Neuronal Signaling

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  1. Cholinesterase (ChE) Antagonist

    Pipenzolate bromide is a muscarinic receptor antagonist that functions by inhibiting cholinesterase (ChE) activity, thereby preventing the binding of acetylcholine to its receptors. This compound exhibits significant anticholinergic properties, making it valuable in pharmacological research related to disorders such as motion sickness, asthma, and gastrointestinal motility. Pipenzolate bromide serves as a useful reagent in studies aimed at understanding the modulation of cholinergic signaling pathways.
  2. hAChE Inhibitor

    7-Methoxytacrine is a potent inhibitor of human acetylcholinesterase (hAChE) with an IC50 value of 10 μM. This compound is utilized in research related to Alzheimer's disease, highlighting its potential role in modulating neurotransmitter levels and improving cognitive function. Its mechanism of action makes it a valuable tool for investigating therapeutic strategies in neurodegenerative disorders.
  3. Insecticide

    Demeton-S is an organophosphate insecticide that primarily targets butyrylcholinesterase and acetylcholinesterase enzymes. By inhibiting these enzymes, Demeton-S disrupts cholinergic neurotransmission, leading to paralysis and mortality in insects. This compound is utilized in agricultural research and pest management studies to evaluate insect resistance and to develop sustainable control strategies.
  4. ChE Activator

    HP 184 is an acetylcholine release stimulator, functioning as a cholinesterase (ChE) activator. This compound enhances synaptic transmission by promoting the release of acetylcholine, making it valuable for studies in neurobiology and neuromuscular disorders. Additionally, the compound's ADME properties can be modified by substituting hydrogen with deuterium, allowing for further exploration of its pharmacokinetics and pharmacodynamics in research applications.
  5. Microbial Metabolite

    Arisugacin E is a microbial metabolite with a structural similarity to Arisugacin A. This compound has been characterized for its unique biological properties but does not exhibit activity against acetylcholinesterase (AChE). Arisugacin E may serve as a useful tool for studying microbial metabolites and their role in biochemical pathways within various research applications.
  6. ChE Inhibitor

    Lycodine is a lycopodium alkaloid that acts as a cholinesterase inhibitor. It demonstrates significant anticholinesterase activity, making it a valuable tool for research into neurological disorders and cognitive function. Its potential applications extend to studying mechanisms of acetylcholine modulation and developing therapeutic approaches for conditions such as Alzheimer’s disease.
  7. AChE Inhibitor

    Graphislactone A is an acetylcholinesterase (AChE) inhibitor, which demonstrates significant potential in the investigation of neurodegenerative diseases. With an IC50 value of 27 μM, it effectively inhibits AChE activity, contributing to enhanced cholinergic signaling. Additionally, Graphislactone A exhibits antioxidant properties, making it a valuable compound for research focused on oxidative stress-related disorders.
  8. Cholinesterase (ChE) Inhibitor

    Echinenone acts as an acetylcholinesterase (AChE) inhibitor, exhibiting an IC50 value of 16.29 μg/mL. This compound demonstrates anti-Aβ(25-35) activity and has been shown to decrease malondialdehyde (MDA) levels while enhancing the activities of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GSH-Px). These properties indicate its potential use in research focused on neuroprotection and alleviating oxidative stress-related damage.
  9. Microbial Metabolite

    Arisugacin H is a microbial metabolite that functions as a structural analog of Arisugacin A. This compound exhibits notable biological activity, primarily contributing to the study of microbial interactions and metabolites. Although it has been characterized, it does not demonstrate inhibition of acetylcholinesterase (AChE), making it a useful tool for exploring alternative pathways in microbial research.
  10. AChE Inhibitor

    Isodimethoate is an acetylcholinesterase (AChE) inhibitor that demonstrates potent anticholinesterase activity. As a thermal decomposition product of Dimethoate, it effectively inhibits AChE in human red blood cells, making it valuable for studying cholinergic signaling and related neurochemical pathways. This compound is frequently utilized in research focused on neurotoxicology and the effects of organophosphates on enzymatic activity.
  11. Organophosphorus Insecticide

    Heterophos is an organophosphorus insecticide that functions as an acetylcholinesterase (AChE) inhibitor. By disrupting the normal breakdown of acetylcholine, Heterophos leads to the accumulation of this neurotransmitter, resulting in disturbances of nerve conduction in insects. This mechanism underpins its efficacy in pest control applications, particularly in the study of insect neurophysiology and insecticide resistance mechanisms.
  12. Natural Product

    Dihydrokaempferol-3-O-β-D-glucoside is a natural product that acts as an inhibitor of acetylcholinesterase (AChE). Isolated from the bark of Cudrania tricuspidata, this compound demonstrates potential biological activity in modulating cholinergic signaling. Its research applications include studies on neurodegenerative diseases and exploration of cognitive enhancement mechanisms.
  13. AChE Inhibitor

    Galactamine is an acetylcholinesterase (AChE) inhibitor that plays a crucial role in modulating neurotransmitter levels by preventing the breakdown of acetylcholine. This compound is primarily utilized in research investigating Alzheimer's disease and other neurodegenerative disorders, where it helps to elucidate the mechanisms underlying cognitive decline and potential therapeutic strategies. Galactamine's ability to enhance cholinergic signaling makes it a valuable tool in the study of efficacy and safety in neuropharmacology.
  14. hBuChE Inhibitor

    Deoxynojirimycin tetrabenzyl ether is an inhibitor of human butyrylcholinesterase (hBuChE), with an IC50 value of 2.0 μM. This compound is utilized in research focused on neurological disorders and cholinergic system regulation, making it valuable for studies involving enzyme inhibition and potential therapeutic applications in cognitive decline.
  15. Stable Isotope

    Acephate-d6 is a deuterium-labeled derivative of Acephate, a widely used anticholinesterase insecticide. It functions by inhibiting acetylcholinesterase (AChE) activity in insects, leading to disruption of their nervous system and effective pest control. This stable isotope variant is useful for research applications involving metabolic studies, pesticide residue analysis, and environmental monitoring in agricultural and horticultural settings.
  16. Microbial Metabolite

    Arisugacin F is a microbial metabolite that serves as a structural analog of Arisugacin A. This compound is primarily investigated for its role in various biological pathways, although it has been reported to exhibit no activity against acetylcholinesterase (AChE). Arisugacin F may be utilized in research exploring microbial metabolism and the structural influences of similar compounds on biological systems.
  17. Insecticide

    Quintiofos is an insecticide that functions by inhibiting the enzyme acetylcholinesterase in insects, leading to disruptions in nerve conduction. This mechanism results in effective insecticidal activity against a variety of pests, including aphids, whiteflies, and stem borers. Quintiofos is a valuable tool for researchers studying insect physiology and pest management strategies.
  18. AChE Inhibitor

    Arisugacin C is an acetylcholinesterase (AChE) inhibitor exhibiting an IC50 of 2.5 μM, demonstrating its potent activity in modulating cholinergic neurotransmission. This compound is valuable for research into neurodegenerative diseases, including Alzheimer’s disease, where AChE inhibition may alleviate cognitive decline. Its selectivity and efficacy make it a useful tool in studying the mechanisms of cholinergic signaling and developing potential therapeutic strategies.
  19. Monoamine Oxidase Inhibitor

    4-Chlorochalcone is a selective monoamine oxidase inhibitor, demonstrating an IC50 of 0.082 μM against hMAO-B and 9.95 μM against hMAO-A. This compound also shows inhibitory activity towards acetylcholinesterase, with an IC50 of 2.79 μM. As a chalcone derivative, 4-Chlorochalcone is valuable for research focused on neurodegenerative diseases and the modulation of neurotransmitter levels.
  20. Cholinesterase (ChE) Inhibitor

    AChE-IN-83 is a potent acetylcholinesterase (AChE) inhibitor targeting cholinesterases in various biological systems. This compound effectively inhibits the growth and behavior of Aphelenchoides oryzae, a nematode pathogen in rice, demonstrating an LC50 value of 19.0 μg/mL over 48 hours. AChE-IN-83 disrupts the nematode cuticle, promoting the accumulation of reactive oxygen species, lipofuscin, and lipids, thereby offering applications in nematode management and enhancing rice seed health.
  21. ChE Inhibtior

    (S)-Ladostigil is a cholinesterase (ChE) inhibitor known for its neuroprotective properties. While it exhibits limited inhibition of monoamine oxidase B (MAO-B), its primary mechanism enhances cholinergic neurotransmission, making it of interest in the study of neurodegenerative disorders. This compound is utilized in research focusing on Alzheimer's disease and other conditions where cholinergic dysfunction is implicated.
  22. Cholinesterase Inhibitor

    Mobam is a cholinesterase inhibitor with significant efficacy against Anoplura Pediculidae. This compound effectively reduces cholinesterase (ChE) levels in plasma, erythrocytes, and brain tissue of rat models, leading to suppressed avoidance behavior. Mobam is primarily utilized in toxicological research and studies focused on neurological effects and insecticidal applications.
  23. Stable Isotope

    Donepezil-d7 is a deuterium-labeled analog of Donepezil, a selective and potent inhibitor of acetylcholinesterase (AChE). This compound demonstrates impressive inhibitory activity with IC50 values of 8.12 nM for bovine AChE and 11.6 nM for human AChE, making it a valuable tool for studying cholinergic signaling and Alzheimer's disease. Researchers can utilize Donepezil-d7 in pharmacokinetic studies and metabolic profiling to better understand the compound's activity and metabolism in various biological contexts.
  24. Cholinesterase (ChE) Inhibitor

    SZ1676 is a cholinesterase (ChE) inhibitor that functions primarily by blocking the enzymatic activity of acetylcholinesterase. This compound demonstrates significant potential in studying neuromuscular transmission and related disorders. Its biological activity may support research in pharmacology and toxicology, particularly concerning neuromuscular blocking agents and their therapeutic implications.
  25. Glucosylceramide Synthase Inhibitor

    Glucosylceramide synthase-IN-6 is a selective inhibitor of glucosylceramide synthase (GCS), targeting the enzymatic pathway involved in the synthesis of glucosylceramide. This compound is valuable for investigating the role of GCS in various diseases, particularly lysosomal storage disorders. Its application in research facilitates a better understanding of GCS activity and its implications in cellular metabolism and pathology.
  26. Glucosylceramide Synthase Inhibitor

    Glucosylceramide synthase-IN-5 is a potent inhibitor of glucosylceramide synthase (GCS). This compound is instrumental in the exploration of diseases and disorders linked to GCS activity, particularly lysosomal storage disorders. Its ability to modulate GCS activity makes it a valuable tool in biochemical research aimed at understanding sphingolipid metabolism and related pathologies.
  27. Glucosylceramide Synthase Inhibitor

    Lucerastat is a potent inhibitor of glucosylceramide synthase (GCS), specifically in its galactose form derived from Miglustat. This compound exhibits significant biological activity in modulating glycosphingolipid metabolism and has potential applications in the investigation of Fabry disease. Researchers may employ Lucerastat to explore therapeutic avenues and understand the pathophysiology associated with GCS-related disorders.
  28. Glucosylceramide Synthase Inhibitor

    Ibiglustat (L-Malic acid) is a potent inhibitor of glucosylceramide synthase (GCS), demonstrating oral bioavailability and the ability to penetrate the blood-brain barrier. This compound is instrumental for research into various lysosomal storage disorders, including Gaucher disease type 3, Parkinson's disease linked to GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease. Its selective inhibition of GCS makes it a valuable tool for studying the biochemical pathways associated with these conditions.
  29. Glucosylceramide Synthase Inhibitor

    Ibiglustat succinate is a potent glucosylceramide synthase (GCS) inhibitor with oral bioavailability and the ability to penetrate the blood-brain barrier. This compound is primarily used in research focused on Gaucher disease type 3, Parkinson's disease linked to GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease. Its inhibitory action on GCS has potential implications for understanding and treating these neurodegenerative and lysosomal storage disorders.
  30. Glucosylceramide Synthase Inhibitor

    Ibiglustat hydrochloride is a potent glucosylceramide synthase (GCS) inhibitor that effectively penetrates the blood-brain barrier. This compound is primarily used in research related to Gaucher disease type 3, Parkinson's disease linked to GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease. Its mechanism of action contributes to the modulation of glucocerebroside metabolism, offering a valuable tool for studies focused on lysosomal storage disorders and related neurodegenerative conditions.
  31. Glucosylceramide Synthase Inhibitor

    (−)-L-threo-PDMP hydrochloride is a potent inhibitor of glucosylceramide synthase (GCS). This compound has been shown to promote the proliferation of cultured aortic smooth muscle cells and elevate levels of lactosylceramide (LacCer) in B16 melanoma cells. Its unique activity profile makes it a valuable tool for research applications related to glycosphingolipid metabolism and cellular signaling pathways.
  32. AAK1 Inhibitor

    BMS-986176 is a potent and selective inhibitor of adaptor associated kinase 1 (AAK1) with an IC50 value of 2 nM. This compound is designed for effective brain penetration, making it a valuable tool in the investigation of neurodegenerative diseases. It is applicable in research focused on the modulation of AAK1 pathways and their implications in various neurological disorders.
  33. AAK1 Inhibitor

    AAK1-IN-12 is a selective inhibitor of the AP2-associated kinase 1 (AAK1) that demonstrates oral bioavailability and the ability to cross the blood-brain barrier. This compound has important implications for research into neurodegenerative disorders, including schizophrenia, Parkinson's disease, neuropathic pain, and Alzheimer's disease. AAK1-IN-12 serves as a valuable tool for investigating the therapeutic potential of AAK1 modulation in various neurological contexts.
  34. AAK1 Inhibitor

    LP-922761 is a selective inhibitor of adapter protein-2 associated kinase 1 (AAK1), demonstrating potent activity with IC50 values of 4.8 nM in enzyme assays and 7.6 nM in cellular assays. Additionally, LP-922761 inhibits BMP-2-inducible protein kinase (BIKE) at an IC50 of 24 nM. Importantly, it shows no significant activity against cyclin G-associated kinase (GAK), opioid receptors, adrenergic α2 receptors, or GABAa receptors, making it a valuable tool for studying AAK1-related signaling pathways and its role in cellular processes.
  35. AAK1

    BMS-911172 is an inhibitor of adaptor-associated kinase 1 (AAK1), exhibiting an IC50 value of 35 nM. This compound is primarily used in research focused on modulating clathrin-mediated endocytosis and exploring the role of AAK1 in cellular processes. Its ability to selectively inhibit AAK1 makes it a valuable tool for investigating signaling pathways related to receptor internalization and trafficking.
  36. AAK1 Inhibitor

    BMT-124110 is a highly selective inhibitor of AAK1 (AP2-associated protein kinase 1) with an IC50 value of 0.9 nM. This compound exhibits notable antinociceptive activity, making it relevant in pain management research. Additionally, BMT-124110 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 17 nM and 99 nM, respectively, further supporting its utility in kinase-related studies.
  37. AAK1 Inhibitor

    SGC-AAK1-1N is a selective inhibitor of AAK1 (AP2 associated kinase 1) with an IC50 value of 1.8 μM. This compound is utilized in research to elucidate the role of AAK1 in cellular processes, particularly in clathrin-mediated endocytosis and signaling pathways. Its potency makes it a valuable tool in studies focused on understanding the therapeutic potential of AAK1 modulation in various diseases.
  38. AAK1 Inhibitor

    BMS-901715 is a highly selective inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC50 of 3.3 nM. This compound disrupts clathrin-mediated endocytosis, making it valuable for studying cellular processes related to membrane trafficking. BMS-901715 is particularly useful in research applications focused on viral infections and the modulation of synaptic transmission.
  39. AAK1 Inhibitor

    AAK1-IN-2 TFA is a selective and potent inhibitor of Adaptor Protein 2-Associated Kinase 1 (AAK1), demonstrating an IC50 value of 5.8 nM. This compound effectively penetrates the blood-brain barrier, making it a valuable tool for research in neuropathic pain mechanisms. AAK1-IN-2 TFA enables the investigation of AAK1's role in various neurological conditions, providing insights into potential therapeutic targets for pain management.
  40. AAK1 Inhibitor

    AAK1-IN-3 is a potent inhibitor of adaptor protein 2-associated kinase 1 (AAK1), exhibiting an IC50 of 11 nM. This quinoline analogue effectively penetrates the blood-brain barrier, making it suitable for investigating the role of AAK1 in neuropathic pain mechanisms. AAK1-IN-3 is a valuable tool for research focused on neuropharmacology and the modulation of pain pathways.
  41. AAK1 Inhibitor

    AAK1-IN-4 is a selective inhibitor of adaptor protein-2-associated kinase 1 (AAK1), demonstrating an IC50 of 4.6 nM. This orally active compound effectively penetrates the central nervous system, with a filtration Ki of 0.9 nM and a cell IC50 of 8.6 nM. AAK1-IN-4 is primarily utilized in research studies focused on neuropathic pain, offering insights into its underlying mechanisms and potential therapeutic applications.
  42. AAK1 Inhibitor

    AAK1-IN-3 TFA is a quinoline derivative that selectively inhibits adaptor protein 2-associated kinase 1 (AAK1) with an IC50 of 11 nM. This compound demonstrates significant brain penetration and is suitable for investigating neuropathic pain mechanisms. Its ability to modulate AAK1 activity makes it a valuable tool for research applications focused on pain pathways and related neurobiological processes.
  43. AAK1 Inhibitor

    HW161023 is a potent inhibitor of AP2-associated protein kinase 1 (AAK1), demonstrating an IC50 of 5.4 nM against AAK1 and a much higher IC50 of 11.9 μM against hERG. This compound has shown efficacy in alleviating pain in a chronic constriction injury model of the sciatic nerve in rats. HW161023 is valuable for research in pain mechanisms and the modulation of AAK1-related signaling pathways.
  44. AAK1 Inhibitor

    AAK1-IN-10 is a selective inhibitor of adapter-associated kinase 1 (AAK1), exhibiting potent enzyme inhibitory activity with an IC50 of 9.62 nM. This compound primarily functions by impairing the activity of AAK1, a kinase involved in various cellular processes. AAK1-IN-10 demonstrates low cardiotoxicity, with an IC50 of 13.7 μM, making it a suitable candidate for research into conditions such as diabetic neuropathy and postherpetic pain. Its distinct mechanism and safety profile facilitate investigations into therapeutic applications targeting nerve pain and associated disorders.
  45. AAK1 Inhibitor

    AAK1-IN-2 is a selective inhibitor of Adaptor Protein 2-Associated Kinase 1 (AAK1), exhibiting an IC50 of 5.8 nM. This compound demonstrates the ability to penetrate the blood-brain barrier, making it suitable for neurological research. AAK1-IN-2 is particularly relevant for studies investigating the mechanisms underlying neuropathic pain.
  46. AAK1 Inhibitor

    AAK1-IN-5 is a selective inhibitor of adaptor protein-2-associated kinase 1 (AAK1), demonstrating an IC50 of 1.2 nM and a filtrate Ki of 0.05 nM, along with a cell-based IC50 of 0.5 nM. This compound is notable for its ability to penetrate the central nervous system and is orally active, making it suitable for in vivo studies. AAK1-IN-5 is primarily used in research focused on neuropathic pain, providing a valuable tool for understanding AAK1's role in pain pathways.
  47. PROTAC

    PROTAC AAK1 Degrader-1 is a potent PROTAC designed to selectively degrade the AAK1 protein, a known modulator of clathrin-mediated endocytosis. This compound facilitates targeted protein degradation, thereby influencing cellular pathways critical in cancer research. Its application is valuable for studying the role of AAK1 in tumor biology and therapeutic resistance, potentially leading to innovative cancer treatment strategies.

  48. AAK1 Inhibitor

    BMT-046091 is a selective inhibitor of adaptor-associated kinase 1 (AAK1), targeting its activity to modulate cellular processes. This compound effectively inhibits the phosphorylation of the μ2 peptide by AAK1, demonstrating an IC50 value of 2.8 nM. BMT-046091 is useful in research applications studying AAK1's role in endocytic trafficking and signaling pathways, contributing to a better understanding of its implications in various diseases.
  49. Aβ1-42 Aggregation Inhibitor

    Aβ1–42 aggregation inhibitor 1 is a potent inhibitor of Aβ1-42 aggregation, targeting its self-mediated aggregation pathway. This compound effectively inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) with IC50 values of 2.64 μM and 1.29 μM, respectively. At a concentration of 25 μM, it reduces Aβ1-42 aggregation by 51.29%. Aβ1–42 aggregation inhibitor 1 is suitable for research applications focused on the mechanisms of Alzheimer's disease and potential therapeutic interventions.
  50. AChE Inhibitor

    Phenserine is a potent, noncompetitive inhibitor of acetylcholinesterase (AChE), derived from Physostigmine. It selectively targets AChE and has been shown to reduce the formation of β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ). This compound is primarily utilized in research related to cognitive function and the progression of Alzheimer's disease, demonstrating potential therapeutic benefits in enhancing cognitive performance.

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