Catalog No.
Product Name
Application
Product Information
Citations
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Parasite
Triazophos is a potent non-systemic insecticide and acaricide that functions as an acetylcholinesterase (AChE) inhibitor. By covalently and irreversibly binding to the acetylcholine binding site, Triazophos effectively disrupts the hydrolysis of acetylcholine, resulting in increased neuroexcitability. This compound demonstrates efficacy against a broad spectrum of soil insects and mites, including aphids, thrips, and spider mites, making it valuable for crop protection in various agricultural settings, such as ornamentals, cotton, rice, maize, soybeans, oil palms, olives, and coffee. -
Parasite Inhibitor
Phosalone is an organophosphate insecticide that primarily targets acetylcholinesterase, leading to the inhibition of neurotransmission in parasites. Its potent biological activity makes it effective in controlling a wide range of insect pests. Phosalone is utilized in entomological research and in studies focusing on pest management strategies and the biochemical pathways of insecticide resistance. -
nAChR Modulator
GSK575594A is an allosteric modulator of the nicotinic acetylcholine receptor (nAChR) in Ascaris suum. This compound enhances muscle contractions triggered by acetylcholine (ACh) by binding to the allosteric site within the transmembrane domain of the nAChR, leading to a significant increase in contraction amplitude (Emax from 1.19 g to 1.51 g) at a concentration of 3 μM. GSK575594A is applicable in antiparasitic research, providing insights into neuromuscular mechanisms in parasitic infections. -
ChE Inhibitor
Isogarcinol is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), exhibiting IC50 values of 1.13 μM and 8.30 μM, respectively. This compound also demonstrates significant leishmanicidal activity, with an IC50 of 0.33 μM against Leishmania donovani. Isogarcinol's dual action makes it a valuable tool for research in neurodegenerative disorders and parasitic diseases. -
Stable Isotope
Temephos-d12 is a deuterated form of Temephos, an organophosphate larvicide. It targets the central nervous system of aquatic larvae, including those of mosquitoes, midges, and black flies, by inhibiting cholinesterase activity. This mechanism leads to larval mortality prior to reaching the adult stage, making Temephos-d12 valuable for research on pesticide efficacy and environmental impact studies. -
CRMP2-NMDAR Inhibitor
TAT-CBD3 is a 15-amino acid peptide derived from CRMP2 that incorporates the TAT cell-penetrating motif from HIV-1, enabling efficient cellular uptake. This peptide disrupts the interaction between CRMP2 and NMDA receptors (NMDAR) while maintaining NMDAR localization. TAT-CBD3 is valuable for research applications focused on neurobiology and synaptic signaling, particularly in studies investigating the role of CRMP2 in neuronal function and related disorders. -
hDAT Modulator
SRI-32743 is an allosteric modulator of the human dopamine transporter (hDAT) with an IC50 value of 9.86 μM. This compound is of particular interest for research into HIV-Tat-induced neurotoxicity. Its modulation of hDAT may provide insights into the neurobiological mechanisms underlying dopamine dysregulation in various neurotoxic conditions. -
AChE Inhibitor
Temephos is an organophosphate insecticide that functions as an irreversible inhibitor of acetylcholinesterase (AChE). This inhibition leads to cholinergic overactivation, effectively disrupting the larval development of Aedes aegypti and Aedes albopictus, making it a valuable tool in research concerning Dengue Virus, Zika Virus, and other mosquito-borne pathogens. While exhibiting important biological activity, Temephos has been shown to cause genotoxicity, neurodevelopmental toxicity, and potential liver and reproductive system effects in mammals. Additionally, it can accumulate in adipose tissues and aquatic organisms, with its metabolism primarily occurring through oxidation and hydrolysis. Temephos serves as a critical reagent in studies of vector control and viral transmission dynamics. -
AAK1 Inhibitor
AAK1-IN-6 is a potent inhibitor of AP-2-associated protein kinase 1 (AAK1) with an IC50 value of 12 nM. This compound exhibits significant antiviral activity against dengue virus (DNEV2, EC50 = 0.24 μM) and Venezuelan equine encephalitis virus (VEEV, EC50 = 0.30 μM). AAK1-IN-6 is a valuable tool for researchers investigating antiviral mechanisms and potential therapeutic strategies. -
SMase Inhibitor
SMase-IN-1 is a specific inhibitor of bacterial sphingomyelinase (SMase), exhibiting an IC50 value of 6.43 µM against B. cereus SMase. In addition to its primary activity, SMase-IN-1 also demonstrates a significant inhibition rate of 59.50% for equine butyrylcholinesterase (eqBuChE) at a concentration of 50 µM. This compound forms a complex with Cu2+ in biometal interactions and effectively reduces hemolysis induced by B. cereus in sheep erythrocytes. SMase-IN-1 is valuable for research in microbial pathogenesis and enzyme inhibition studies. -
Stable Isotope
Itopride-d6 is a deuterated form of Itopride, a potent dopamine D2 receptor antagonist and acetylcholinesterase (AChE) inhibitor. Its unique stable isotope labeling allows for advanced metabolic and pharmacokinetic studies. Itopride enhances gastric motility through its combined antidopaminergic and anti-AChE actions, making it valuable in research applications focused on gastrointestinal prokinetics and conditions such as gastro-esophageal reflux disease (GERD). -
Babesicidal Agent
Quinuronium disulfate is a potent babesicidal agent with demonstrated anticholinesterase activity. It is primarily utilized in the study of protozoan infections, particularly those caused by Babesia species. This compound serves as a valuable tool in researching therapeutic interventions for babesiosis and related parasitic diseases. -
AChE/Dopamine 2 Inhibitor
Itopride is a potent dopamine D2 receptor antagonist and an acetylcholinesterase (AChE) inhibitor. Itopride enhances gastric motility through its dual mechanisms of action, promoting both antidopaminergic and anti-acetylcholinesterase effects. This compound is primarily utilized in research related to gastrointestinal disorders, particularly gastroesophageal reflux disease (GERD), offering insights into prokinetic therapies. -
Stable Isotope
(R)-3-O-Methyldopa-d3 is a deuterated form of the R-enantiomer of 3-O-Methyldopa, which acts as a metabolite of L-DOPA. The compound exerts its biological activity by competitively inhibiting catechol-O-methyltransferase (COMT), thus influencing the pharmacological effects of both L-DOPA and dopamine. This stable isotope is essential for research applications involving metabolic pathways and neurological studies. -
Anti-aggregation Agent
CLR01 sodium is an anti-aggregation agent that effectively penetrates the blood-brain barrier. It inhibits the de novo aggregation of key proteins, including Amyloid-β 40/42, α-synuclein, IAPP, tau protein, and SOD1. CLR01 sodium has demonstrated the ability to reduce amyloid plaque burden in the cortex of triple-transgenic mice, resulting in improvements in memory and motor functions. This compound is applicable in research focused on neurodegenerative disorders such as Alzheimer's disease, Parkinson's disease, and amyotrophic lateral sclerosis (ALS). -
P2Y1 receptor/[35S]GTPγS binding/β-arrestin 2 recruitment Agonist
MRS2365 is a highly potent and selective agonist of the P2Y1 receptor, exhibiting an EC50 of 0.4 nM for [35S]GTPγS binding and β-arrestin 2 recruitment. This compound effectively alleviates mechanical allodynia and enhances mechanical sensitivity, making it valuable for pain research. Notably, MRS2365 demonstrates minimal activity at P2Y12 and P2Y13 receptors, highlighting its specificity for P2Y1. -
BChE Inhibitor/CB2R Agonist
hBChE-IN-2 is a potent butyrylcholinesterase (BChE) inhibitor with an IC50 of 0.62 μM and functions as an agonist for cannabinoid receptor 2 (CB2R). This compound exhibits significant neuroprotective activities, making it a valuable tool in the study of neurodegenerative diseases and cannabinoid signaling pathways. Its dual action positions hBChE-IN-2 as an important reagent for research applications targeting cholinergic regulation and endocannabinoid modulation. -
Alkaloid
Aposcopolamine is an alkaloid isolated from Datura ferox, known for its ability to bind closely with acetylcholinesterase (ACHE), adrenergic receptor alpha-2A (ADRA2A), and muscarinic receptor subtype 2 (CHRM2). This compound is of significant interest in Alzheimer's disease research due to its potential effects on cholinergic signaling pathways. Aposcopolamine serves as a valuable tool in investigating neurodegenerative mechanisms and developing therapeutic strategies. -
M3 mAChR Antagonist
p-F-HHSiD hydrochloride is a potent and selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR). This compound also demonstrates antagonistic properties towards other mAChR subtypes and the alpha1-adrenoceptor. p-F-HHSiD hydrochloride is useful for research applications involving cancer, metabolic disorders, neurological conditions, and cardiovascular diseases, including colon cancer, Alzheimer’s disease, and diabetes. -
mAChR Antagonist
Batefenterol Succinate is an inhaled bifunctional bronchodilator that acts as a muscarinic acetylcholine receptor (mAChR) antagonist and a beta2-adrenoceptor agonist. This dual mechanism results in effective smooth muscle relaxation, enhancing respiratory function. Batefenterol Succinate is primarily utilized in research focused on chronic obstructive pulmonary disease (COPD) and other respiratory conditions, providing insights into therapeutic strategies for airway obstruction. -
mAChR/Adrenergic Receptor Antagonist
Muscarinic toxin 3 (MT3) is a selective and non-competitive antagonist of muscarinic acetylcholine receptors (mAChRs) and adrenergic receptors. It exhibits high potency with pIC50 values of 6.71, 8.79, 8.86, 7.57, 8.13, and 8.49 against M1, M4, α1A, α1B, α1D, α2A, α2B, and α2C receptors, respectively, highlighting its prominent adrenoceptor activity. This compound is valuable in studying receptor signaling pathways and has potential applications in pharmacological research focused on nervous system disorders and cardiovascular diseases. -
M3 mAChR Antagonist
p-F-HHSiD (p-Fluorohexahydrosiladifenidol) functions as a selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR). This compound exhibits antagonistic activity against various muscarinic receptor subtypes as well as the alpha-1 adrenergic receptor. p-F-HHSiD is valuable for research in cancer, metabolic disorders, neurological pathologies, and cardiovascular diseases, including colon cancer, Alzheimer's disease, and diabetes. -
P2Y14R Antagonist
MK-852 is a potent P2Y14 receptor antagonist that plays a crucial role in modulating platelet aggregation. This compound effectively inhibits the binding of fibrinogen to platelets in vitro, making it a valuable tool for studying thrombotic processes. Research applications include investigations into platelet function and the development of antithrombotic therapies. -
Topoisomerase I Inhibitor
RPR121056 is a topoisomerase I inhibitor that functions as a metabolite of the chemotherapy agent Irinotecan (CPT-11), produced by the enzyme CYP3A4. This compound induces cell death by disrupting DNA replication, making it relevant for cancer research, particularly in the context of colorectal cancer treatment. Additionally, RPR121056 demonstrates direct inhibition of acetylcholinesterase (AChE), further expanding its potential applications in pharmacological studies. -
Stable Isotope
RPR121056-d3 is a deuterated analog of RPR121056, a metabolite of the anticancer drug Irinotecan. It primarily targets and inhibits topoisomerase type I, leading to apoptosis in cancer cells. RPR121056-d3 is utilized in research applications focused on understanding the metabolic pathways and pharmacokinetics of Irinotecan, particularly in the context of colorectal cancer therapy. Additionally, it may also provide insights into the inhibition of acetylcholinesterase (AChE). -
Integrated Stress Response Pathway Modulator
Comtifator is an integrated stress response pathway modulator that influences cellular responses to various stressors. This compound is essential for studying the role of the integrated stress response in diseases such as neurodegeneration and cancer. Its ability to alter stress signaling makes it a valuable tool for research investigating therapeutic interventions and mechanisms underlying stress-related disorders. -
Tau-aggregation and Neuroinflammation Inhibitor
Tau-aggregation and neuroinflammation-IN-1 is an effective inhibitor of tau aggregation and neuroinflammation. This compound demonstrates significant inhibitory activity against both AcPHF6 and full-length tau aggregation, while exhibiting low cytotoxicity. Additionally, it reduces nitric oxide release in lipopolysaccharide-stimulated BV2 cells. Research applications include investigations into memory impairment, as Tau-aggregation and neuroinflammation-IN-1 has been shown to reverse okadaic acid-induced cognitive deficits in rat models. -
Tau Tracer
Tau Tracer 2 (PI-2620) is a selective imaging agent targeting Tau protein aggregates. It is designed for the visualization and diagnosis of neurodegenerative diseases, aiding in the assessment of Tau pathology. This reagent is valuable for researchers exploring Tau-related mechanisms and monitoring the progression of Tau-associated disorders. -
Tau Aggregation Inhibitor
3,3'-Diethyl-9-methylthiacarbocyanine iodide is a cyanine dye that functions as a tau aggregation inhibitor, exhibiting an IC50 value of 0.28 μM for tau proteins. It interferes with the proper functioning of the microtubule cytoskeleton, making it valuable for studies investigating tau pathologies. This compound is particularly relevant in Alzheimer's disease research, enabling the exploration of therapeutic strategies targeting tau aggregation. -
Tau Binding Drug
THK-5117 is an arylquinoline derivative that exhibits a strong binding affinity to tau fibrils, with a Ki of 10.5 nM. It shows remarkable specificity for tau protein aggregates, making it a valuable tool for studying tau pathology in Alzheimer's disease. Additionally, 18F-THK-5117 has potential applications in tau imaging as a PET probe, providing insights into tau-related neurodegenerative processes. -
Tau Tracer
Tau Tracer 1 is a selective imaging agent designed for the visualization of Tau protein aggregates, a hallmark of neurodegenerative diseases. This compound enables the detection and quantification of Tau pathology, facilitating the diagnosis and study of conditions such as Alzheimer's disease. Its application is crucial in both preclinical and clinical research settings, allowing for a better understanding of Tau-related pathologies. -
Tau441 Aggregation Inhibitor
Tau-aggregation-IN-1 is a potent inhibitor of tau441 protein aggregation, exhibiting an IC50 value of 21 µM. This compound also acts as an agonist for dopamine D2 and D3 receptors, making it relevant in studies of neurodegenerative diseases and tauopathies. Its dual mechanism offers potential for investigating tau-related pathologies and dopaminergic signaling in experimental research settings. -
Tau Imaging Probe
THK-5105 is an arylquinoline derivative that serves as a tau imaging probe, exhibiting high binding affinity for tau fibrils and protein aggregates. Its specific interaction with tau-rich Alzheimer disease brain homogenates makes it a valuable tool for studying tau pathology. The radiofluorinated derivative, 18F-THK-5105, is particularly promising for use as a positron emission tomography (PET) imaging probe in Alzheimer's research. -
Alkaloid
Circumdatin C is an alkaloid that demonstrates inhibitory effects on lipopolysaccharide (LPS)-stimulated nitric oxide production. Additionally, it inhibits acetylcholinesterase (AChE) activity with an IC50 value of 13.9 μM. This compound is valuable for research into neurodegenerative diseases, particularly Alzheimer's disease, by exploring mechanisms related to neurotransmitter regulation and neuroinflammation. -
Antioxidant Agent
4-Hydroxyisophthalic acid functions primarily as an antioxidant agent, activating crucial antioxidant enzymes such as catalase (CAT) and superoxide dismutase (SOD). Its ability to scavenge free radicals contributes to its protective effects on neuronal function, as it enhances the activity of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). In research applications, 4-Hydroxyisophthalic acid has demonstrated potential in improving cognitive defects and alleviating circadian rhythm disorders in model organisms, such as fruit flies. -
Stable Isotope
Imidazole-15N2 is a stable isotope-labeled derivative of imidazole, a heterocyclic aromatic compound. It serves as a valuable tool in metabolic studies and tracing experiments due to its nitrogen-15 labeling. Imidazole and its derivatives exhibit a wide range of biological activities, including inhibition of acetylcholinesterase and xanthine oxidase, as well as properties such as antifungal, antituberculosis, anti-inflammatory, and antioxidant effects. Additionally, imidazole derivatives have shown promise in the inhibition of SARS-CoV-2 3CLPro enzyme, highlighting their potential applications in research related to Alzheimer's disease, gout, COVID-19, and thromboembolic disorders. -
COX Inhibitor
SC57666 is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 value of 26 nM. This compound exhibits anti-inflammatory activity by specifically blocking COX-2, thereby reducing prostaglandin synthesis. SC57666 is valuable for research applications focused on understanding inflammation and pain mechanisms, as well as for screening in drug discovery efforts targeting COX-2 related conditions. -
COX Inhibitor
FR-188582 is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 value of 17 nM. This compound exhibits potent anti-inflammatory activity, making it a valuable tool for studies related to pain and inflammation pathways. Its specificity for COX-2 allows for the exploration of therapeutic applications in conditions such as arthritis and other inflammatory diseases. -
COX Inhibitor
Nitroflurbiprofen is a cyclooxygenase (COX) inhibitor known for its nitric oxide (NO)-donating properties. It effectively modulates increased intrahepatic vascular tone, making it a valuable tool in studying portal hypertension and liver diseases. This compound is utilized in research contexts focused on the therapeutic mechanisms of COX inhibition and its impact on hepatic vascular dynamics. -
COX Inhibitor
RWJ 63556 is an orally active inhibitor of cyclooxygenase-2 (COX-2) and a 5-lipoxygenase inhibitor, exhibiting significant anti-inflammatory properties. This compound is utilized in research to explore its potential therapeutic effects in conditions characterized by inflammation, such as arthritis and other inflammatory diseases. Its selective inhibition may provide insights into the role of COX-2 and lipoxygenase pathways in various biological processes. -
COX Inhibitor
COX-2-IN-6 is a selective cyclooxygenase-2 (COX-2) inhibitor, specifically designed for oral administration and exhibiting gut-restricted properties. With an IC50 value of 0.84 μM and a Ki of 69 nM, COX-2-IN-6 effectively targets COX-2, inhibiting COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM. This compound is utilized in research focused on colorectal cancer chemoprevention, offering valuable insights into inflammatory processes and therapeutic strategies. -
COX-2 Inhibitor
COX-2-IN-28 is a potent and selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 of 0.054 µM for COX-2, while demonstrating significantly lower inhibitory activity against 15-lipoxygenase (2.14 µM) and cyclooxygenase-1 (13.21 µM). This selective inhibition positions COX-2-IN-28 as a valuable tool for investigating the role of COX-2 in inflammation and pain pathways. It is suitable for research applications focused on inflammatory diseases and therapeutic development targeting COX-2 pathways. -
COX Inhibitor
Tolmetin sodium is a potent inhibitor of cyclooxygenase (COX), demonstrating IC50 values of 0.35 μM for human COX-1 and 0.82 μM for COX-2. As a non-steroidal anti-inflammatory drug (NSAID), it is primarily used for its analgesic and anti-inflammatory properties. Tolmetin sodium is valuable in research applications focused on pain management, inflammation, and associated disorders. -
COX-2 Inhibitor
SD 8381 is a potent and selective inhibitor of cyclooxygenase-2 (COX-2). It demonstrates an IC50 value of 0.0098 μM against human COX-2 and 0.69 μM against human COX-1, indicating a high degree of selectivity. This compound is valuable for research applications focused on inflammation and pain management, as well as studies examining the role of COX-2 in various disease states. -
COX2 Inhibitor
COX-2-IN-56 is a selective inhibitor of cyclooxygenase-2 (COX-2), demonstrating minimal inhibition of cyclooxygenase-1 (COX-1). This compound is valuable for investigating COX-2-dependent disorders, particularly in the context of inflammatory processes. Its specificity makes it suitable for research applications focused on understanding the role of COX-2 in various pathological conditions. -
COX Inhibitor
Benzoylgomisin O is a selective inhibitor of cyclooxygenase enzymes COX-1 and COX-2, as well as 15-lipoxygenase (15-LOX). This compound, isolated from Schisandra rubriflora, exhibits significant anti-inflammatory activity, making it a valuable reagent for research into inflammatory diseases and related pathways. Its ability to modulate lipid mediators positions it as a potential tool in the study of pathophysiological conditions where COX and LOX pathways are implicated. -
COX-1 inhibitor
COX-1-IN-1 is a selective inhibitor of cyclooxygenase-1 (COX-1) with an IC50 value of 0.23 μM, demonstrating a high degree of selectivity over COX-2 (IC50 > 50 μM), resulting in a selectivity index of 217. This compound effectively inhibits platelet aggregation, making it a useful tool in the study of inflammatory processes and cardiovascular research applications. COX-1-IN-1 can aid in understanding the role of COX-1 in various physiological and pathological conditions. -
COX-2 Inhibitor
Desmethyl etoricoxib is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 of 1 μM in whole blood, demonstrating significant potential in modulating inflammatory responses. It exhibits a lower affinity for COX-1, with an IC50 of 16 μM in U937 cells, highlighting its selectivity. This compound is valuable for research applications targeting inflammatory pathways and exploring therapeutic effects in various inflammatory conditions. -
COX1/2 Inhibitor
COX-1/2-IN-2 is a selective inhibitor of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), demonstrating potent activity with IC50 values of 9.7 ± 0.09 µM for COX-1 and 4.6 ± 1.45 µM for COX-2. This compound is useful in research applications involving inflammation and pain modulation, as it effectively reduces the synthesis of pro-inflammatory prostaglandins. Its utility in pharmacological studies makes it a valuable reagent for exploring COX-related pathways. -
COX-2 Inhibitor
Cassiatannin A is a proanthocyanidin tetramer that acts as a selective COX-2 inhibitor. It has demonstrated significant inhibition rates of 38%, 52%, and 97% at concentrations of 10, 100, and 1000 μg/mL, respectively. This compound is valuable for research into inflammatory processes and the molecular pathways associated with COX-2-mediated responses.
