Catalog No.
Product Name
Application
Product Information
Citations
- COG 133 TFA is a fragment of Apolipoprotein E (APOE) peptide. COG 133 TFA competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 TFA is also a nAChR antagonist with an IC50 of 445 nM.
- Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
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FFAR3 agonist
AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, also known as GPR41), with an IC₅₀ of 117 nM. It demonstrates anti-inflammatory, antitumor, and antidiabetic activities. AR420626 improves neurogenic diarrhea by modulating neural pathways mediated by nicotinic acetylcholine receptors (nAChRs). In cancer models, it suppresses the growth of HepG2 xenografts and inhibits hepatoma cell proliferation through apoptosis induction. Additionally, AR420626 mitigates allergic asthma and eczema and enhances glucose uptake by activating FFAR3-mediated Ca²⁺ signaling, offering potential therapeutic benefits in metabolic disorders such as diabetes. -
Nicotinic α7 Positive Allosteric Modulator
RGH-857 acts as a selective and potent positive allosteric modulator of nicotinic α7 receptors. It demonstrates effectiveness in ameliorating amnesia and is valuable in studies related to Alzheimer's disease. This compound can facilitate research into cognitive impairment and potential therapeutic interventions in neurodegenerative disorders. -
Apoptosis Inducer
Crebanine is an isoquinoline-like alkaloid that acts as an apoptosis inducer through antagonism of the α7-nAChR, exhibiting an IC50 value of 19.1 μM. This compound suppresses cancer cell proliferation, migration, and invasion while triggering a reactive oxygen species (ROS) burst that promotes apoptosis. Additionally, Crebanine modulates critical signaling pathways including AKT/FoxO3a, NF-κB, and MAPK, and demonstrates antioxidant properties in microglia by reducing ROS and lipid peroxidation. With applications in studying hepatocellular carcinoma, cerebral ischemia, and Alzheimer's disease, Crebanine may also ameliorate cognitive deficits and ischemia-reperfusion brain damage in rodent models. -
Histone Methyltransferase
Lobelane hydrochloride selectively inhibits the vesicular monoamine transporter-2 (VMAT2). This compound demonstrates an affinity for VMAT2 with a K(i) value of 630 nM, while exhibiting low interaction with nicotinic acetylcholine receptors (nAChR). The unique mechanism of action of lobelane hydrochloride makes it a valuable tool for studying neurotransmitter dynamics and offers potential in the development of therapeutic agents aimed at addressing methamphetamine abuse. Its structural analogs may further expand its applications in neuropharmacological research. -
α7 nAChR Agonist/5-HT3 antagonist
(S)-PNU-282987 hydrochloride is a potent agonist of the α7 nicotinic acetylcholine receptor (nAChR), exhibiting an EC50 of 154 nM. In addition, it acts as a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. This compound is valuable for research applications exploring the central and peripheral nervous systems, facilitating the study of neurotransmission and signaling pathways involving cholinergic and serotonergic systems. -
nAChR Agonist
Facinicline (RG3487) is an orally active partial agonist of the nicotinic α7 receptor, exhibiting a Ki of 6 nM for human nAChR. This compound has been shown to enhance cognitive function and sensorimotor gating in rodent models, providing a valuable tool for research into cognitive disorders. Additionally, Facinicline hydrochloride demonstrates high affinity as an antagonist at 5-HT3 receptors with a Ki value of 1.2 nM, further broadening its potential applications in neuroscience research. -
α7-nAChR Agonist
GTS-21 is a selective agonist of the alpha7 nicotinic acetylcholine receptor (α7-nAChR), known for its anti-inflammatory and cognitive-enhancing properties. Additionally, GTS-21 exhibits antagonistic activity at the α4β2 receptor (Ki=20 nM) and the 5-HT3A receptor (IC50=3.1 μM). This compound is utilized in research related to age-associated memory impairment (AAMI) and Alzheimer's disease, making it a valuable tool for investigating cognitive dysfunction and neuroinflammatory processes. -
Apoptosis Inhibitior
(S)-Oxiracetam is an apoptosis inhibitor that targets the PI3K/Akt/GSK3β signaling pathway via α7 nAChR activation. It has demonstrated efficacy in reducing brain infarct size and alleviating neurological dysfunction in middle cerebral artery occlusion/reperfusion (MCAO/R) models. This compound effectively prevents neuronal apoptosis, making it a valuable research tool for studies focused on ischemic stroke and neuroprotection. -
α7 nAchR/JAK2/STAT3 Agonist
α7 nAchR-JAK2-STAT3 agonist 1 is a selective agonist targeting the α7 nicotinic acetylcholine receptor, modulating the JAK2-STAT3 signaling pathway. It demonstrates significant anti-inflammatory activity by inhibiting the expression of inducible nitric oxide synthase (iNOS), interleukin-1 beta (IL-1β), and interleukin-6 (IL-6) in murine RAW264.7 macrophages, with an IC50 of 0.32 μM for nitric oxide production. Additionally, it effectively suppresses lipopolysaccharide (LPS)-induced nitric oxide release, NF-κB activation, and related cytokine production. This compound is valuable for studying sepsis and inflammatory responses. -
Anti-Inflammatory Compound
Cynandione A is an acetophenone compound with anti-inflammatory properties. It has been shown to protect hepatocytes and cortical neurons from toxicity, as well as improve neurological deficits in a rat model of cerebral ischemia. Additionally, Cynandione A exerts significant anti-inflammatory effects through the activation of macrophage α7 nAChR and the expression of IL-10, making it a valuable tool for research in neuroprotection and inflammation. -
nAChR Antagonist
Mecamylamine is a nonselective, noncompetitive antagonist of nicotinic acetylcholine receptors (nAChR). It functions as a ganglionic blocker and is capable of crossing the blood-brain barrier. Mecamylamine is utilized in research focused on neuropsychiatric disorders, hypertension, and the development of antidepressant therapies. -
α7 nAChR Agonist
A-582941 is a selective α7 nicotinic acetylcholine receptor (nAChR) agonist that effectively crosses the blood-brain barrier. With Ki values of 10.8 nM in rat brain and 17 nM in human frontal cortex, it demonstrates significant biological activity by promoting ERK1/2 and CREB phosphorylation, inhibiting GSK-3β through Ser-9 phosphorylation, and enhancing acetylcholine release. Additionally, A-582941 induces the expression of activity-regulated cytoskeleton-associated protein (Arc) and c-Fos while activating brain regions linked to working memory and attention. This compound is valuable for investigating mechanisms involved in Alzheimer's disease and schizophrenia. -
Nicotine Metabolite
(±)-Nornicotine is a significant metabolite of nicotine, acting as a partial agonist of nicotinic acetylcholine receptors (nAChRs) that contain α7 and α6 subunits. This compound is known to disrupt β-catenin and ZO-1 interactions while inducing depolymerization of F-actin, contributing to its biological effects. (±)-Nornicotine has been implicated in research on various conditions, including atherosclerosis, Alzheimer's disease, and schizophrenia, making it a valuable tool for studies involving neural and vascular pathophysiology. -
Stable Isotope
(±)-Nornicotine-d4 is a deuterium-labeled analog of (±)-Nornicotine, a significant metabolite of nicotine. It acts as a partial agonist at nicotinic acetylcholine receptors (nAChRs), particularly those containing α7 and α6 subunits, influencing various biological pathways. This compound has been shown to disrupt β-catenin and ZO-1 interactions while inducing F-actin depolymerization. (±)-Nornicotine-d4 is valuable for research focused on atherosclerosis, Alzheimer's disease, and schizophrenia, providing insights into nicotine's metabolic effects and related neurological conditions. -
α7nAChR Activator
Lemairamin, an α7nAChR activator, is a hydroxylamine compound derived from the pericarps of Zanthoxylum species. This compound is known to stimulate the expression of anti-inflammatory cytokine IL-10 and proopiomelanocortin (POMC), while concurrently reducing Akt activity. Lemairamin has demonstrated efficacy in attenuating dextran sulfate sodium (DSS)-induced intestinal inflammation and alleviating pain hypersensitivity, making it a valuable reagent for research in inflammation and pain modulation. -
α4β2 nAChR Agonist
TC-2559 free base is an agonist of the α4β2 nicotinic acetylcholine receptor (nAChR), demonstrating an EC50 value of 0.18 μM. It exhibits reduced potency on β4-containing nAChR subtypes, such as α2β4, α4β4, and α3β4, with EC50 values between 10-30 µM. Research indicates that TC-2559 enhances dopamine neuron activity in the ventral tegmental area, which may influence excitability and aggression. Additionally, it possesses anti-inflammatory effects via STAT3 inhibition, proving beneficial in models of mechanical allodynia and cognitive deficits. This compound is useful for investigations into nerve pain and related neurological conditions. -
RVG Peptide
RVG (RVG29) is a peptide derived from Rabies Virus Glycoprotein that specifically binds to the α-7 subunit of nicotinic acetylcholine receptors (nAChRs) on neuronal cells. This interaction facilitates the enhanced delivery of Mycobacterium tuberculosis antigens to antigen-presenting cells, making RVG valuable for immunological research and vaccine development studies targeting tuberculosis. -
nAChR Agonist
Pyrantel is an orally active anthelmintic that functions as an agonist of the nicotinic acetylcholine receptor (nAChR). It induces spasmodic muscle paralysis in parasitic organisms, making it effective in the eradication of a variety of helminthic infections. Pyrantel is commonly utilized in the study and treatment of conditions such as ascariasis, hookworm infections, pinworm infections, and trichinosis, providing critical research insights into parasitic diseases. -
nAChR Agonist
Facinicline hydrochloride is a selective partial agonist of the nicotinic α7 acetylcholine receptor (nAChR), exhibiting a Ki of 6 nM. This compound has demonstrated potential in enhancing cognitive function and sensorimotor gating in rodent models, making it a valuable tool for research on cognitive disorders. Additionally, Facinicline hydrochloride shows high affinity as an antagonist at the 5-HT3 receptor, with a Ki of 1.2 nM, widening its applicability in neurological and psychiatric research. -
α7 nAChR Agonist
NS-6740 is a partial agonist of the α7 nicotinic acetylcholine receptor (α7 nAChR), exhibiting an IC50 of 3 nM. This compound functions as a potent modulator of the cholinergic anti-inflammatory pathway, influencing α7 signaling in an ion channel-independent manner, which ultimately reduces synaptic function. NS-6740 promotes the desensitized state of α7 nAChR and elicits substantial nAChR-mediated currents. It is effective in decreasing LPS-induced TNF-α release from microglia, making it a valuable tool for research into neuroinflammation and neuropathic pain mechanisms. -
α7 Nicotinic Acetylcholine Receptor Inhibitor
NS-6740 hydrochloride is a potent partial agonist of the α7 nicotinic acetylcholine receptor (α7 nAChR), exhibiting an IC50 of 3 nM. It functions as a modulator of the cholinergic anti-inflammatory pathway and alters α7 signaling in an ion channel-independent manner, which diminishes synaptic function and promotes receptor desensitization. NS-6740 hydrochloride has been shown to significantly reduce LPS-induced TNF-α release from microglia, making it a valuable tool in the study of neuroinflammation and neuropathic pain mechanisms. -
α7 nAChR Inhibitor
Conofurin-Delta is a potent inhibitor of the α7 nicotinic acetylcholine receptor (nAChR), exhibiting an IC50 of 177 nM. Additionally, it demonstrates inhibitory activity against the α9α10 nAChR with an IC50 of 98.1 nM. This compound is relevant for research applications in the study of SARS-CoV-2 infection and its impact on cholinergic signaling pathways. -
Pesticide
(S)-Dinotefuran is a neonicotinoid pesticide that primarily targets the α8 subunit of nicotinic acetylcholine receptors (nAChRs) in honeybees, Apis mellifera. It exhibits higher toxicity compared to its R-enantiomer, R-dinotefuran, affecting the survival and behavior of these important pollinators. This compound is utilized in ecological and toxicological research to study the impact of pesticides on non-target species and to evaluate the risks associated with neonicotinoid exposure in agricultural settings. -
Insecticide
Thiacloprid is an orally active neurotoxic insecticide that functions as an agonist of nicotinic acetylcholine receptors (nAChR). It has been shown to reduce cellular viability, deplete reduced glutathione, and elevate malondialdehyde (MDA) levels, leading to cytotoxicity and oxidative stress. While Thiacloprid exhibits lower acute toxicity to honeybees compared to some other insecticides, it adversely affects their learning, memory, immune function, and overall survival. Additionally, this compound disrupts intestinal microbiota, increasing the risk of premature colony collapse in bumblebees. Thiacloprid is utilized in the broad-spectrum control of agricultural pests across various crops, including potatoes, cabbages, fruits, vegetables, and nuts. -
nAChR Aagonist
Simpinicline (OC-02) is a highly selective agonist of the nicotinic acetylcholine receptor (nAChR). This compound exhibits potent antiviral activity against SARS-CoV-2 variants in cell culture, with an IC50 value of 0.04 µM. Its unique selectivity and efficacy make it a valuable tool for research in virology and neuropharmacology. -
Anthelmintic Agent/Immunoregulatory Agent
Levamisole is an anthelmintic agent recognized for its immunoregulatory properties. This compound functions as a positive allosteric modulator of the α3β2 (EC50 = 300 μM) and α3β4 (EC50 = 100 μM) subtypes of nicotinic acetylcholine receptors (nAChRs), enhancing receptor activity. It is orally active and is commonly used in research applications related to parasitic infections and immune response modulation. -
Nicotinic acetylcholine receptors Inhibitor
Dinotefuran is a competitive inhibitor targeting insect nicotinic acetylcholine receptors (nAChRs). This compound effectively disrupts neural signaling in insects, leading to dysfunction. With an IC50 of 890 nM for [3H]epibatidine and 36.1 μM for [3H]α-bungarotoxin in American cockroach neural membranes, Dinotefuran demonstrates significant knockdown (KD50=0.351 nmol/g) and lethal activity (LD50=0.173 nmol/g) against German cockroach. Its primary applications include agricultural pest control, specifically targeting piercing-sucking and chewing insects like aphids and planthoppers, and it also serves as a tool for studying environmental toxicological impacts such as oxidative stress and reproductive neurotoxicity in earthworms. -
nAChR Antagonist
Derquantel is a spirocyclic anthelmintic that functions as a competitive antagonist of nicotinic acetylcholine receptors (nAChRs). It inhibits acetylcholine-induced depolarization with an IC50 of 0.22 μM, leading to flaccid paralysis of nematode somatic muscles. This mechanism effectively dislodges parasites from the host gastrointestinal tract, making Derquantel a valuable tool in research related to Haemonchus contortus and Ascaris suum infections. -
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. -
nAChR Desensitizer
Anagyrine is a quinolizidine alkaloid that acts as a desensitizer of nicotinic acetylcholine receptors (nAChR). It demonstrates binding affinity with IC50 values of 132 µM for muscarinic receptors and 2096 µM for nicotinic receptors, effectively modulating nAChR activity. This compound is utilized in research to study nAChR desensitization mechanisms and its implications in various neural and pharmacological contexts. -
nAChR/mAChR Agonist
Arecoline hydrochloride is a partial agonist of nicotinic and muscarinic acetylcholine receptors (nAChR/mAChR). This psychoactive alkaloid demonstrates stimulation, increased alertness, anxiolytic effects, and possesses anti-parasitic properties. Additionally, Arecoline hydrochloride can induce oxidative stress, making it a valuable compound for research in neuropharmacology and parasitology. -
nAChR Desensitizer
Anagyrine hydrochloride is a quinolizidine alkaloid that serves as a desensitizer of nicotinic acetylcholine receptors (nAChR). It exhibits potent binding to muscarinic acetylcholine receptors with an IC50 value of 132 µM and a weaker interaction with nAChR at 2096 µM. This compound effectively desensitizes nAChR without requiring metabolic conversion, making it valuable for research involving cholinergic signaling and receptor function studies. -
nAChR Inhibitor
Meclofenoxate, a nAChR inhibitor, is an ester derived from dimethylaminoethanol (DMAE) and para-chlorophenylalanine (pCPA). It is known for its potential to enhance memory and cognitive function. Meclofenoxate is commonly utilized in neurological research to investigate mechanisms underlying cognitive enhancement and memory improvement. -
α-isomer of Nicotine
α-Nicotine is the α-isomer of nicotine and functions as an agonist of nicotinic acetylcholine receptors (nAChRs). This compound exhibits notable biological activity that may be beneficial for understanding neuropsychiatric disorders, including schizophrenia and attention deficit hyperactivity disorder (ADHD). Its potential applications in research make it a valuable tool for exploring the pharmacological effects of nAChR activation. -
Endogenous Metabolite
Cotinine, a primary metabolite of nicotine, acts as an endogenous biomarker for tobacco exposure. This alkaloid exhibits vasodepressor activity and has demonstrated antiproliferative effects when combined with nicotine against conditions such as pterygium. Additionally, (S)-(-)-Cotinine activates nicotinic acetylcholine receptors (nAChR) in a calcium-dependent manner, facilitating dopamine release. Due to its diverse biological activities, cotinine is employed in research focused on cardiovascular and inflammatory diseases. -
nAChRs Antagonist
Dihydro-β-erythroidine hydrobromide is a competitive antagonist specifically targeting neuronal nicotinic acetylcholine receptors (nAChRs). It demonstrates notable selectivity for the α4β4 and α4β2 nAChR subtypes, with IC50 values of 0.19 μM and 0.37 μM, respectively. This compound is utilized in research exploring its potential antidepressant-like effects and its role in understanding nAChR-mediated signaling pathways. -
Acetylcholine Agonist
Spinosad is an acetylcholine agonist that acts primarily on the nicotinic acetylcholine receptors (nAChRs) in the insect nervous system. Derived from the fermentation products of the soil actinomycete Saccharopolyspora spinosa, Spinosad exhibits potent biological neurotoxic activity, making it effective as a broad-spectrum insecticide. Its favorable environmental and mammalian safety profile, along with its larvicidal properties, supports its use in various pest control applications. -
Insecticide
Acetamiprid is a neonicotinoid insecticide that acts as a selective agonist of nicotinic acetylcholine receptors (nAChRs). It disrupts normal synaptic transmission, leading to paralysis and death in target pests. Research applications include studies on neuromuscular function, insect behavior, and potential reproductive impacts in non-target organisms. -
α7 nAChR Agonist
PHA-543613 is a selective agonist of the α7 nicotinic acetylcholine receptor (nAChR), exhibiting a Ki value of 8.8 nM. This compound demonstrates significant selectivity for the α7 nAChR compared to other nicotinic and serotonergic receptors, including α3β4, α1β1γδ, α4β2, and 5-HT3. PHA-543613 is applicable in research focused on cognitive deficits associated with Alzheimer's disease and schizophrenia, making it a valuable tool for neuropharmacological studies. -
Insecticide
Flupyradifurone is a systemic agonist of nicotinic acetylcholine receptors (nAChRs) that disrupts signal transduction in the central nervous system of sap-sucking insects. It functions as a butenolide insecticide, effectively targeting pest populations while offering low toxicity to non-target organisms. Research applications include studying insect neurobiology and developing pest management strategies. -
nAChR Agonist
Tebanicline dihydrochloride is a selective agonist of nicotinic acetylcholine receptors (nAChRs), particularly targeting the α4β2 subtype. It exhibits strong analgesic properties and demonstrates oral bioavailability. This compound is valuable for research into pain management and the modulation of cholinergic signaling in neurological studies. -
nAChR Antagonist
Coclaurine is a tetrahydroisoquinoline alkaloid and a potent antagonist of nicotinic acetylcholine receptors (nAChRs). It exhibits significant anticancer activity by downregulating EFHD2-related NOX4-ABCC1 signaling, thereby enhancing the sensitivity of cancer cells to Cisplatin. Coclaurine also suppresses the stemness and metastatic potentials of non-small cell lung cancer (NSCLC) cells through the disruption of the FOXG1-EFHD2 promoter interaction, leading to reduced EFHD2 transcription. This compound serves as a valuable tool for research focused on cancer therapy and the modulation of nAChR signaling. -
AChE Reversible Inhibitor
Asoxime dichloride is a reversible inhibitor of acetylcholinesterase (AChE) that functions as a thiosemicarbazone-based antidote. Its primary mechanism involves reactivating AChE that has been inhibited by nerve agents, thus restoring cholinergic nerve function. Additionally, Asoxime dichloride enhances muscle function in the presence of poisoning without reactivating AChE and acts as an antagonist to acetylcholine receptors, including nicotinic and α7 nAChRs. Due to its immunomodulatory properties, Asoxime dichloride can also enhance the immune response of the nervous system, making it valuable in neuropharmacological research. -
nAChR Inhibitor
Lupanine is a natural ketonic derivative of Sparteine that acts as an inhibitor of nicotinic acetylcholine receptors (nAChR). It exhibits binding affinity to these receptors with a Ki value of 500 nM, demonstrating its potential as a ganglioplegic agent. Lupanine is utilized in research applications related to neuromodulation and the study of cholinergic signaling pathways. -
nAChR Activator
Myosmine is a specific alkaloid derived from tobacco that acts as an activator of nicotinic acetylcholine receptors (nAChR). It exhibits a relatively low affinity for the α4β2 nAChR subtype, with a Ki value of 3300 nM. Myosmine is utilized in research to explore the pharmacological effects of nAChR modulation and its implications in neurobiology and addiction studies. -
nAChR Antagonist
AT 1001 is a selective antagonist of the α3β4 nicotinic acetylcholine receptor (nAChR), with a high affinity characterized by a Ki value of 2.64 nM. This compound effectively reverses inward currents triggered by Epibatidine in HEK cells expressing α3β4 nAChR. AT 1001 demonstrates dose-dependent inhibition of nicotine self-administration in rat models, while sparing food-reinforced responding, making it a valuable tool in nicotine addiction and smoking cessation therapy research. -
nAChR Agonist
Pozanicline dihydrochloride is a selective agonist for nicotinic acetylcholine receptors (nAChRs), specifically targeting the α4β2 subtype with a binding affinity (Ki) of 17 nM at rat brain nAChR sites. It exhibits an affinity of 16.7 nM for [3H]cytisine binding sites, demonstrating its potential in modulating cholinergic signaling. This compound is instrumental in research focused on neurological disorders, cognition enhancement, and the exploration of nAChR-related pathways. Its oral bioavailability further supports its utility in in vivo studies. -
nAChR Antagonist
Chlorisondamine diiodide is a potent antagonist of the nicotinic acetylcholine receptor (nAChR), functioning as a ganglion blocker. It effectively inhibits specific central actions of nicotine with notable potency and pharmacological selectivity. This compound is valuable in research applications exploring neural signaling, autonomic regulation, and addiction pathways.
