 receptor, Contilisant demonstrates significant therapeutic potential. In preclinical studies, it has been shown to restore cognitive deficits induced by Aβ1-42 in the radial maze assay, making it a valuable tool for Alzheimer's disease research. -
mAChR Antagonist
GS 283 is a muscarinic acetylcholine receptor (mAChR) antagonist that exhibits calcium antagonist properties. This compound effectively modulates smooth muscle contraction by inhibiting contractions induced by carbachol and histamine in guinea pig tracheal smooth muscle, as well as high H+ levels in both guinea pig and rat tracheal smooth muscle. Additionally, GS 283 has been shown to inhibit Ca2+-induced contractions, and at elevated concentrations, it can completely abolish carbachol-induced contractions in a Ca2+-free environment. This makes GS 283 a valuable tool for research related to respiratory physiology and the pharmacological modulation of smooth muscle activity. -
Histamine H3 Receptor Antagonist
AChE/BChE-IN-21 is a histamine H3 receptor antagonist that also functions as a calcium channel blocker and acetylcholinesterase inhibitor. This compound demonstrates neuroprotective properties against oxidative stress induced by H2O2 and amyloid-beta peptide Aβ1-40. Additionally, AChE/BChE-IN-21 has been shown to improve cognitive function in mouse models of Alzheimer's disease, making it a valuable tool for research into neurodegenerative disorders. -
H3R Antagonist
H3R Antagonist 2 is a selective antagonist of the histamine H3 receptor (H3R) with a Ki value of 170 nM for human H3R. This compound demonstrates inhibitory activity against acetylcholinesterase, butyrylcholinesterase, and human monoamine oxidase B (hMAO B), with IC50 values of 180 nM, 880 nM, and 775 nM, respectively. Additionally, H3R Antagonist 2 exhibits promising anti-neuropathic pain and memory-enhancing effects, effectively crossing the blood-brain barrier (BBB). This makes it a valuable tool for research in neuropharmacology and cognitive enhancement studies. -
mAChR antagonist
Atropine is a competitive antagonist for the muscarinic acetylcholine receptor types M1, M2, M3, M4 and M5. -
muscarinic receptor antagonist
Biperiden hydrochloride is a muscarinic receptor antagonist that displays some selectivity for the M1 subtype -
Gamma-secretase inhibitor
BMS-708163 is an oral gamma secretase inhibitor designed for selective inhibition of amyloid beta synthesis. -
Muscarinic receptor agonist
Bethanechol is a parasympathomimetic choline carbamate that selectively stimulates muscarinic receptors without any effect on nicotinic receptors. -
COX-2 inhibitor
Celecoxib is a sulfa non-steroidal anti-inflammatory drug (NSAID) and selective COX-2 inhibitor used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain, painful menstruation and menstrual symptoms, and to reduce numbers of colon and rectum polyps in patients with familial adenomatous polyposis.
- Chlormezanone (Trancopal), a non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm. Chlormezanone binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.
- (+)-Clopidogrel hydrogen sulfate is an oral, thienopyridine class antiplatelet agent used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.
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Dihydropyrimidinase Inhibitor
Dihydromyricetin (Ampelopsin (flavanol); Ampeloptin) is a natural antioxidant with good prospects. -
COX inhibitor
Diclofenac Sodium is a non-selective COX inhibitor with IC50 of 0.5 μg/ml and 0.5 μg/ml for COX-1 and -2 in intact cells, respectively, used as a nonsteroidal anti-inflammatory drug (NSAID) to relieve pain and reduce swelling in flammation. -
Neuroprotectant
Dimebon dihydrochloride is a non-selective antihistamine that displays cognitive enhancing abilities. -
AChE inhibitor
Donepezil is a centrally acting reversible acetylcholinesterase inhibitor. -
COMT inhibitor
Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment. -
AChR antagonist
Fesoterodine fumarate is a medicine which is used in urinary urgency, reducing the frequency of passing urine and urge urinary incontinence -
Benzodiazepine antagonist
Flumazenil, an imidazobenzodiazepine derivative, antagonizes the actions of benzodiazepines on the central nervous system. Flumazenil competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex. Flumazenil is a weak partial agonist in some animal models of activity, but has little or no agonist activity in humans. -
nonsteroidal anti-inflammatory agent
Flurbiprofen is a nonsteroidal anti-inflammatory agent (NSAIA) with antipyretic and analgesic activity. - Furosemide is a non-competitive antagonist at GABAA receptors with ~ 100-fold greater selectivity for α6-containing receptors than α1-containing receptors.
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AChE inhibitor
Galanthamine is an AChE inhibitor with IC50 of 14 nM. -
mAChR M2 antagonist
Gallamine Triethiodide is a mAChR M2 antagonist with pronounced cardioselectivity. -
COX-1 inhibitor
Ibuprofen Lysine(Motrin) is a non-steroidal anti-inflammatory drug. - Ipratropium bromide is a muscarinic antagonist, bronchodilator, N-Isopropyl salt of atropine.
- Rsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
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COX-1/COX-2 inhibitor
Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively. - Methscopolamine bromide is a competitive antimuscarinic agent that blocks the binding of acetylcholine at muscarinic acetylcholine receptors (mAChR M).
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COX inhibitor
Naproxen sodium is a non-selective cyclooxygenase (COX) inhibitor that displays anti-inflammatory, antipyretic and analgesic effects. Has a neuroprotective role against colchicine-induced cognitive impairment and oxidative stress. - Nefiracetam is cognitive enhancer. It activates L/N-type calcium channels, cholinergic, monoaminergic and GABAergic systems.
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AChE inhibitor
Neostigmine bromide is a reversible acetylcholine esterase inhibitor that binds to the anionic binding site of AChE. - Oxybutynin(Ditropan) is an anticholinergic medication used to relieve urinary and bladder difficulties.
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α-adrenergic (AR) antagonist/CaM inhibitor
Phenoxybenzamine is a cell-permeable, non-specific, irreversible α-adrenergic (AR) antagonist that also acts as an CaM inhibitor. -
COX inhibitor
Phenylbutazone is a compound of research interest as an anti-inflammatory and anti-proliferative agent. -
COX inhibitor
Piroxicam is an effective and potent inhibitor of prostaglandin synthesis and a Cox-1 and Cox-2 inhibitor. -
platelet inhibitor
Prasugrel is a novel platelet inhibitor used for the reduction of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome who are to be managed with PCI. - Pyrantel pamoate is a deworming agent in the treatment of hookworms (all species) and roundworms in domesticated animal; acts as a depolarizing neuromuscular blocking agent.
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AchR antagonist
Rocuronium Bromide is a competitive AchR antagonist, used in modern anaesthesia. -
muscarinic receptor antagonist
SVT-40776 is a novel M3 muscarinic receptor antagonist, for the treatment of overactive bladder. -
GABA uptake inhibitor
SKF 89976A hydrochloride is a potent inhibitor of GABA uptake with IC50 of 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively. -
COX inhibitor
Sulindac is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions
