Catalog No.
Product Name
Application
Product Information
Citations
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CXCR4/STAT3 Inhibitor
Minecoside is a potent inhibitor of the CXCR4 receptor and STAT3 signaling pathway. It demonstrates significant anticancer and anti-inflammatory activities by downregulating CXCR4 expression and suppressing STAT3 activation, which leads to the inhibition of CXCL12-induced cellular invasion. Minecoside has been shown to effectively hinder cancer metastasis and enhance apoptosis, making it a valuable tool for research in cancer biology and therapeutic development. -
Dopamine Receptor Antagonist
Pimozide-d4 is a deuterated derivative of Pimozide, functioning primarily as a dopamine receptor antagonist. It demonstrates potent inhibitory activity with Ki values of 1.4 nM, 2.5 nM, and 588 nM against the dopamine D2, D3, and D1 receptors, respectively. Additionally, Pimozide-d4 exhibits affinity for the α1-adrenoceptor (Ki = 39 nM) and inhibits signaling pathways associated with STAT3 and STAT5. This compound is valuable for research focusing on neuropharmacology and the modulation of dopaminergic signaling pathways. -
Stable Isotope
Pimozide-d5 is a stable isotope-labeled form of Pimozide, a potent antagonist of dopamine receptors primarily targeting D2, D3, and D1 receptors with Ki values of 1.4 nM, 2.5 nM, and 588 nM, respectively. This compound also exhibits affinity for the α1-adrenoceptor with a Ki of 39 nM and has been shown to inhibit signaling pathways through STAT3 and STAT5. Pimozide-d5 is valuable in pharmacological studies and research involving dopamine signaling and receptor interaction. -
S1P Inhibitor
Pro-FTY is a sphingosine-1-phosphate (S1P) inhibitor functioning as an anticancer prodrug derived from FTY720. It selectively disrupts S1P signaling in cancer cells using a drug delivery system that reacts with acrolein, demonstrating significant cytotoxic effects on breast cancer cells, including multidrug-resistant variants. Pro-FTY effectively suppresses tumor growth in xenograft models with 4T1 cells and organoids, while maintaining immune cell integrity by avoiding lymphocytopenia. This reagent is valuable for research in cancer therapy and resistance mechanisms. -
Stable Isotope
Pimozide-d5 N-Oxide is a deuterium-labeled derivative of Pimozide, which primarily functions as a dopamine receptor antagonist, exhibiting Ki values of 1.4 nM, 2.5 nM, and 588 nM for dopamine D2, D3, and D1 receptors, respectively. Additionally, this compound has notable affinity for the α1-adrenoceptor with a Ki of 39 nM. Pimozide also inhibits the signaling pathways of STAT3 and STAT5, making it relevant for research applications in neurobiology and cancer biology studies. -
Histamine receptors inhibitor
Histamine Receptors Inhibitor 1 (compound 303) functions as an inhibitor of H1 and H4 histamine receptors. This compound demonstrates key biological activity in modulating inflammatory processes and is particularly relevant for research applications focusing on autoimmune, allergic, and ocular conditions. Its ability to selectively inhibit these receptors makes it a valuable tool for investigating histamine-mediated pathways in various biological contexts. -
Dopamine Receptor Agonist
Apomorphine is a potent dopamine receptor agonist with additional inhibitory effects on monoamine oxidases A and B. It demonstrates neuroprotective properties, evidenced by its ability to reduce reactive oxygen species production, inhibit DNA fragmentation, and downregulate JNK and ERK1/2 phosphorylation. Apomorphine also facilitates the degradation of intracellular Aβ40 and Aβ42, lowers tau protein levels, and suppresses MMP-9 expression. Its radical scavenging and iron chelating capabilities make it valuable for research in neurodegenerative conditions such as Alzheimer's disease and Parkinson's disease, as well as studies related to breast carcinoma and erectile dysfunction. -
PDD4 Inhibitor
Sitagliptin phosphate is a selective DPP4 inhibitor with a powerful mechanism of action, featuring an IC50 value of 19 nM. By inhibiting DPP4, this compound prevents the degradation of incretins such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP), resulting in enhanced active incretin levels. Additionally, it can directly stimulate GLP-1 secretion from intestinal L cells via the cAMP/PKA and ERK1/2 pathways, which operates independently of DPP-4. Sitagliptin phosphate is valuable for researching both type 1 and type 2 diabetes and demonstrates protective effects on pancreatic islet grafts in type 1 diabetes models. -
CRFR Agonist
Urocortin II, human is a selective agonist of the type-2 corticotropin-releasing factor (CRF2) receptor, exhibiting key biological activities that include promoting satiety and providing neuroprotective effects. This peptide also demonstrates bactericidal and antiparasitic properties, as well as pro-inflammatory activity. Additionally, Urocortin II, human can activate the NF-κB pathway and ERK1/2 MAP kinase, making it relevant for research in pulmonary arterial hypertension and cardiac protection. Its diverse applications extend to studies in infection, inflammation, metabolic disorders, neurological conditions, and cardiovascular diseases. -
Stable Isotope
Sitagliptin-d4 phosphate is a deuterium-labeled derivative of Sitagliptin phosphate, a selective inhibitor of dipeptidyl peptidase-4 (DPP4) with an IC50 value of 19 nM. This compound increases the levels of active incretins by inhibiting the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). Additionally, Sitagliptin-d4 phosphate can stimulate GLP-1 secretion from intestinal L cells through the activation of the cAMP/PKA and ERK1/2 pathways, independent of DPP-4. This reagent is valuable for research into type 1 and type 2 diabetes and can contribute to studies exploring pancreatic islet function. -
Vasoconstrictor
Endothelin-1 (1-31) (Human) is a potent vasoconstrictor that primarily targets endothelin receptors to induce vascular smooth muscle contraction. This peptide plays a significant role in regulating blood pressure and is involved in various cardiovascular pathologies. It is widely utilized in research applications focused on cardiovascular physiology, hypertension, and related therapeutic interventions. -
Stable Isotope
Carvedilol-d4 is a deuterated derivative of Carvedilol, a non-selective β/α-1 adrenergic receptor antagonist. It exhibits dose-dependent inhibition of lipid peroxidation with an IC50 value of 5 μM. Carvedilol acts as a multifaceted antihypertensive agent, demonstrating potential therapeutic applications in managing conditions such as angina and congestive heart failure. Additionally, it has been identified as an autophagy inducer and a modulator of the NLRP3 inflammasome, making it a valuable tool for research into cardiovascular and inflammatory diseases. -
Platelet Aggregation Inhibitor
Notoginsenoside Fc is a protopanaxadiol-type saponin derived from the leaves of Panax notoginseng, functioning primarily as a platelet aggregation inhibitor. This compound effectively mitigates platelet aggregation and has been shown to enhance reendothelialization after vascular injury in diabetic rat models by promoting autophagy. Its biological activity makes Notoginsenoside Fc a valuable reagent for research in cardiovascular health and vascular regeneration. -
Stable Isotope
Theophylline-d6 is a deuterium-labeled analog of Theophylline, primarily utilized as a stable isotope in research. Theophylline functions as a nonselective phosphodiesterase (PDE) inhibitor and adenosine receptor antagonist, while also acting as an activator of histone deacetylase (HDAC). This compound is valuable in studies exploring cellular signaling pathways, pharmacology, and the biochemical mechanisms underlying various therapeutic effects. -
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.
