Catalog No.
Product Name
Application
Product Information
Citations
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Anticholinergic Agent
Mazaticol is an anticholinergic agent targeting muscarinic acetylcholine receptors. It effectively blocks cholinergic nerve activity and serves as a potent inhibitor of 3H-QNB and 3H-PZ binding, demonstrating high affinity for M2 receptors. Additionally, Mazaticol exhibits inhibitory effects on dopamine uptake in striatal nerve terminals, making it valuable for research into parkinsonian syndromes. -
Pro-cholinergic Agent
Deanol pidolate is an orally active pro-cholinergic agent that enhances cognitive function by promoting the release of acetylcholine (ACh), while minimizing the side effects commonly associated with cholinesterase inhibitors. It has demonstrated the ability to mitigate the negative impacts of scopolamine on long-term memory, facilitating a quicker recovery to baseline memory performance. Deanol pidolate is particularly useful in research applications related to Alzheimer's disease and other cognitive disorders. -
mAChR Antagonist
UH-AH 37 is a selective antagonist of muscarinic acetylcholine receptors (mAChR). It demonstrates enhanced potency in inhibiting muscarinic responses in intestinal tissue compared to cardiac tissue. This compound is valuable for research into gastrointestinal motility disorders and the pharmacological modulation of mAChR signaling pathways. -
M4 Modulator
VU6008677 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor, with an EC50 value of 120 nM for hM4. This compound enhances receptor activity and is valuable for studying M4 receptor functions and related signaling pathways. Additionally, VU6008677 demonstrates inhibition of cytochrome P450 and possesses favorable pharmacokinetic properties in rat models, making it suitable for in vivo research applications. -
Bronchospasmolytic Agent
Flutropium bromide is a potent bronchospasmolytic agent that exerts its effects through anticholinergic action. It is effective in suppressing bronchospasms and is primarily utilized in research related to asthma and chronic obstructive pulmonary disease (COPD). This compound provides valuable insights into respiratory mechanisms and potential therapeutic interventions for obstructive airway disorders. -
Presynaptic Cholinergic Modulator
SM-21 maleate serves as a presynaptic cholinergic modulator and binds to central muscarinic receptors with an affinity of 0.174 μM. This compound exhibits significant biological activity related to cholinergic signaling, making it a valuable tool for studying synaptic transmission and neuropharmacology. Its application in research may provide insights into cholinergic dysfunctions and potential therapeutic targets for neurological disorders. -
mAChR Inhibitor
Cyclobuxine D is a steroidal alkaloid that functions as a muscarinic acetylcholine receptor (mAChR) inhibitor. It exhibits a notable bradycardic effect in rat models and effectively inhibits contractions induced by acetylcholine and Ba++ in isolated rabbit jejunum muscle. Due to its biological activities, Cyclobuxine D is valuable for research in pharmacology and cardiovascular studies. -
Stable Isotope
Tolterodine-d14 hydrochloride is a deuterium-labeled version of Tolterodine hydrochloride, a potent muscarinic acetylcholine receptor (mAChR) inhibitor. This compound competitively binds to acetylcholine, thereby reducing involuntary bladder muscle contractions and modulating sympathetic nervous activity. In addition to its role in managing overactive bladder and urinary tract infections, Tolterodine has been shown to restore the Nrf2/NF-κB signaling pathway, offering protective effects against inflammation and ferroptosis. Its applications extend to studies involving reactive oxygen species and lipid oxidation. -
Muscarinic M1 Receptor Agonist
Muscarinic M1 receptor agonist-1 is a selective agonist targeting the muscarinic M1 receptor. This compound plays a significant role in modulating neurotransmission and is of particular interest in the study of psychiatric disorders, including schizophrenia. Its ability to activate the M1 receptor may provide insights into therapeutic strategies for managing cognitive dysfunction associated with these conditions. -
Sigma 1 Recognition Site Ligand
RLH-033 is a potent and selective ligand for the sigma 1 recognition site. It exhibits high affinity for sigma 1 sites labeled by [3H](+)-pentazocine, demonstrating a Ki value of 50 pM. This compound is valuable for research applications targeting sigma 1 receptor functions, contributing to the understanding of its roles in neuroprotection and various pathophysiological conditions. -
mAChR Antagonist
AQ-RA 721 is a selective muscarinic acetylcholine receptor (mAChR) antagonist that exhibits a differential affinity for the M2 and M4 receptor subtypes. This compound is valuable for studying muscarinic receptor diversity and function, facilitating research into receptor pharmacology and potential therapeutic applications. It can be employed in investigations into central nervous system activities and cardiovascular regulation, contributing to a better understanding of muscarinic signaling pathways. -
M1 Receptor Partial Agonist
Sabcomeline is a selective partial agonist of the muscarinic M1 receptor, known for its ability to enhance cognitive function. This compound holds promise for research applications related to Alzheimer's disease, where modulation of the M1 receptor may assist in ameliorating cognitive deficits. Its functional selectivity makes Sabcomeline a valuable tool for investigating the role of muscarinic receptors in neurodegenerative disorders. -
M1 Cholinergic Agonist
Trans-Cevimeline hydrochloride is a selective M1 cholinergic agonist, known for its potential in modulating cholinergic neurotransmission. This compound exhibits significant biological activity relevant to neurodegenerative conditions, particularly Alzheimer's disease. Researchers can utilize trans-Cevimeline hydrochloride to investigate its effects on cognitive function and cholinergic signaling pathways. -
M3 Muscarinic Receptor Antagonist
AE9C90CB is a selective antagonist of the M3 muscarinic receptor, exhibiting a high affinity with a pKi value of 9.90. This compound is 20-fold more selective for M3 compared to the M2 muscarinic receptor, making it a valuable tool for studying M3 receptor-mediated signaling pathways. AE9C90CB is suitable for research applications investigating the role of M3 muscarinic receptors in various physiological and pathological processes. -
mAChR Agonist
CDD0102 Hydrochloride is a potent agonist of the M1 muscarinic acetylcholine receptor (mAChR). This compound exhibits significant biological activity in modulating cholinergic signaling, making it valuable for research into neurological disorders and cognitive function. Its application extends to studying M1 receptor-related pathways and developing potential treatments for conditions such as Alzheimer's disease and schizophrenia. -
mAChR Antagonist
4,4-Difluorobenzhydrol serves as a precursor for a muscarinic acetylcholine receptor (mAChR) antagonist, with potential applications in neuroscience research. Its derivative, 4,4-Difluorobenzhydrol Carbamate, can selectively target the M1 receptor subtype. This specificity makes 4,4-Difluorobenzhydrol an important compound for studying the physiological roles of mAChRs and developing therapeutics for related disorders. -
Stable Isotope
Itopride-d6 hydrochloride is a deuterium-labeled derivative of Itopride hydrochloride that serves as a stable isotope. Itopride functions as a gastroprokinetic agent by inhibiting acetylcholinesterase (AChE) and antagonizing dopamine D2 receptors. This compound is valuable for studies investigating gastrointestinal motility and neurotransmitter interactions, as well as for tracing and quantifying its metabolic pathways in biological research. -
Phosmet Metabolite
Phosmet oxon is a potent metabolite of phosmet, functioning primarily as a cholinesterase inhibitor. This compound exhibits significant neurotoxic activity, making it relevant in studies investigating insecticidal mechanisms and their effects on cholinergic signaling pathways. Phosmet oxon's utility extends to research on pesticide metabolism and its implications for environmental toxicology and safety assessments. -
Corydaline Metabolite
Isocorybulbine is a primary metabolite of Corydaline, produced in human liver microsomes and liver cells. It exhibits significant biological activities, including anti-acetylcholinesterase and anti-allergic effects. This compound is valuable for metabolic studies of Corydaline, contributing to research in pharmacology and potential therapeutic applications. -
AChE Inhibitor
Donepezil N-oxide is an acetylcholinesterase (AChE) inhibitor derived from Donepezil. It exhibits significant biological activity by inhibiting AChE in human erythrocytes, which is crucial for regulating acetylcholine levels in neurological pathways. This reagent is utilized in research focused on Alzheimer's disease and other cognitive disorders where modulation of cholinergic transmission is a key area of investigation. -
Disulfoton Oxidation Metabolite
Demeton-S sulfone is the oxidative metabolite of the organophosphorus insecticide Disulfoton, primarily targeting acetylcholinesterase. This compound exhibits significant acetylcholinesterase inhibition, which is essential for studying neurotoxic effects related to organophosphate exposure. It serves as a crucial reagent for evaluating the biochemical pathways of organophosphate metabolism and understanding their environmental and health impacts. -
Pesticide Metabolite
Malaoxon is a pesticide metabolite that serves as an inhibitor of acetylcholinesterase, impacting neurotransmitter regulation. This compound has been shown to induce cellular death in cultured human pulmonary cells, making it relevant for studies on pulmonary toxicity and its underlying mechanisms. Its application extends to research focused on the toxicological effects of pesticide exposure in human respiratory systems. -
Drug Metabolite Control
4-Hydroxypentanoate sodium is an active metabolite of gamma-Valerolactone, functioning primarily as a sedative. Its primary mechanism involves modulation of GABA receptors, leading to enhanced inhibitory neurotransmission. This compound is utilized in pharmacological research to study drug metabolism and to evaluate sedative effects in various experimental models. -
Drug Metabolite Control
7-Bromo-5-(2-fluorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one is a primary metabolite of Flubromazepam, acting on the central nervous system through modulation of GABA receptors. This compound exhibits potential anxiolytic and sedative properties, making it relevant for studies on drug metabolism and pharmacokinetics. Its application is beneficial in research focused on benzodiazepine derivatives and their metabolic pathways. -
Etoricoxib Metabolite
Etoricoxib N1'-oxide is a metabolite of Etoricoxib that serves as an important biochemical marker in pharmacological studies. This compound is notable for its lack of inhibition on both COX-1 and COX-2 enzymes, making it a valuable tool for researchers investigating the metabolic pathways and safety profiles of COX inhibitors. Its characterization can aid in understanding the pharmacodynamics and pharmacokinetics of Etoricoxib in clinical settings. -
P2X1 Receptor Activator
Diadenosine pentaphosphate (pentasodium) is an agonist and negative modulator of the P2X1 receptor, an important endogenous purine dinucleotide primarily sourced from platelets. This compound is known to negatively regulate dendritic growth and branching by activating both homologous and heterologous P2X1 receptors, resulting in a modest transient increase in intracellular calcium levels in dendritic growth cones. Diadenosine pentaphosphate demonstrates selective inhibition of dendrite growth in cultured hippocampal neurons while leaving axon growth unaffected. Its presence in secretory vesicles such as platelets and brain synaptosomes highlights its biological relevance in neurophysiological studies. -
Cholinesterase (ChE) Inhibitor
N-Desmethyl Galanthamine is a potent cholinesterase inhibitor, specifically targeting acetylcholinesterase (AChE) with an IC50 value of 2.76 μM. As a metabolite of Galanthamine, it holds significant relevance in neuropharmacological research. This compound is utilized in studies related to Alzheimer's disease, providing insights into therapeutic strategies aimed at enhancing cholinergic transmission. -
Aldicarb Metabolite
Aldicarb sulfoxide is a metabolite of aldicarb that primarily interacts with glutathione-linked enzymes in CHO-K1 cells. This compound exhibits inhibitory activity against cholinesterase (ChE) and carboxylesterase (CaE), with an IC50 of 10 μM in zebrafish models. Its mechanism of action and biological activity make it a valuable tool for research on neurotoxicology and enzymatic regulation. -
COX Inhibitor
1-Oxo Ibuprofen is a cyclooxygenase (COX) inhibitor, specifically targeting COX-1 and COX-2 enzymes. As a degradation product and potential impurity of Ibuprofen, it demonstrates significant anti-inflammatory activity with IC50 values of 13 μM for COX-1 and 370 μM for COX-2. This compound is useful for research applications involving the study of prostaglandin synthesis and the metabolic pathways of nonsteroidal anti-inflammatory drugs. -
AChE Inhibitor
3-Hydroxycarbofuran is a reversible inhibitor of acetylcholinesterase (AChE), acting primarily by competing with acetylcholine at the enzyme's active site. This compound serves as a significant metabolite of Carbofuran and exhibits notable biological activity in the modulation of cholinergic signaling. It is utilized in research related to neurobiology, toxicology, and pesticide biochemistry, providing insights into the effects of AChE inhibition on synaptic transmission and potential neurotoxic mechanisms. -
α-Amylase Inhibitor
α-Amylase-IN-3 is a potent inhibitor of α-Amylase, exhibiting an IC50 of 18.04 μM, and also targets acetylcholinesterase (AChE) with IC50s of 21.04 μM and 22.2 μM, respectively. This compound demonstrates antioxidant activity, making it valuable for studies related to diabetes and diseases associated with oxidative stress. Its biochemical properties make α-Amylase-IN-3 a useful tool for researchers investigating metabolic disorders and neuroprotective mechanisms. -
α-glucosidase/α-amylase enzyme Dual Inhibitor
α-Amylase/α-Glucosidase-IN-7 is a competitive dual inhibitor targeting α-glucosidase and α-amylase, demonstrating IC50 values of 18.52 µM and 20.25 µM, respectively. Additionally, this compound effectively inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 values of 9.25 µM and 10.06 µM. α-Amylase/α-Glucosidase-IN-7 is valuable for research applications related to diabetes and Alzheimer’s disease. -
CES Inhibitor
Dibromsalicil is a selective inhibitor of carboxylesterases (CES), exhibiting inhibitory activity with IC50 values of 72.7 nM against human intestinal carboxylesterase (hiCE) and 53.5 nM against rabbit liver carboxylesterase (rCE). This compound demonstrates minimal activity against human liver carboxylesterase (hCE1) and cholinesterase, making it a valuable tool for research applications focused on drug metabolism and enzymatic activity modulation. Its specificity for hiCE and rCE positions Dibromsalicil as an important reagent for studying carboxylesterase-related pathways. -
AChE/CES Inhibitor
Heptenophos is a potent inhibitor of acetylcholinesterase (AChE) and plasma carboxylesterase (CES). By obstructing AChE activity, Heptenophos leads to the accumulation of acetylcholine at cholinergic synapses, which can result in symptoms characteristic of organophosphate poisoning. Its rapid toxicity in animal models, such as male albino mice, allows for the investigation of detoxification strategies, particularly in conjunction with agents like obidoxime and Memantine. This compound is widely utilized in research exploring the mechanisms underlying organophosphate effects and potential antidotal treatments. -
COMT Inhibitor
Neluxicapone is a potent inhibitor of catechol-O-methyltransferase (COMT), primarily utilized in the research of Parkinson's disease (PD). By inhibiting COMT, this compound enhances dopamine levels in the brain, which may alleviate motor symptoms associated with PD. Researchers can use neluxicapone to investigate its pharmacological effects and potential therapeutic benefits in neurodegenerative conditions. -
Hydroxycinnamic Acid
5-Hydroxyferulic acid is a hydroxycinnamic acid derived from the phenylpropanoid pathway. It serves as a key precursor in the biosynthesis of sinapic acid and acts as a non-esterified substrate for catechol-O-methyltransferase (COMT). This compound is utilized in various research applications focused on studying phenolic compounds and their roles in plant metabolism and health benefits. -
COMT Inhibitor
Ro 41-0960 is a selective inhibitor of catechol-O-methyltransferase (COMT), which plays a crucial role in the metabolism of catecholamines. By inhibiting COMT, this compound enhances the levels of neurotransmitters such as dopamine, norepinephrine, and epinephrine. It is widely used in research to investigate the biochemical pathways of neurotransmission and to explore potential therapeutic applications in conditions such as Parkinson's disease and other neuropsychiatric disorders. -
COMT Inhibitor
Nitecapone is an orally active and short-acting catechol-O-methyltransferase (COMT) inhibitor. It exhibits notable gastroprotective and antioxidant properties by scavenging reactive oxygen and nitrogen species, thereby preventing lipid peroxidation. Nitecapone is valuable in research applications focusing on neurodegenerative diseases and other conditions where COMT modulation may play a therapeutic role. -
COMT
3-O-Methyldopa monohydrate is a notable metabolite of L-DOPA, primarily interacting with catechol O-methyltransferase (COMT). It does not function as a substrate or inhibitor of L-amino acid decarboxylase, distinguishing it from its precursor. The inhibition of COMT by this compound may enhance the therapeutic effects of L-DOPA in Parkinson's disease, making it a valuable tool in neurological research and studies on Parkinson's treatments. -
hMAO-B/MB-COMT Inhibitor
hMAO-B/MB-COMT-IN-1 is a dual inhibitor of human monoamine oxidase B (hMAO-B) and membrane-bound catechol-O-methyltransferase (MB-COMT), exhibiting IC50 values of 2.5 µM and 3.84 µM, respectively. This compound is effective in protecting cells from oxidative damage, making it a valuable tool for studying neurodegenerative diseases, including Parkinson's Disease. Its dual inhibition profile provides insights into the molecular mechanisms underlying these conditions and aids in the development of potential therapeutic strategies. -
COMT Inhibitor
S-Adenosylhomocysteine sulfoxide is a potent inhibitor of catechol-O-methyltransferase (COMT) with an IC50 value of 860 μM. This compound is utilized in research to investigate the modulation of methylation reactions, providing valuable insights into biochemical pathways involving methyltransferases. Its inhibitory properties make it a significant tool for studies related to neurotransmitter metabolism and epigenetic regulation. -
Stable Isotope
Entacapone-d10 is a deuterium-labeled version of Entacapone, a potent, reversible inhibitor of catechol-O-methyltransferase (COMT). This compound selectively inhibits COMT with IC50 values of 10 nM in rat brain, 20 nM in erythrocytes, and 160 nM in liver, demonstrating minimal interaction with other catecholamine metabolizing enzymes. Entacapone-d10 is utilized primarily in research related to Parkinson's disease and metabolic disorders, serving as an FTO demethylation inhibitor with an IC50 of 3.5 μM. -
COMT Inhibitor
U-0521 is a selective inhibitor of catechol-O-methyltransferase (COMT), an enzyme involved in the metabolism of catecholamines. This compound exhibits significant biological activity by modulating neurotransmitter levels, which is crucial for investigations into Parkinson's disease and related disorders. U-0521 is valuable for research focused on understanding the role of COMT in neurodegenerative conditions and for exploring potential therapeutic strategies targeting this pathway. -
COMT Inhibitor
(Z)-Entacapone is a selective inhibitor of catechol-O-methyltransferase (COMT), crucial for catecholamine metabolism. This compound serves as a valuable tool in studying COMT's role in neurological disorders and drug metabolism. Additionally, it may appear as a potential impurity in commercial Entacapone preparations or as a degradation product due to UV light exposure, providing further relevance in quality control and biological research applications. -
Hydroxycinnamic Acid
(E)-5-Hydroxyferulic acid is an isomer of the hydroxycinnamic acid class, functioning as a key intermediate in the phenylpropanoid pathway. It plays a crucial role as a precursor in the biosynthesis of sinapic acid and serves as a non-esterified substrate for catechol-O-methyltransferase (COMT). This compound is important for studying metabolic pathways and the functions of phenolic compounds in various biological systems. -
hMAO-B/MB-COMT Inhibitor
hMAO-B/MB-COMT-IN-2 is a potent dual inhibitor of hMAO-B and MB-COMT, exhibiting IC50 values of 4.27 μM and 2.69 μM, respectively. This compound effectively protects cells from oxidative damage, making it valuable for studies related to neurodegenerative diseases. hMAO-B/MB-COMT-IN-2 is particularly relevant in the research of conditions such as Parkinson’s Disease, offering insights into potential therapeutic strategies. -
COMT Inhibitor
COMT-IN-1 is a potent catechol-O-methyltransferase (COMT) inhibitor, demonstrating an IC50 of 0.37 μM for COMT activity. This nitrophenolic analogue effectively inhibits monoamine oxidase A (MAO-A) and MAO-B with IC50 values of 95.58 μM and 58.82 μM, respectively. With good blood-brain barrier permeability, COMT-IN-1 enhances dopamine levels and alleviates symptoms associated with MPTP-induced Parkinson's disease in murine models, making it a valuable tool for research into Parkinson's disease and dopamine metabolism. -
COMT Inhibitor
CGP 28014 is a potent inhibitor of catechol-O-methyltransferase (COMT), an enzyme involved in the metabolism of catecholamines. This compound has been shown to lower homovanillic acid (HVA) levels and increase dihydroxyphenylacetic acid (DOPAC) levels in the striatum of rat models. CGP 28014 is valuable in research focused on the pathophysiology and potential treatment strategies for Parkinson's disease, providing insights into dopaminergic signaling and neurotransmitter dynamics. -
COMT Inhibitor
BIA 3-335 is a potent inhibitor of catechol-O-methyltransferase (COMT), an enzyme involved in the metabolism of catecholamines. Its primary mechanism disrupts the methylation of catechols, leading to increased levels of dopamine, which may be beneficial in the study of Parkinson's disease and related neurological disorders. This compound is widely used in research settings to explore therapeutic strategies aimed at enhancing dopaminergic signaling. -
COMT Inhibitor
Methylspinazarin is a potent inhibitor of catechol O-methyltransferase (COMT), exhibiting an IC50 of 0.8 μg/ml. Isolated from the actinobacterium Streptomyces, Methylspinazarin demonstrates selectivity for COMT compared to tyrosine hydroxylase. This compound is valuable for research applications focused on neurotransmitter metabolism and the pharmacological modulation of catecholamine pathways.
