Catalog No.
Product Name
Application
Product Information
Citations
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α7 nAChR Antagonist
nAChR antagonist 3 is a selective antagonist of the α7 nicotinic acetylcholine receptor, demonstrating an IC50 of 0.86 μM. It exhibits protective effects against toxicity induced by paraoxon, making it a valuable tool for studying organophosphate poisoning. This compound is suitable for research applications focusing on neuroprotection and receptor modulation associated with cholinergic signaling pathways. -
Stable Isotope
Varenicline-d4 is a deuterium-labeled derivative of Varenicline, a potent partial agonist of the α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Additionally, Varenicline acts as a full agonist at the α3β4 and α7 nAChRs, exhibiting EC50 values of 55 μM and 18 μM, respectively. This stable isotope is instrumental for research involving smoking cessation therapies and the pharmacological investigation of nicotinic receptors. -
nAChR Inhibitor
nAChR-IN-1 hydrochloride is a selective nicotinic acetylcholine receptor (nAChR) inhibitor that specifically targets nAChRs lacking the α5, α6, or β3 subunits. This compound is particularly useful in studying the roles of nAChRs in neurological disorders and offers potential insights into therapeutic strategies for conditions involving nicotinic acetylcholine receptor dysfunction. Its effectiveness in modulating nAChR activity makes it a valuable tool for chemical biology and pharmacological research. -
nAChR Agonist
Rivanicline fumarate is a selective agonist of neuronal nicotinic acetylcholine receptors (nAChRs), primarily targeting the α4β2 subtype with a Ki of 26 nM and an EC50 of 16 μM. This compound has demonstrated the ability to significantly restore learning impairments and alleviate cognitive dysfunctions. Rivanicline fumarate is valuable in research focused on neurodegenerative diseases, including schizophrenia and Alzheimer's disease, providing insights into potential therapeutic approaches. -
nAChR Antagonist
(rel)-Asperparaline A is a potent antagonist of nicotinic acetylcholine receptors (nAChR), extracted from okara fermented with Aspergillus japonicas JV-23. This compound displays significant paralytic activity in silkworms, highlighting its potential as an anthelmintic agent. Its selectivity and effectiveness make it valuable for research applications focused on neurotransmission and parasitic control. -
nAChR Inhibitor
Lupanine hydrochloride is a natural ketonic derivative of Sparteine, functioning as a nicotinic acetylcholine receptor (nAChR) inhibitor. It demonstrates binding affinity for the nAChR with a Ki value of 500 nM, indicating its potential role in modulating cholinergic signaling. This compound is suitable for research applications related to neuromuscular transmission and ganglioplegic activity. -
nAChR Agonist
Spinosyn L is a selective agonist of nicotinic acetylcholine receptors (nAChR). It induces sustained neural excitation and paralysis in insects, demonstrating effective activity against various agricultural pests, including Lepidoptera and Diptera. This compound is valuable for research applications focused on developing novel pesticides and understanding insect physiology. -
Insecticide Agent
nAChR modulator-2 is an orthosteric modulator of insect nicotinic acetylcholine receptors (nAChRs). This compound functions as an effective insecticide by influencing neurotransmission in target insects, leading to neurotoxic effects. It is particularly useful in research applications aimed at understanding insect physiology and the development of novel pest control strategies. -
nAChR Inhibitor
Xanthoplanine is an nAChR inhibitor derived from the root of Xylopia parviflora. It effectively inhibits the EC50 acetylcholine responses of both alpha7 and alpha4beta2 nicotinic acetylcholine receptors, demonstrating estimated IC50 values of 9 μM for alpha7 and 5 μM for alpha4beta2. Its potent inhibitory activity makes it a valuable tool for studying cholinergic signaling and related neurological pathways in research applications. -
α7 nAChR Agonist
Bradanicline tosylate is a selective agonist for the α7 nicotinic acetylcholine receptor (nAChR) with significant oral bioavailability and moderate blood-brain barrier penetration. It demonstrates high affinity and subtype specificity for human α7 nAChR, exerting antitussive effects through prolonged receptor activation. Bradanicline tosylate effectively inhibits cough responses induced by citric acid, bradykinin, and inhaled nicotine in a dose-dependent manner. This compound is well tolerated in preclinical studies, making it a valuable tool in research focused on chronic refractory cough and related therapeutic areas. -
Insecticide Agent
nAChR modulator-1 is an orthosteric modulator of insect nicotinic acetylcholine receptors (nAChR), functioning as a targeted insecticide agent. This compound demonstrates significant biological activity by disrupting neurotransmission in insects, leading to paralysis and death. It is widely utilized in research applications for studying pest control mechanisms and developing novel insecticide strategies. -
NF-κB Inhibitor
(R)-(+)-Anatabine is an NF-κB inhibitor that acts to lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). As the less active R-enantiomer of Anatabine, it retains the ability to modulate α4β2 nAChR activity. This compound exhibits anti-inflammatory properties and is being investigated for its potential applications in the treatment of neurodegenerative disorders. -
nAChR Agonist
SIB-1508Y is an orally active and selective agonist of the nicotinic acetylcholine receptor (nAChR). It holds potential for research applications related to parkinsonism and neurodegenerative disorders. Additionally, SIB-1508Y features an alkyne group, enabling its use as a click chemistry reagent for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
α7 nAChR Agonist
Nelonicline citrate is a selective agonist of the α7 nicotinic acetylcholine receptor (nAChR) with high affinity, as demonstrated by a Ki value of 12.3 nM in human brain tissue. This compound is primarily utilized in research investigating schizophrenia and Alzheimer's disease, providing insights into the modulation of cognitive processes and synaptic plasticity associated with these neurological disorders. Its oral bioavailability makes it a valuable tool for in vivo studies. -
nAChR Agonists
SIB 1663 is a conformationally restricted analog of nicotine that selectively activates α2β4 and α4β4 human recombinant neuronal nicotinic acetylcholine receptors (nAChRs). This compound has been shown to enhance the release of dopamine (DA) and norepinephrine (NE), making it a valuable tool in the study of neurotransmitter dynamics. SIB 1663 is applicable in neurological disease research, providing insights into the mechanisms underlying various neuropharmacological conditions. -
α7nACh Agonist
Epibatidine is an α7 nicotinic acetylcholine receptor (nAChR) agonist with a Kd of 100 nM. This compound is a valuable tool for investigating neurodegenerative diseases such as Alzheimer's and Parkinson's, as well as psychiatric conditions like schizophrenia. By activating the α7nACh receptors, Epibatidine can provide insights into cholinergic signaling and its implications in these disorders. -
α7 nAChR Agonist
WYE-103914 is a selective agonist of the α7 nicotinic acetylcholine receptor (nAChR), exhibiting EC50 values of 0.49 µM for rat and 0.57 µM for human receptors. This compound is known to enhance cognitive functions and memory in various experimental models. It is also utilized in research focusing on schizophrenia and can be administered alongside antipsychotic therapies to investigate potential synergistic effects. -
α7 nAChR Activator
IND8 is an activator of the α7 nicotinic acetylcholine receptor (nAChR), known for its cognitive enhancement properties. This compound has demonstrated efficacy in improving spatial working memory, episodic short-term memory, and spatial long-term memory in amnesic mice induced by Scopolamine. IND8 is particularly relevant for research on Alzheimer's disease and can be utilized in studies investigating interventions for cognitive decline. -
Antidepressant Agent
Cypenamine hydrochloride is an antidepressant agent that selectively interacts with human nicotinic acetylcholine receptors (nAchR) subtypes, specifically α2β4, α3β4, and α4β4, exhibiting Ki values of 4.65 μM, 2.69 μM, and 4.11 μM, respectively. This compound is commonly used in research to investigate its potential therapeutic effects in mood disorders and the underlying mechanisms of action related to neurotransmitter regulation. -
α7 nAChR PAMs
GAT107 is a potent positive allosteric modulator (PAM) of the α7 nicotinic acetylcholine receptor (nAChR). It enhances receptor activity, making it useful for research into neuropharmacology and potential treatments for cognitive disorders. Its mechanism allows for modulation of cholinergic signaling, which is crucial in areas such as memory and learning. GAT107 can aid in elucidating the functional properties of α7 nAChR in various biological contexts. -
α7 nAChR Agonist
Bradanicline hydrochloride is a selective agonist for the α7 nicotinic acetylcholine receptor (nAChR), exhibiting an EC50 of 17 nM and a Ki of 1.4 nM for the human α7 nAChR. This compound demonstrates significant biological activity that supports research into cognitive disorders and schizophrenia. Its targeted mechanism makes it a valuable tool for studying therapeutic approaches in neuropsychiatric conditions. -
nAChR Antagonist
SR 16584 is a selective antagonist of the α3β4 nicotinic acetylcholine receptor (nAChR), exhibiting an IC50 value of 10.2 μM. This compound is utilized in research investigating the role of nAChRs in neurological disorders and potential therapeutic applications. Its specific inhibition of α3β4 nAChR makes it valuable for studying the receptor's involvement in neurotransmission and related signaling pathways. -
nAChRs Agonist
SIB-1553A free base is an orally bioavailable agonist of nicotinic acetylcholine receptors (nAChRs), exhibiting selective activity towards receptors containing the β4 subunit. This compound serves as a selective ligand for neuronal nAChRs and demonstrates significant cognitive-enhancing properties. SIB-1553A free base shows therapeutic potential for addressing symptoms associated with Alzheimer's disease and other cognitive disorders in research applications. -
α7 nAChR Partial Agonist
AZD0328 is a selective partial agonist of the α7 nicotinic acetylcholine receptor (nAChR). It is known to enhance midbrain dopaminergic neuronal activity and increase cortical dopamine levels, contributing to improved cognitive performance. This compound is primarily used in research related to cognitive disorders and neurological modeling. -
α7 nACh Receptor Partial Agonist
BMS-933043 is a selective partial agonist of the α7 nicotinic acetylcholine receptor (nAChR). This compound has been shown to mitigate cognitive impairment in murine models, making it a valuable tool for research focused on cognitive dysfunction, particularly in the context of schizophrenia. Its unique mechanism facilitates the exploration of neuropsychological pathways and potential therapeutic interventions. -
α7 nAChR Agonist
CP-810123 is a brain-permeable agonist of the α7 nicotinic acetylcholine receptor (nAChR). It demonstrates significant potential in enhancing cognitive function and is valuable for investigating cognitive impairments associated with psychiatric and neurological disorders, including schizophrenia and Alzheimer's disease. This compound serves as an important tool for researchers exploring therapeutic strategies aimed at modulating cholinergic systems in the context of cognitive deficits. -
α4β2 Agonist
RJR-2429 is a potent agonist of the α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 59 nM and a binding affinity (Ki) of 1 nM. This compound is known to induce contraction in the ileum, making it relevant for studies examining gastrointestinal motility and nAChR-mediated signaling pathways. RJR-2429 serves as a valuable tool in pharmacological research focused on neuropharmacology and cholinergic function. -
nAChR Agonist
1,1-Dimethyl-4-acetylpiperazinium iodide is a potent agonist of nicotinic acetylcholine receptors (nAChRs), facilitating the opening of ion channels and leading to cell membrane depolarization. This compound is instrumental in studying synaptic transmission and has applications in neuropharmacology and neuromuscular research, providing insights into cholinergic signaling pathways and potential therapeutic interventions for related disorders. -
nAChR Ligand
Hepzidine is a novel ligand for nicotinic acetylcholine receptors (nAChRs). It demonstrates binding affinity for acetylcholine binding protein (AChBP), making it a valuable tool in the study of cholinergic signaling. This compound is particularly relevant for neurobiological research, providing insights into the roles of nAChRs in various neurological conditions and processes. -
Stable Isotope
Mecamylamine-d3 hydrochloride is a deuterium-labeled derivative of Mecamylamine hydrochloride, functioning as a nonselective, noncompetitive antagonist of nicotinic acetylcholine receptors (nAChR). This stable isotope is employed in research applications focused on neuropsychiatric disorders and the pharmacological assessment of nAChR activity. Its ability to cross the blood-brain barrier facilitates investigations into central nervous system functions and disorders, as well as potential therapeutic interventions. -
nAChR Modulator
Bensultap is a nicotinic acetylcholine receptor (nAChR) modulator known for its insecticidal properties against the Colorado beetle and other insect pests. This compound exhibits mild and temporary neuromodulatory effects on the rat nervous system, making it relevant for research into nAChR function and insect neurobiology. Its applications extend to studies in pest management and the exploration of neural signaling pathways impacted by nAChR modulation. -
Alkaloid
(±)-Coniine is a piperidine alkaloid known for its function as an nAChR agonist, demonstrating an EC50 of 0.3 mM. This compound exhibits acute toxicity in murine models, with an LD50 value of 7.7 mg/kg. Its unique properties make it valuable for research applications focused on neuromuscular transmission and toxicity studies. -
nAChR Agonist
Hydroxy Varenicline is a metabolite of varenicline, functioning as a nicotinic acetylcholine receptor (nAChR) agonist. This compound exhibits key biological activity by modulating nAChR signaling, making it relevant for research on nicotine addiction and its neuropharmacological effects. Hydroxy Varenicline serves as a valuable tool in studies aimed at understanding receptor dynamics and developing therapeutic strategies for smoking cessation and related disorders. -
α4β2 nAChR Partial Agonist
3-Pyr-Cytisine is a cytisine derivative that functions as a partial agonist of the α4β2 nicotinic acetylcholine receptor (nAChR). This compound exhibits weak agonistic properties, making it of interest in antidepressant research. Its modulation of α4β2 nAChR may provide insights into therapeutic strategies for mood disorders and further understanding of cholinergic signaling pathways. -
nAChR Agonist
Sofinicline benzenesulfonate is a potent agonist of the nicotinic acetylcholine receptor, specifically targeting the α4β2 subtype with an IC50 of 0.1 nM. This compound has demonstrated potential to enhance cognitive functions, including attention and memory, making it a valuable tool in the investigation of cognitive impairments. Its applications extend to research on attention deficit hyperactivity disorder (ADHD) and other cognitive disorders. -
nAChR Antagonist
Microgrewiapine A is a selective antagonist of nicotinic acetylcholine receptors (nAChR), specifically inhibiting human α4β2 and α3β4 subtypes with 60% and 70% efficacy, respectively. This compound demonstrates cytotoxic effects in HT-29 human colon cancer cells, exhibiting an IC50 value of 6.8 μM. Microgrewiapine A holds potential for research applications in cancer biology and neuropharmacology. -
AChE/nAChR Inhibitor
AChE/nAChR-IN-1 is a dual inhibitor targeting acetylcholinesterase (AChE) and nicotinic acetylcholine receptors (nAChR). This compound exhibits potent toxicity and larvicidal activity against Culex pipiens larvae, with an LC50 of 4 ng/mL. AChE/nAChR-IN-1 is utilized in research focused on controlling mosquito populations and studying mosquito-borne diseases. -
Stable Isotope
Varenicline-13C,15N is a stable isotope-labeled variant of Varenicline, a partial agonist of the α4β2 nicotinic acetylcholine receptor (nAChR), with an IC50 of 250 nM. This compound also interacts with α6β2 nAChR as a partial agonist and activates α7β2 nAChR as a full agonist. Varenicline-13C,15N is utilized in research to study nicotine dependence and the pharmacodynamics of smoking cessation therapies, providing valuable insights into receptor interactions and metabolic pathways. -
nAChR Antagonist
Dexmecamylamine is a selective antagonist of the nicotinic acetylcholine receptors (nAChR), specifically targeting the α3β4, α4β2, α7, and α1β1γδ subtypes with IC50 values in the micromolar range. This compound demonstrates notable anxiolytic and antidepressant-like effects, making it a valuable tool in neurological research and the study of mood disorders. Its ability to modulate nAChR activity positions it as a potential lead for therapeutic development in psychiatric conditions. -
nAChR Agonist
TC-2216 is an agonist of the α4β2 neuronal nicotinic acetylcholine receptors (nAChRs). This compound demonstrates significant antidepressant and anxiolytic properties, validated by multiple animal models. TC-2216's modulation of nAChR activity represents its potential utility in neuropharmacological research and the development of therapeutic strategies for mood disorders. -
AChE Inhibitor
Sinapine is an acetylcholinesterase (AChE) inhibitor derived from cruciferous seeds. This compound demonstrates a range of biological activities, including anti-inflammatory, antioxidant, anti-tumor, anti-angiogenic, and radio-protective effects. Sinapine is instrumental in research targeting neurodegenerative disorders such as Alzheimer's disease, myasthenia gravis, ataxia, and Parkinson’s disease, making it a valuable tool for advancing scientific understanding in these areas. -
Calmodulin Inhibitor
Zaldaride is a selective calmodulin inhibitor that effectively inhibits CaM-stimulated cAMP phosphodiesterase activity, exhibiting an IC50 of 3.3 nM. This compound demonstrates significant biological activity by preventing estrogen-induced transcription activation mediated by estrogen receptors. Additionally, Zaldaride reversibly blocks voltage-activated sodium, calcium, and potassium currents in PC12 cells, and also inhibits nicotinic acetylcholine receptors (nAChR), making it a valuable tool for research into calcium signaling pathways and their related physiological processes. -
GABA/Glutamate-gated Chloride Channel Potentiator
4''-Oxoavermectin B1a is a potent modulator of GABA (γ-aminobutyric acid) and glutamate-gated chloride channels, exhibiting significant insecticidal and acaricidal properties. This compound demonstrates efficacy in disrupting neurological processes in target pests, making it a valuable tool for research in agricultural pest management. Its application contributes to understanding the mechanisms of action in pest control strategies. -
GABAA Receptor Chloride channel Inhibitor
Leptophos oxon is a potent GABAA receptor chloride channel inhibitor, exhibiting an IC50 value of 89.6 μM. This compound effectively inhibits GABA-induced chloride influx through binding to the TBPS sites associated with GABAA receptors, as well as inhibiting TBPS binding to voltage-dependent chloride channels. Leptophos oxon is primarily utilized in studies related to neurological diseases and functions as an insecticide, making it relevant for research in both neurobiology and pest management. -
Stable Isotope
γ-Aminobutyric acid-d6 is a deuterium-labeled form of γ-Aminobutyric acid, a crucial inhibitory neurotransmitter in the mammalian central nervous system. This compound primarily targets ionotropic GABA receptors (GABAA) and metabotropic receptors (GABAB), playing a significant role in regulating neuronal excitability. It is useful in research applications focused on neurotransmitter dynamics, GABAergic signaling, and metabolic studies involving stable isotopes. -
GABA(A) Receptors Blocker
Bicuculline methiodide is a potent blocker of GABA(A) receptors, serving to inhibit GABA-mediated neurotransmission. By altering membrane properties and firing patterns, it effectively reduces Apamin-sensitive afterhyperpolarization, enhancing neuronal excitability. This compound is valuable for research applications focused on understanding the role of GABA(A) receptors in synaptic transmission and studying neuronal firing behaviors in various neurological models. -
GABAB Receptor Antagonist
Saclofen is a competitive antagonist of the GABAB receptor, exhibiting an IC50 value of 7.8 μM. It demonstrates weak antagonistic activity towards the GABAB1b and GABAB2 heterodimeric receptors. Saclofen effectively inhibits Baclofen binding to rat cerebellar membranes and blocks Baclofen-induced circadian phase shifts. Additionally, it has shown anti-inflammatory and analgesic effects in preclinical models. This makes Saclofen a valuable tool for investigating GABAB receptor functions and related biological processes. -
GABAB Receptor Antagonist
CGP35348 is a selective GABAB receptor antagonist exhibiting a central nervous system penetration with an EC50 of 34 μM. This compound specifically targets the GABAB receptor, demonstrating potential to enhance neuromuscular coordination and spatial learning in animal models, particularly following neonatal brain injury. Its unique mechanism offers a valuable tool for researching the effects of GABAB receptor modulation on cognitive functions and motor behavior. -
GABAB Receptor Antagonist
CGP55845 hydrochloride is a potent and selective antagonist of the GABAB receptor, exhibiting an IC50 of 6 nM. This compound is valuable in neurological research, providing insights into GABAergic signaling pathways and their implications in various neurological disorders. Researchers use CGP55845 hydrochloride to investigate the role of GABAB receptors in synaptic transmission and neuronal excitability. -
GABA Receptor
17β-Estradiol sulfate sodium is a neuroactive steroid that acts as a modulator of the GABA receptor. This compound exhibits significant biological activity by influencing neurotransmission and neuroprotection, making it useful in research related to neuropharmacology and hormone signaling. Its applications include studying the effects of estrogens on the central nervous system and investigating potential therapeutic targets for neurological disorders.
