Shop By
Catalog No.
Product Name
Application
Product Information
Citations
-
BACE1 Inhibitor
CTS-21166 is a selective inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1), designed to penetrate the blood-brain barrier effectively. It demonstrates the ability to reduce levels of amyloid-beta (Aβ) in the brain, making it a valuable tool for studying the pathogenesis of Alzheimer's disease. CTS-21166 is suitable for use in both in vitro and in vivo research applications focused on Alzheimer's and related neurodegenerative disorders. -
Amyloid-β Inhibitor
YIAD-0205 is an orally bioavailable inhibitor of amyloid-β (Aβ) aggregation, specifically targeting Aβ(1-42). This compound exhibits significant in vivo efficacy in a transgenic mouse model of Alzheimer's disease carrying five familial mutations (5XFAD). Its application lies in Alzheimer's research, particularly in studies exploring therapeutic strategies aimed at mitigating Aβ-related neurodegeneration. -
Amyloid β Inhibitor
Aβ-IN-3 is a potent inhibitor of amyloid β (Aβ) aggregation, specifically targeting Aβ42. This compound effectively inhibits the aggregation of Aβ42, making it a valuable tool in the study of amyloid-related pathologies. However, Aβ-IN-3 does not mitigate the neurotoxicity associated with Aβ42 in SH-SY5Y cells, nor does it alter the aggregation state of Aβ42 into a non-toxic form. Its primary applications lie in research focused on Alzheimer's disease and amyloid aggregation mechanisms. -
Aβ Inhibitor
PPI-1019 is an amyloid beta (Aβ) inhibitor that specifically targets the aggregation of Aβ peptides. This compound demonstrates potential neuroprotective effects, making it a valuable tool for researching neurodegenerative disorders, particularly Alzheimer's disease. Its role in modulating Aβ-related toxicity makes PPI-1019 significant for studies aimed at understanding the pathophysiology of amyloid plaque formation and developing therapeutic strategies. -
Aβ Oligomers Formation Inhibitor
Aβ-IN-6 is an Aβ oligomers formation inhibitor that effectively reduces pro-inflammatory cytokine release from microglia. This compound significantly promotes Nrf2 nuclear translocation, thereby interfering with the aggregation of Aβ oligomers. Aβ-IN-6 offers neuroprotective effects through modulation of redox-sensitive signaling pathways in in vivo oxidative stress models. Its oral bioactivity and combined anti-inflammatory, antioxidant, and anti-oligomeric properties make Aβ-IN-6 a valuable reagent for research into Alzheimer's disease. -
Prolyl Endopeptidase (PREP) Inhibitor
ONO 1603 is a selective inhibitor of prolyl endopeptidase (PREP), investigated for its potential in antidementia therapy. This compound has demonstrated neuroprotective properties and neurotrophic effects in cerebellar granule cells, enhancing neuronal survival and promoting neurite outgrowth at a concentration of 0.03 µM. Additionally, ONO 1603 increases m3-muscarinic acetylcholine receptor (mAChR) mRNA levels and stimulates mAChR-mediated signaling pathways. These pharmacological properties suggest that ONO 1603 could be a promising therapeutic agent for Alzheimer's disease by enhancing cholinergic neurotransmission and supporting neuronal function. -
Cholinesterase (ChE) Inhibitor
Pyridostigmine bromide is an orally active cholinesterase (ChE) inhibitor that enhances acetylcholine levels by inhibiting the enzyme responsible for its breakdown. This compound demonstrates significant biological activity in modulating cholinergic signaling, making it useful in studying neurodegenerative disorders and neuromuscular junction diseases. Its applications extend to cardiovascular disease research, where it can elucidate cholinergic mechanisms underlying cardiac function and dysfunction. -
MAO Inhibitor
Rosmarinic acid racemate acts as a monoamine oxidase inhibitor, specifically targeting the MAO-A and MAO-B enzymes as well as catechol-O-methyltransferase (COMT). It demonstrates inhibition with IC50 values of 50.1 μM for MAO-A, 184.6 μM for MAO-B, and 26.7 μM for COMT. This compound is useful in research applications focused on neurochemical regulation, mood disorders, and the modulation of catecholamine levels. -
COX-1 Inhibitor
FR122047 (hydrochloride) is a selective inhibitor of cyclooxygenase-1 (COX-1) with an IC50 value of 28 nM. This compound exhibits antiplatelet, analgesic, and anti-inflammatory activities, making it a valuable tool for research in the fields of pain management and cardiovascular studies. Its ability to modulate COX-1 offers insights into the therapeutic targeting of inflammatory pathways. -
Cholinesterase (ChE) Inhibitor
Corydaline is an isoquinoline alkaloid that functions as a cholinesterase (ChE) inhibitor with an IC50 of 226 μM. In addition to its cholinergic activity, Corydaline acts as a μ-opioid receptor agonist (Ki of 1.23 μM) and demonstrates significant antiviral effects by inhibiting enterovirus 71 (EV71) replication, with an IC50 of 25.23 μM. This compound also exhibits anti-angiogenic, anti-allergic, gastric-emptying, and antinociceptive properties, making it a valuable reagent for various biological research applications. -
Cholinesterase (ChE) Inhibitor
Sinapine thiocyanate is a cholinesterase (ChE) inhibitor known for its multifaceted biological activities. This alkaloid, derived from cruciferous plant seeds, exhibits anti-inflammatory, antioxidant, antitumor, anti-angiogenic, and radioprotective properties. Its ability to inhibit acetylcholinesterase (AChE) highlights its potential in research related to neurodegenerative disorders such as Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease. -
mAChR Inhibitor
Methylbenactyzium Bromide is a selective inhibitor of muscarinic acetylcholine receptors (mAChR). This compound effectively modulates cholinergic signaling pathways and is utilized in research focused on neuropharmacology, cardiovascular physiology, and respiratory function. Its ability to inhibit mAChR activity makes it a valuable tool in studies investigating the role of acetylcholine in various physiological processes and disease states. -
AChE/D2DR Inhibitor
Itopride hydrochloride is a potent acetylcholinesterase (AChE) inhibitor and dopamine D2 receptor antagonist. By enhancing gastric motility through its antidopaminergic and anti-AChE effects, Itopride hydrochloride serves as an effective gastrointestinal prokinetic agent. This compound is particularly useful for investigating conditions such as gastroesophageal reflux disease (GERD) and related gastrointestinal disorders. -
mAChR Inhibitor
Otilonium bromide is a selective inhibitor of muscarinic acetylcholine receptors (mAChR) with pronounced smooth muscle relaxant properties. This compound primarily functions by modulating calcium mobilization in intestinal smooth muscle, making it a valuable tool in the study of gastrointestinal disorders. Otilonium bromide is widely utilized in research related to irritable bowel syndrome and other smooth muscle-related conditions. -
COX Inhibitor
Zaltoprofen is a non-steroidal anti-inflammatory drug (NSAID) that acts as a preferential inhibitor of cyclooxygenase-2 (COX-2), exhibiting IC50 values of 1.3 μM for COX-1 and 0.34 μM for COX-2. It demonstrates significant anti-inflammatory and analgesic properties, making it beneficial for the management of inflammatory pain. Zaltoprofen is utilized in research settings to explore mechanisms of inflammation and pain pathways. -
mAChR Inhibitor
Camylofine is an antimuscarinic compound that selectively inhibits muscarinic acetylcholine receptors (mAChRs). It functions as a smooth muscle relaxant, making it useful in various research applications related to muscle contraction and neurotransmission. This compound is valuable for studying the physiological effects of cholinergic signaling and exploring potential therapeutic interventions for conditions related to smooth muscle hyperactivity. -
AChE Inhibitor
Acotiamide is a selective and reversible inhibitor of acetylcholinesterase (AChE), exhibiting an IC50 value of 1.79 μM. It has demonstrated the ability to enhance gastric contractility and promote accelerated gastric emptying. This compound is valuable for investigating functional dyspepsia related to gastric motility dysfunction and intestinal inflammation. -
COX-1/COX-2 Inhibitor
6-Methoxy-2-naphthoic acid is a potent inhibitor of COX-1 and COX-2 enzymes. It effectively inhibits the synthesis of gastric mucosal prostaglandin E2, making it relevant in studies related to inflammation and pain-related conditions. Additionally, 6-Methoxy-2-naphthoic acid serves as an impurity in Naproxen and can be utilized in the synthesis of various active compounds, contributing to diverse research applications in pharmaceutical development. -
COX-2 Inhibitor
Parecoxib Sodium is a selective COX-2 inhibitor that effectively penetrates the blood-brain barrier and serves as a proagent for Valdecoxib. This nonsteroidal anti-inflammatory drug (NSAID) inhibits prostaglandin synthesis, making it suitable for the relief of acute postoperative pain as well as for managing symptoms associated with chronic inflammatory conditions, including osteoarthritis and rheumatoid arthritis. It has important applications in both clinical and preclinical research focused on pain management and inflammation. -
AChEI Inhibitor, XO Inhibitor, Thromboxane Inhibitor
Imidazole acts as an inhibitor of acetylcholinesterase (AChEI), xanthine oxidase (XO), and thromboxane. This heterocyclic aromatic compound exhibits significant biological activities, including antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic properties. By inhibiting the conversion of endoperoxides (PGG2 and PGH2) to thromboxane A2, Imidazole plays a role in cardiovascular research. Additionally, its derivatives have shown potential in inhibiting the SARS-CoV-2 3CLPro enzyme, making it a valuable candidate for studies related to Alzheimer's disease, gout, COVID-19, and thrombo-embolic conditions. -
nAChR Inhibitor
(+)-Sparteine is a natural alkaloid that functions as a competitive inhibitor of nicotinic acetylcholine receptors (nAChRs). By blocking these receptors in neurons, it serves as a ganglionic blocking agent, impacting neurotransmission. This compound is utilized in research applications related to neurotransmitter signaling and the study of ganglionic transmission. -
Cholinesterase (ChE) Inhibitor
Demecarium Bromide is a potent cholinesterase (ChE) inhibitor, exhibiting an apparent affinity (Kiapp) of 0.15 μM. It primarily functions by inhibiting the enzyme cholinesterase, thereby increasing acetylcholine levels. This compound is widely utilized in research related to glaucoma treatment and the study of acetylcholine metabolism, providing valuable insights into neurodegenerative diseases and neurotransmission pathways. -
COX Inhibitor
Tolmetin sodium dihydrate is a potent non-steroidal anti-inflammatory drug (NSAID) that primarily targets cyclooxygenase (COX) enzymes, exhibiting IC50 values of 0.35 μM for human COX-1 and 0.82 μM for COX-2. This compound is commonly utilized in research related to inflammation and pain modulation. Its ability to effectively inhibit COX activity makes it valuable for studying various inflammatory pathways and developing new therapeutic strategies in pain management. -
mAChR Inhibitor
Tolterodine is an mAChR inhibitor that competitively binds to acetylcholine, leading to a reduction in sympathetic excitation and inhibition of involuntary bladder muscle contractions. It is known to restore the Nrf2/NF-κB signaling pathway, providing protection against inflammatory responses and ferroptosis. Additionally, Tolterodine mitigates LPS-induced reactive oxygen species production and lipid oxidation, making it valuable for research in urinary tract infections and overactive bladder conditions. -
Acetylcholinesterase Inhibitor
Neostigmine methyl sulfate is a reversible inhibitor of acetylcholinesterase, primarily targeting the peripheral nervous system. This compound enhances cholinergic transmission by preventing the breakdown of acetylcholine, resulting in increased neurotransmitter levels at the neuromuscular junction. It is widely used in research applications related to neuromuscular disorders and pharmacological studies of cholinergic function. -
Monoamine Oxidase Inhibitor
Minaprine dihydrochloride is a selective monoamine oxidase inhibitor that penetrates the blood-brain barrier. It exhibits biological activity by reducing intraneuronal dopamine metabolism, lowering levels of striatal homovanillic acid and dihydroxyphenylacetic acid, while increasing levels of 3-methoxytyramine and 5-hydroxytryptamine in the striatum. Additionally, Minaprine dihydrochloride weakly inhibits acetylcholinesterase activity and displays both convulsant and antidepressant properties, making it a valuable reagent for research in neuropharmacology and mood disorder studies. -
Amyloid-β Inhibitor
Dihydroergocristine mesylate is a potent inhibitor of γ-secretase, targeting the enzyme responsible for the generation of amyloid-β peptides implicated in Alzheimer’s disease. It effectively reduces the production of these peptides by binding directly to γ-secretase and Nicastrin, exhibiting equilibrium dissociation constants (Kd) of 25.7 nM and 9.8 μM, respectively. This compound can be utilized in research aimed at unraveling the mechanisms of Alzheimer’s pathology and developing potential therapeutic strategies. -
mAChR Inhibitor
Trospium chloride is a selective and competitive antagonist of muscarinic acetylcholine receptors (mAChRs). It exhibits potent antimuscarinic activity by binding with high affinity to M1, M2, and M3 receptor subtypes, while showing no interaction with nicotinic cholinergic receptors. This compound is primarily utilized in research related to neurological conditions and to explore the pharmacological modulation of cholinergic signaling. -
AChE Inhibitor
Ambenonium chloride is a potent, reversible inhibitor of acetylcholinesterase (AChE), demonstrating a high affinity for the enzyme. With an IC50 value of 0.7 nM for human AChE, this compound effectively enhances cholinergic transmission. It is primarily utilized in research applications focused on neurological disorders, particularly those involving impaired cholinergic function. -
COX Inhibitor
Hamaudol is a chromone derived from Saposhnikovia divaricata, acting as a potent inhibitor of cyclooxygenase (COX)-1 and COX-2, with IC50 values of 0.30 mM and 0.57 mM, respectively. This compound exhibits significant analgesic and anti-inflammatory properties, making it a valuable tool in research focused on pain relief and inflammation modulation. Hamaudol is suitable for investigations into COX inhibition and related biological pathways. -
AChE Inhibitor
1,1'-Bi-2-naphthol is a potent acetylcholinesterase (AChE) inhibitor, demonstrating an IC50 value of 21.9 μM against human AChE. This compound also exhibits cytotoxic effects on Artemia nauplii, making it valuable for studies in neuropharmacology and toxicology. Its dual functionality positions it as a useful reagent in researching cholinergic signaling and the potential effects of AChE inhibition. -
Cholinesterase (ChE) Inhibitor
Physostigmine, a reversible acetylcholinesterase (AChE) inhibitor, effectively increases acetylcholine levels in the central nervous system by crossing the blood-brain barrier. This compound enhances cholinergic neurotransmission and has been shown to reverse memory deficits in transgenic mice models of Alzheimer's disease. Additionally, Physostigmine serves as a critical antidote for anticholinergic poisoning, providing valuable insights for neuropharmacological research and therapeutic applications. -
ChE Inhibitor
Flavonol is a cholinesterase (ChE) inhibitor, demonstrating an IC50 of 120 μM and a Ki value of 74 μM. This compound exhibits notable antioxidant, free radical-scavenging, and antibacterial activities, while also modulating immune responses. Flavonol effectively inhibits the PriA helicase in Staphylococcus aureus and reduces nitric oxide (NO) production in LPS-activated RAW 264.7 cells by downregulating iNOS expression. Its protective and analgesic effects in murine models suggest potential applications in research focused on tumors and atherosclerosis. -
nAChR Inhibitor
Adiphenine is a non-competitive inhibitor of nicotinic acetylcholine receptors (nAChR), exhibiting IC50 values of 1.9 μM for α1, 1.8 μM for α3β4, 3.7 μM for α4β2, and 6.3 μM for α4β4. This compound demonstrates significant anticonvulsant properties, making it valuable for studies related to seizure disorders and neuropharmacology. Its selective action on various nAChR subtypes positions Adiphenine as a useful tool for exploring the role of these receptors in different biological contexts. -
COX Inhibitor
Methylhydroquinone is a potent COX inhibitor with noted activity against ovine COX-1 and human recombinant COX-2, exhibiting IC50 values of 480.7 μM and 52.2 μM, respectively. This compound demonstrates anti-inflammatory properties primarily through the inhibition of prostaglandin synthesis. Additionally, it has been associated with potential DNA-damaging effects, including the induction of DNA single-strand breaks. Methylhydroquinone functions by competitively binding to the active sites of COX-1, engaging in non-covalent interactions to exert its biological activities. -
AChE Inhibitor
Buphanidrine is an acetylcholinesterase (AChE) inhibitor with an IC50 of 52.8 μM. This compound, isolated from Brunsvigia josephinae, demonstrates significant potential in the study of neurodegenerative diseases, particularly Alzheimer's disease. Its ability to modulate cholinergic signaling makes it a valuable tool for understanding the pathophysiology of cognitive decline and exploring therapeutic strategies.
