Catalog No.
Product Name
Application
Product Information
Citations
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A1 Adenosine Receptor Agonist
CCPA (2-Chloro-N6-cyclopentyladenosine) is a highly selective agonist for A1 adenosine receptors, demonstrating a Ki value of 0.4 nM. This compound effectively inhibits adenylate cyclase, with an IC50 of 33 nM. CCPA is relevant in studies investigating anti-seizure and cardioprotective effects, making it a valuable tool for research related to seizures and myocardial infarction. -
NF-κB Expression Reducer, ERK 1/2 Activator, Beta-Adrenergic Receptor Modulator, Calcium Channel Inhibitor
Eupatorin is a flavonoid that functions primarily as an NF-κB expression reducer and an ERK 1/2 activator, while also modulating beta-adrenergic receptors and inhibiting calcium channels. It demonstrates significant antiproliferative and vasodilatory effects, inducing apoptosis and causing G2/M phase cell cycle arrest, alongside reactive oxygen species (ROS) production. Eupatorin has been shown to impact inflammatory mediators and calcium signaling pathways, making it relevant for research in breast cancer, hypertension, and leukemia. Metabolized by CYP1A1 and other CYP1 enzymes, Eupatorin yields bioactive metabolites that maintain antiproliferative properties. -
Adrenergic Receptor Antagonist
Aaptamine is an alkaloid derived from the marine sponge Aaptos suberitoides, functioning primarily as a competitive antagonist of the α-adrenergic receptor. This compound exhibits significant cytotoxicity against tumor cells, inducing apoptosis and cell cycle arrest while promoting p21 expression through a p53-independent mechanism. Aaptamine also demonstrates a variety of biological activities, including anti-tumor, antioxidant, antibacterial, and analgesic effects, making it a valuable tool for cancer research and therapeutic applications. -
α-1A Adrenergic Receptor Agonist
Dabuzalgron is a selective α-1A adrenergic receptor agonist primarily utilized for the treatment of urinary incontinence. This compound exhibits key biological activity by enhancing bladder function, thereby mitigating symptoms associated with overactive bladder. Additionally, Dabuzalgron has been shown to provide protection against Doxorubicin-induced cardiotoxicity through the preservation of mitochondrial function, making it relevant in cardiovascular research. -
S1PR1 Antagonist
W146 TFA is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1), exhibiting an EC50 value of 398 nM. This compound is instrumental in studying the role of S1PR1 in various biological processes, including immune modulation and cardiovascular function. W146 TFA is valuable for research applications involving cytokine signaling and cellular proliferation pathways. -
ICMT Inhibitor
UCM-1336 is a potent inhibitor of Isoprenylcysteine Carboxyl Methyltransferase (ICMT), exhibiting an IC50 of 2 μM. This compound effectively induces mislocalization of endogenous Ras, resulting in decreased Ras activation. UCM-1336 has shown the ability to trigger cell death through autophagy and apoptosis, making it a valuable tool for research in cancer biology and signal transduction pathways. -
5-HT2/D1/D2 Antagonist
Olanzapine-d3 is a deuterated form of olanzapine, targeting multiple receptors, including serotonin receptors 5-HT2A, 5-HT2C, and dopamine receptors D1 to D4. This selective and orally active monoaminergic antagonist exhibits high affinity binding with Ki values ranging from 4 to 57 nM for relevant targets. It is primarily utilized in research related to psychopharmacology and the treatment of schizophrenia and bipolar disorder, enabling detailed pharmacokinetic studies and investigation of receptor interactions. -
mGlu1 Antagonist
LY456236 is a selective, non-competitive antagonist of the metabotropic glutamate receptor 1 (mGlu1), exhibiting an IC50 of 0.145 μM for the inhibition of phosphatidylinositol hydrolysis. Additionally, it demonstrates inhibitory activity against EGFR with an IC50 of 0.918 μM. By targeting the MAPK pathway, LY456236 effectively blocks cell proliferation and reverses the anti-apoptotic effects of DHPG. This reagent is suitable for investigations in epilepsy and related neurological research. -
GLP-1R Agonist/GIPR Antagonist
Maridebart cafraglutide is a novel peptide-antibody conjugate that serves as a GLP-1 receptor agonist and GIP receptor antagonist. This compound exhibits potent agonistic activity against GLP-1 receptors across species, with EC50 values of 24.4 pM for human, 5.7 pM for cynomolgus monkey, 2.4 pM for rat, and 123 pM for mouse. Additionally, it shows antagonistic effects on GIP receptors with IC50 values of 46.4 nM in human, 26.5 nM in cynomolgus monkey, and 822.3 nM in rat models. Maridebart cafraglutide is primarily used for investigating mechanisms of obesity and type 2 diabetes. -
GIP/GLP-1 Agonist
Ribupatide is a dual agonist targeting both gastric inhibitory polypeptide (GIP) and glucagon-like peptide 1 (GLP-1) receptors. It exhibits significant antidiabetic activity, making it a valuable compound for research applications focused on metabolic disorders and diabetes management. Its dual mechanism may provide insights into the intricate regulation of glucose metabolism. -
GIP/GLP-1 Agnonist
Relsipatide is a dual agonist of the gastric inhibitory polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. This compound demonstrates significant potential in enhancing insulin secretion and reducing glucagon levels, making it a valuable tool in antidiabetic research. Its unique mechanism of action may contribute to improved glycemic control and metabolic regulation in diabetes studies. -
PEGylated Exenatide
Visepegenatide is a PEGylated form of Exenatide, primarily targeting GLP-1 receptors to enhance insulin secretion and improve beta-cell function. This compound demonstrates significant activity in reducing hyperglycemia and managing insulin resistance. Visepegenatide is a valuable tool for research focused on type 2 diabetes and related metabolic disorders. -
GIP/GLP Agonist
Enicepatide is a dual agonist for the gastric inhibitory polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. This compound is primarily investigated for its antidiabetic properties, contributing to glucose metabolism regulation and insulin secretion enhancement. Research applications include exploring its potential role in treating metabolic disorders and obesity-related conditions. -
GIP/GLP-1 Agonist
Astepatide is a dual agonist of the gastric inhibitory peptide (GIP) receptor and glucagon-like peptide-1 (GLP-1) receptor, which primarily influences glucose metabolism and insulin secretion. This compound demonstrates significant anti-diabetic activity, making it a valuable tool for research related to diabetes and metabolic disorders. Astepatide can aid in exploring mechanisms of action and therapeutic potential for obesity and type 2 diabetes. -
Anti-diabete Agent
Glyceollin III is a soybean-derived glyceollin that functions as an anti-diabetic agent. It enhances insulin-stimulated glucose uptake and promotes the secretion of glucagon-like peptide-1 (GLP-1). This compound is valuable for research focused on type 2 diabetes and its metabolic effects. -
H1 receptor Antagonist
R 58639 is a selective histamine H1 receptor antagonist. It demonstrates significant biological activity in the modulation of allergic responses and cognitive processes. This compound is primarily utilized in research focusing on the pathophysiology and treatment of gastric ulcers, providing insights into the role of H1 receptor signaling in gastrointestinal biology. -
Histamine H2 Receptor Agonist
Betazole hydrochloride is a pyrazole derivative that acts as a histamine H2 receptor agonist. This compound stimulates gastric acid secretion and significantly elevates common bile duct pressure. Betazole is primarily utilized as a diagnostic agent, known as histalog, to assess gastric acid secretory capacity. -
Antihistamine
Diphenhydramine is a first-generation antihistamine that functions primarily as a histamine H1-receptor antagonist. It exhibits anti-cholinergic properties, allowing it to effectively alleviate allergic symptoms. This compound is capable of crossing the blood-brain barrier, making it valuable in neurological studies and research focused on central nervous system effects. Its diverse applications also include exploration in pharmacology and behavioral research involving sedative effects. -
Serotonin Receptor Antagonist
Trazodone is a triazolopyridine derivative that primarily functions as a serotonin receptor antagonist and reuptake inhibitor. It exhibits significant antidepressant and sleep-inducing activities, making it valuable in the study of mood disorders and insomnia. Additionally, Trazodone demonstrates antagonistic effects on α1- and α2-adrenergic receptors as well as histamine H1 receptors, while displaying minimal anticholinergic activity. -
Histamine 1 Receptor Blocker
Ketotifen is an orally active second-generation noncompetitive antagonist of the histamine H1 receptor, known for its role as a mast cell stabilizer. It exhibits significant biological activity by inhibiting 6-phosphogluconate dehydrogenase in vitro and displays antiviral properties against SARS-CoV-2 and the Influenza virus. Ketotifen is applicable in research focused on autoimmune encephalomyelitis (EAE) and contributes to studies aimed at preventing asthma attacks. -
Histamine Receptor Antagonist
Levocetirizine is a third-generation peripheral histamine H1-receptor antagonist. As the R-enantiomer of Cetirizine, it demonstrates a higher binding affinity for the H1 receptor compared to its S counterpart. Levocetirizine is primarily utilized in the management of allergic rhinitis and chronic idiopathic urticaria, providing effective relief from allergy-related symptoms. Its efficacy makes it a valuable tool in related pharmacological research. -
H1R-H4R Agonist
Amthamine dihydrobromide is an agonist of the histamine receptors H1R to H4R. This compound has been shown to induce liver congestion and necrosis of hepatocytes, providing a valuable model for studying the hepatotoxic effects associated with H1R-H4R activation. It is suitable for research applications focused on the roles of these receptors in liver function and pathology. -
Anti-histamine
Chlorpheniramine is an H1 antihistamine that primarily targets histamine receptors to alleviate symptoms associated with allergic reactions. It exhibits significant efficacy in reducing peripheral and central histamine-induced effects, making it a valuable tool in the study of allergic diseases and related pathophysiological processes. This compound is widely utilized in research applications focusing on allergy management and pharmacological interventions. -
D2/H1 Antagonist
Thiethylperazine is a potent antagonist of dopamine D2 and histamine H1 receptors. This phenothiazine derivative exhibits notable anti-emetic, antipsychotic, and antimicrobial properties, making it valuable in various therapeutic contexts. Additionally, it acts as a selective ABCC1 activator, contributing to the reduction of amyloid-β (Aβ) load in murine models, thus highlighting its potential relevance in neurodegenerative research. -
Histamine-1 (H1R) Receptor Agonist
2-Pyridylethylamine hydrochloride functions as an agonist for the histamine-1 (H1R) receptor. This compound has demonstrated the ability to mitigate joint injury induced by formalin in rat models. Additionally, it serves as a valuable tool for investigating spinal cord neuropeptide Y (NPY) release, contributing to research in neurobiology and pain mechanisms. -
Histamine 4 Receptor Agonist
4-Methylhistamine dihydrochloride is a potent and selective agonist of the histamine H4 receptor (H4R), exhibiting a Ki value of 50 nM. It demonstrates greater than 100-fold selectivity for hH4R compared to other histamine receptor subtypes, with an effective activation pEC50 of 7.4. This compound is valuable for research in cancer, inflammation, and immunology, particularly in studies related to lung cancer and skin inflammation. -
Histamine Receptor Antagonist
Adriforant hydrochloride is a potent antagonist of the histamine H4 receptor, exhibiting a binding affinity (Ki) of 2.4 nM and functional antagonism with a Ki of 1.56 nM. This compound is valuable for research applications related to immune modulation and inflammation, providing insights into histamine signaling pathways. Its specificity for H4 receptors positions it as a useful tool for studying various biological processes influenced by histamine. -
Antihistamine Agent
Hydroxyzine is an antihistamine agent that primarily targets histamine H1 receptors and functions as a serotonin antagonist. This compound exhibits anxiolytic properties, making it valuable for research applications related to generalized anxiety disorder. Its dual action provides insights into the interplay between histamine and anxiety regulation in various biological contexts. -
H1 receptor Antagonist
Mianserin is an orally active antagonist of the H1 receptor, exhibiting unique pharmacological properties. In addition to its primary mechanism, Mianserin activates κ-opioid and octopamine receptors, leading to the phosphorylation of ERK1/2 and CREB. This compound has demonstrated effects on social and exploratory behavior, as well as raising electroconvulsive thresholds. Mianserin is valuable for research into neurological disorders including depression and epilepsy. -
H1-Receptor Antihistamine
Methapyrilene hydrochloride is an orally active H1-receptor antihistamine that also exhibits anticholinergic properties. This pyridine-derived compound is primarily utilized in research related to allergic responses and histamine-mediated processes. Additionally, due to its hepatotoxic effects, methapyrilene hydrochloride can serve as a tool for studying periportal hepatic necrosis in vivo, providing insights into liver pathology and toxicity mechanisms. -
H3 Agonist
(R)-(-)-α-Methylhistamine dihydrochloride is a potent and selective agonist for the H3 histamine receptor, demonstrating a Kd of 50.3 nM. This compound has been shown to enhance memory retention and reduce memory impairment in preclinical models, making it valuable for research focused on cognitive function and neurological disorders. Its ability to penetrate the blood-brain barrier further supports its potential in brain-related studies. -
Histamine H2-receptor Antagonist
Tiotidine is a selective antagonist of the histamine H2 receptor, exhibiting a pA2 value of 7.3-7.8 in the guinea pig right atrium. This compound demonstrates low affinity for H1 and H3 receptors, allowing for targeted modulation of H2 receptor activity. Tiotidine is primarily used in research applications related to gastric acid secretion and histamine-related signaling pathways. -
H1 Histamine Receptor Antagonist
Clemastine is a potent H1 histamine receptor antagonist with the ability to cross the blood-brain barrier, providing effective antiallergic properties. In addition to its antihistamine action, Clemastine also interacts with muscarinic acetylcholine receptors, specifically M1 and M4 subtypes. This compound demonstrates significant biological activities, including promoting central nervous system remyelination, activating autophagy, and exhibiting anti-apoptotic and neuroprotective effects. Its anti-inflammatory properties further highlight its potential in various research applications related to allergy, neurodegeneration, and inflammation. -
Histamine Receptor Agonist
N-Methylhistamine dihydrochloride is a selective agonist of the histamine H3 receptor, playing an important role in the study of mastocytosis. This compound is instrumental in the diagnosis and management of this condition. Additionally, it acts as a valuable biomarker for evaluating mast cell accumulation in clinical assessments. -
Histamine H3/H4 Receptor Agonist
Imetit dihydrobromide is a potent and selective agonist of the histamine H3 and H4 receptors, exhibiting binding affinities with Ki values of 0.3 nM and 2.7 nM, respectively. This compound effectively mimics histamine, inducing morphological changes in eosinophils, with an EC50 value of 25 nM. Imetit dihydrobromide is valuable for researching mechanisms related to allergic responses and inflammation modulation. -
Histamine Metabolite
1-Methyl-4-imidazoleacetic acid hydrochloride is a stable histamine metabolite formed through the oxidation of N-methylhistamine. This compound serves as a valuable tool in research investigating histamine metabolism and its physiological roles. It can be utilized in studies related to receptor interactions and the biochemical pathways involving histamine. -
H1 Receptor Antagonist
Tecastemizole, a major metabolite of Astemizole, functions as a potent and selective antagonist of the H1 receptor. It exhibits notable anti-inflammatory properties, making it valuable for research into allergic responses and inflammation-related conditions. This compound is useful for studies investigating the modulation of histamine signaling pathways and their implications in various biological processes. -
Histamine Inhibitor
Spinacetin is a natural compound derived from Inula japonica that acts as a histamine inhibitor. It effectively inhibits histamine release, demonstrating notable anti-inflammatory properties. This reagent is valuable for research applications focused on allergic responses, inflammation studies, and the elucidation of histamine-related pathways. -
Histamine Receptor Inhibitor
Quinotolast sodium is a histamine receptor inhibitor that effectively blocks the release of histamine, LTC4, and PGD2 in a concentration-dependent manner within the range of 1-100 μg/mL. This compound is valuable for research applications focused on allergic responses and inflammatory processes, as it helps elucidate the mechanisms of histamine signaling and associated pathophysiologies. -
H1 Receptor Antagonist
Antazoline is a histamine H1 receptor antagonist that exhibits anticholinergic and antiviral activities. It functions by competitively inhibiting histamine binding to H1 receptors, thereby mitigating physiological allergic responses. This compound demonstrates a dose-dependent reduction of HBV DNA levels in HepAD38 and Huh7 cell lines, with EC50 values of 2.910 μmol/L and 2.349 μmol/L, respectively. Additionally, Antazoline may possess anti-arrhythmic properties relevant to acute myocardial infarction. Its diverse biological activities make it a valuable reagent for research in cardiovascular diseases and hepatitis B virus infections. -
Anticholinergic Agent
Benztropine is an orally active anticholinergic agent that effectively crosses the blood-brain barrier. It serves as a dopamine re-uptake inhibitor and a human D2 dopamine receptor allosteric antagonist, making it relevant in Parkinson's disease research. Additionally, Benztropine demonstrates potential anti-cancer stem cell activity, enhancing its applicability in oncology studies. -
Antipsychotic Agent
Levomepromazine maleate is an N-substituted phenylthiazine compound that acts as an antipsychotic agent primarily targeting dopamine receptors. This compound exhibits significant sedative properties and is also a potent inhibitor of CYP2D6, making it a valuable tool for investigating the pharmacological mechanisms underlying schizophrenia. Its multifaceted receptor-blocking activity contributes to its role in research applications related to neuropsychiatric disorders. -
Histamine H2 Antagonist
Zolantidine dimaleate is a potent and selective histamine H2 antagonist that effectively crosses the blood-brain barrier. This compound demonstrates significant antinociceptive activity, making it valuable for research focused on pain modulation and related neurological studies. Zolantidine dimaleate can be utilized in various experimental settings to investigate the mechanisms of pain relief and the role of histamine signaling in the central nervous system. -
H1 Histamine Receptor Antagonist
Thonzylamine is an orally active H1 histamine receptor antagonist that exhibits notable antihistaminic and antianaphylactic properties. This compound is valuable for research involving hypersensitivity diseases, as well as conditions such as nasal congestion and allergic conjunctivitis. Its targeted action on the H1 receptor makes it a useful tool in the study of various allergic disorders. -
Histamine H4 Receptor Agonist
VUF 8430 dihydrobromide is a potent and selective agonist of the histamine H4 receptor, exhibiting a Ki of 31.6 nM and an EC50 of 50 nM. This compound is valuable for investigating the role of the H4 receptor in immune response modulation and inflammation. Its specificity makes it a useful tool for research into histamine-related disorders and potential therapeutic applications in allergic and inflammatory conditions. -
histamine H4 receptor antagonist.
Seliforant is a selective histamine H4 receptor antagonist that is primarily utilized in the study of immune response modulation and allergic conditions. By inhibiting the H4 receptor, Seliforant demonstrates potential anti-inflammatory and anti-allergic activities, making it a valuable tool for researching pathways related to allergic diseases and immune regulation. Its oral bioavailability allows for convenient administration in various in vivo experimental settings. -
Histamine Antagonist
Dimethindene maleate is a selective histamine H1 antagonist known for its antihistaminic properties. It effectively mitigates hypersensitivity reactions, making it valuable in the study of allergic responses and other histamine-related conditions. Researchers utilize Dimethindene maleate to explore its effects on inflammation and allergic pathways. -
H1 Receptor Antagonist
Olopatadine is an orally active and selective antihistamine that functions as an H1 receptor antagonist and mast cell stabilizer. It effectively inhibits the release of pro-inflammatory mediators from human conjunctival mast cells, making it instrumental in the study of allergic conjunctivitis. Olopatadine is valuable in researching the mechanisms of allergic responses and the management of allergic symptoms. -
Histamine H1-Receptor Antagonist
Niaprazine is a selective histamine H1-receptor antagonist. It exhibits both antihistamine and antiserotonin properties, making it a valuable compound for investigating sleep disorders and related biological effects. Its ability to modulate neurotransmitter signaling is relevant for research into conditions such as insomnia and anxiety. -
H3R Inverse Agonist
H3R Antagonist 1 Hydrochloride is an inverse agonist of the histamine receptor 3 (H3R). This compound has been shown to elevate the expression levels of myelin-associated glycoprotein (MAG) and myelin basic protein (MBP) in differentiating oligodendrocytes. It serves as a valuable reagent for research investigating myelination processes and potential therapeutic strategies for multiple sclerosis.
