Catalog No.
Product Name
Application
Product Information
Citations
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Anti-CXCR4 Antibody
LY-2624587 is a humanized IgG4 monoclonal antibody that antagonizes CXCR4. By blocking the interaction between SDF-1 and CXCR4, it inhibits SDF-1-induced GTP binding, significantly reducing cell migration and promoting apoptosis in human lymphoma and leukemia cells. Additionally, LY-2624587 impedes CXCR4 and SDF-1-mediated signaling pathways, including the activation of MAPK and AKT. This reagent is valuable for research applications involving human hematological malignancies, particularly acute myeloid leukemia (AML). -
CXCR4 Antagonist.
BPRCX807 is a selective and potent antagonist of the CXC chemokine receptor type 4 (CXCR4). It effectively inhibits CXCL12-mediated phosphorylation of ERK and Akt, leading to significant suppression of primary tumor growth. This compound is applicable for research in hepatocellular carcinoma, providing insights into its therapeutic potential in cancer treatment. -
GLP-1R Agonist
Pegloxenatide is a long-acting glucagon-like peptide-1 receptor (GLP-1R) agonist. It exhibits various biological activities, including the reduction of blood glucose and lipids, weight management, anti-inflammatory effects, and promotion of wound healing, as well as providing protective effects on liver and heart tissues. Pegloxenatide is primarily utilized in research focused on type 2 diabetes and its associated complications. -
S1PR Regulator
Mocravimod is a sphingosine-1-phosphate receptor (S1PR) modulator that inhibits the signaling necessary for T cell egress from lymph nodes and other lymphoid tissues. It preferentially binds to S1PR1, exhibiting beneficial effects such as a reduction in reactive oxygen species (ROS) levels, prevention of mitochondrial permeability transition pore opening, and enhancement of mitochondrial membrane potential (MMP). Additionally, Mocravimod promotes the phosphorylation of key signaling proteins including AKT, ERK, GSK-3β, JAK2, and STAT3, while preserving T cell effector function. This reagent is suitable for research into acute myelogenous leukemia, diabetes, and myocardial ischemia-reperfusion injury. -
CXCR4 Inhibitor
Hit 14 is a selective inhibitor of C-X-C chemokine receptor type 4 (CXCR4), demonstrating an IC50 value of 254 nM. This compound effectively inhibits the migration and invasion of MDA-MB-231 cells, highlighting its potential in cancer research. Furthermore, Hit 14 modulates Akt phosphorylation and exhibits anti-inflammatory properties, demonstrating efficacy in reducing ear swelling and damage in mouse models. Its diverse biological activities make it a valuable tool for studies related to cancer metastasis and inflammation. -
α/β-Adrenergic Agonist
Etilefrine is an α/β-adrenergic agonist primarily targeting α1 and β1 receptors. Its activity induces vasoconstriction by stimulating α1 receptors, leading to increased peripheral resistance, while β1 receptor activation enhances myocardial contractility and elevates heart rate, resulting in improved blood pressure and cardiac output. Additionally, Etilefrine modulates the AMPK/Akt signaling pathway, influencing phosphorylation levels. This compound is applicable in cardiovascular research, notably in studies related to postural hypotension, chylothorax, and conditions characterized by low cardiac output. -
Anticancer Agent
Auriculasin is an anticancer agent that primarily targets VEGFR2, PI3K/AKT/mTOR, and MAPK signaling pathways. It effectively inhibits cell proliferation, induces apoptosis, and suppresses angiogenesis, while also promoting mitochondrial oxidative stress and ferroptosis. Additionally, Auriculasin demonstrates activity at the cannabinoid receptor CB1 with an IC50 of 8.92 μM. This compound is valuable for cancer research, particularly in studying prostate cancer, non-small cell lung cancer, and the development of anti-angiogenic therapies. -
Indole Alkaloid
Tetrahydroalstonine is an indole alkaloid that acts as a selective antagonist of the α₂-adrenergic receptor. This compound demonstrates neuroprotective effects and has been shown to modulate autophagy-lysosomal function through the activation of the Akt/mTOR signaling pathway. Additionally, Tetrahydroalstonine significantly mitigates injury to primary cortical neurons induced by oxygen-glucose deprivation/reperfusion, making it a valuable tool for research into neuroprotection and cellular stress responses. -
α/β-Adrenergic Agonist
Etilefrine hydrochloride is an α/β-adrenergic agonist that selectively activates α1 and β1 adrenergic receptors. By stimulating α1 receptors, it induces vascular smooth muscle contraction, thereby increasing peripheral resistance and blood pressure. Additionally, activation of β1 receptors enhances myocardial contractility and heart rate, improving cardiac output. Etilefrine hydrochloride is valuable for cardiovascular research, particularly in studies related to postural hypotension, chylothorax, and the management of low cardiac output conditions. -
Bombesin Receptor Antagonist
Kuwanon G is a flavonoid compound that acts as an antagonist of the bombesin receptor. It demonstrates significant biological activities, including bactericidal, anti-tumor, anti-inflammatory, antioxidant, anti-atherosclerotic, and neuroprotective effects. Kuwanon G exhibits potent antibacterial activity against oral pathogens, particularly cariogenic and periodontal bacteria. Additionally, it induces apoptosis while inhibiting the proliferation, migration, and invasion of tumor cells, making it valuable for research in gastric cancer and atherosclerosis. -
Amino Acid Polypeptide Hormone Analogue
Sincalide ammonium is an amino acid polypeptide hormone analogue of cholecystokinin (CCK) that primarily targets gallbladder function. It is utilized in clinical settings for its ability to promote gallbladder contraction, thus facilitating the diagnosis of gallbladder and pancreatic disorders. By increasing bile secretion and causing the contraction of the gallbladder while relaxing the sphincter of Oddi, Sincalide ammonium aids in the efficient drainage of bile into the duodenum, making it a valuable tool in postevacuation cholecystography. -
Angiotensin Receptor Inhibitor
YS-49 monohydrate is a selective angiotensin receptor inhibitor, primarily targeting the angiotensin II pathway. This compound effectively reduces angiotensin II-stimulated proliferation of vascular smooth muscle cells by inducing heme oxygenase-1, offering potential therapeutic insights for cardiovascular research. Additionally, as an isoquinoline alkaloid, YS-49 demonstrates significant positive inotropic effects through the activation of cardiac β-adrenoceptors, making it a valuable reagent for studies involving cardiac function and vascular biology. -
CB1/P-gp Inhibitor
Voacamine is an indole alkaloid that acts as an antagonist of the cannabinoid receptor 1 (CB1) and also functions as a P-glycoprotein (P-gp) inhibitor. This compound enhances the efficacy of Doxorubicin by modulating P-gp activity, promoting apoptosis-independent autophagic cell death in human osteosarcoma cells. Additionally, Voacamine activates mitochondrial-associated apoptosis signaling pathways while inhibiting the PI3K/Akt/mTOR pathway, thus suppressing breast cancer progression. Moreover, it demonstrates oncogenic activity against colorectal cancer by inhibiting epidermal growth factor receptor (EGFR). -
S1P1 Agonist
SEW2871 is a potent and highly selective agonist of the sphingosine-1-phosphate type 1 receptor (S1P1), exhibiting an EC50 of 13.8 nM. This compound activates critical signaling pathways, including ERK, Akt, and Rac, and facilitates S1P1 internalization and recycling. SEW2871 effectively reduces lymphocyte populations in the bloodstream and shows promise for the study of various conditions, such as diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses. -
5-HT5A Antagonist
SB-699551 is a selective 5-HT5A receptor antagonist with a pKi of 8.2 nM, demonstrating significant brain penetrance. This compound exhibits high selectivity over various 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptors. By disrupting Gαi/o-coupled signaling and the PI3K/AKT/mTOR pathways, SB-699551 influences phosphorylation of key proteins such as CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 in breast tumor cells. It serves as a valuable tool in the study of anxiety, breast cancer, and Alzheimer's disease. -
Artificial Insulin
Insulin Detemir is an artificial insulin that regulates blood glucose levels by mimicking the effects of natural insulin. It activates the secretion of GLP-1 through enhanced expression of Gcg, utilizing signaling pathways involving Akt and extracellular signal-regulated kinase (ERK) alongside CREB. This reagent is primarily used in research related to type 2 diabetes, facilitating studies on glucose metabolism and insulin sensitivity. -
Dopamine β-hydroxylase Inhibitor
Fusaric acid is a potent dopamine β-hydroxylase inhibitor that reduces endogenous levels of norepinephrine and epinephrine in various tissues, including the brain, heart, spleen, and adrenal glands. By inducing oxidative stress and apoptosis, fusaric acid disrupts mitochondrial integrity and activates key apoptosis-related proteases such as Caspase-3/7, -8, and -9. Additionally, fusaric acid regulates pivotal apoptotic proteins, inhibits fibrosis-related signaling pathways including NF-κB and TGF-β1/SMADs, and mitigates collagen deposition. Its applications extend to myocardial fibrosis and cardiac hypertrophy research, as well as studies on esophageal and liver cancers. -
Stable Isotope
Theophylline-d3 is a deuterated form of theophylline, primarily used as a stable isotope in research applications. Theophylline functions as a potent phosphodiesterase inhibitor and adenosine receptor antagonist, contributing to its ability to relax airway smooth muscle. Additionally, it demonstrates anti-inflammatory effects by enhancing IL-10 production and inhibiting NF-κB nuclear translocation. This compound is valuable for studying asthma and chronic obstructive pulmonary disease (COPD) mechanisms and therapies. -
CB2 Agonists
MN-25 is an orally active indolpyridone that functions as a selective CB2 agonist, exhibiting a Ki of 245 nM for CB1 and a potent 11 nM for CB2. This compound demonstrates significant anti-inflammatory properties by inhibiting TNF-R release in human peripheral blood mononuclear cells in vitro, with an IC50 of 33 μM. In vivo studies have shown that MN-25 is effective in reducing acute inflammation in a mouse model at oral doses up to 50 mg/kg, making it a valuable reagent for exploring cannabinoid receptor biology and therapeutic applications in inflammation. -
Stable Isotope
Theophylline-13C2,d6 is a stable isotope-labeled form of Theophylline (1,3-Dimethylxanthine), primarily acting as a phosphodiesterase (PDE) inhibitor and adenosine receptor antagonist. This reagent enhances anti-inflammatory responses by increasing IL-10 levels and inhibiting NF-κB nuclear translocation, while also promoting apoptosis. It serves as a valuable tool for research into airway smooth muscle relaxation and the treatment of respiratory conditions such as asthma and chronic obstructive pulmonary disease (COPD). -
α-Adrenergic Receptor Agonist
Naphazoline is a potent α-adrenergic receptor agonist that exerts its biological activity through vasoconstriction and the reduction of vascular hyperpermeability. It effectively diminishes the levels of inflammatory mediators, including TNF-α, IL-1β, IL-6, IFN-γ, IL-4, as well as IgE, GMCSF, and NGF. Naphazoline is widely utilized in research related to non-bacterial conjunctivitis and other conditions involving inflammation and vascular function. -
IBAT Inhibitor
(S)-Elobixibat is a selective inhibitor of the intestinal bile acid transporter (IBAT). It effectively lowers LDL cholesterol levels, enhances serum levels of GLP-1, and promotes colonic motility, making it a valuable tool in metabolic syndrome research. This compound is utilized in studies related to constipation, dyslipidemia, non-alcoholic fatty liver disease, and liver tumors. -
CB2 Agonist
GW405833 hydrochloride is a selective agonist of the cannabinoid receptor 2 (CB2) with potent activity, characterized by EC50 and Ki values of 0.65 nM and 3.92 nM, respectively. In addition to its action as a CB2 agonist, GW405833 also acts as a non-competitive antagonist at the CB1 receptor, influencing analgesic pathways. This compound has been shown to significantly inhibit cAMP production stimulated by Forskolin and to down-regulate HIF-1α, which contributes to its potential role in alleviating acute liver failure. GW405833 hydrochloride is valuable for research related to pain management and metabolic disorders. -
α-Adrenergic Receptor Agonist
Naphazoline nitrate is an α-adrenergic receptor agonist that effectively induces vasoconstriction and reduces vascular hyperpermeability. It has been shown to lower the levels of inflammatory mediators such as TNF-α, IL-1β, IL-6, as well as cytokines including IFN-γ and IL-4. Naphazoline nitrate is utilized in research related to non-bacterial conjunctivitis, providing insight into its effects on inflammation and vascular response. -
CB2 Agonist
GW-405833 is a selective agonist of the cannabinoid receptor 2 (CB2), with an EC50 value of 0.65 nM. It exhibits a strong affinity for CB2, while displaying significantly lower activity at CB1, with EC50 and Ki values of 16.1 μM and 4772 nM, respectively. In addition to its agonistic effects at CB2, GW-405833 acts as a non-competitive antagonist at CB1, mediating analgesic and anti-inflammatory effects. Furthermore, it inhibits forskolin-stimulated cAMP production and down-regulates HIF-1α, potentially alleviating acute liver failure through modulation of glycolysis. This compound is useful for research in pain management, inflammation, and liver pathology. -
Dopamine D2/D3 Agonist
Piribedil is a potent and orally active agonist of dopamine D2 and D3 receptors, also exhibiting antagonistic activity at α2-adrenoceptors. Additionally, Piribedil inhibits MLL1 methyltransferase with an EC50 value of 0.18 μM. This compound is primarily utilized in research focused on Parkinson’s disease, circulatory disorders, and certain cancers, making it a valuable tool for exploring dopaminergic pathways and related therapeutic strategies. -
A2AAR/HDAC Dual Inhibitor
A2AAR/HDAC-IN-2 is a potent dual inhibitor targeting the adenosine A2A receptor (A2AAR) and histone deacetylase 1 (HDAC1). It demonstrates a strong binding affinity for A2AAR with a Ki value of 10.3 nM and exhibits significant inhibitory activity against HDAC1 with an IC50 of 18.5 nM. This compound is applicable in cancer research, particularly in studies exploring antitumor mechanisms and therapeutic efficacy. -
A2AAR/HDAC Inhibitor
A2AAR/HDAC-IN-1 is a potent dual inhibitor targeting the A2A adenosine receptor (A2AAR) and histone deacetylase 1 (HDAC1), with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. This compound demonstrates significant anticancer activity, making it a valuable reagent for research in cancer therapeutics and epigenetic modulation. Its oral bioavailability enhances its utility in in vivo studies, facilitating investigations into the mechanisms underlying tumor growth and proliferation. -
5-HT1B/1D Agonist
Zolmitriptan is a selective partial agonist of the 5-HT1B and 5-HT1D receptors, demonstrating high affinity with Ki values of 5.01 nM and 0.63 nM, respectively. It effectively crosses the blood-brain barrier, making it a valuable tool in migraine research. This compound is primarily utilized for studying the pathophysiology of migraines and developing targeted therapeutic interventions. -
5-HT3 Receptor Antagonist
Alosetron (Z)-2-butenedioate is a potent and selective antagonist of the serotonin 5-HT3 receptor. This compound is primarily utilized in research related to irritable bowel syndrome (IBS), demonstrating efficacy in blocking fast 5HT3-mediated depolarization in guinea pig myenteric and submucosal neurons, with an IC50 of approximately 55 nM. Additionally, Alosetron has been shown to reduce the visceral nociceptive response to rectal distension in both conscious and anesthetized canine models, indicating its potential for anti-inflammatory applications. -
Antiarrhythmic Agent
Dronedarone is a class III antiarrhythmic agent primarily targeting ion channels to manage atrial fibrillation (AF) and atrial flutter. It effectively inhibits multiple ion currents, including potassium, sodium, and L-type calcium currents, while also displaying antiadrenergic properties through noncompetitive binding to β-adrenergic receptors. Additionally, Dronedarone acts as a moderate inhibitor and substrate for CYP3A4, making it valuable for pharmacological studies in cardiac rhythm disorders. -
5-HT3 Antagonist
Palonosetron is a selective 5-HT3 antagonist that effectively prevents acute, delayed, and overall chemotherapy-induced nausea and vomiting. In addition to its primary application in oncology, Palonosetron demonstrates moderate activity against flaviviruses and exhibits potent antiviral effects against Zika virus in mammalian cells. Furthermore, this compound has been associated with antidepressant properties, making it a valuable tool for diverse research applications in both oncology and virology. -
5-HT3 Antagonist
Palonosetron hydrochloride is a selective 5-HT3 receptor antagonist that primarily functions to prevent acute and delayed nausea and vomiting associated with chemotherapy. Beyond its primary application, Palonosetron hydrochloride demonstrates moderate activity against flaviviruses, including potent efficacy against the Zika virus in mammalian cells. Additionally, this compound has been associated with antidepressant effects, expanding its potential therapeutic applications in neurological research. -
Anticholinergic Agent
Benztropine mesylate is a centrally acting anticholinergic agent that effectively crosses the blood-brain barrier. It primarily functions as a selective antagonist at human D2 dopamine receptors, exhibiting anti-histaminic properties and acting as a dopamine re-uptake inhibitor. This compound is particularly relevant for Parkinson's disease research, as well as in studies exploring its effects on cancer stem cells (CSCs). Researchers can utilize Benztropine mesylate to examine its potential therapeutic benefits in neurodegenerative and cancer treatment contexts. -
Histamine Receptor Modulator
Betahistine dihydrochloride is a potent histamine H1 receptor agonist and H3 receptor antagonist. This compound demonstrates significant biological activity in modulating histaminergic systems and is employed in research focused on conditions such as rheumatoid arthritis (RA). Its dual action makes it a valuable tool for investigating the pathways involved in inflammation and immune response. -
Antidepressant
Doxepin Hydrochloride is a tricyclic antidepressant that primarily functions as a selective antagonist of the histamine receptor H1. It effectively inhibits the reuptake of serotonin and norepinephrine, contributing to its antidepressant properties. Additionally, Doxepin exhibits significant activity as a CYP450 inhibitor, particularly affecting CYP450 2C19 and 1A2. This compound has demonstrated therapeutic potential in conditions such as atopic dermatitis and chronic urticaria, and it may enhance cognitive processes while providing neuroprotective effects against oxidative stress. -
Histamine 1 Receptor Blocker
Ketotifen fumarate is a noncompetitive antagonist of the histamine H1 receptor, functioning as a mast cell stabilizer. It exhibits significant biological activity by inhibiting 6-phosphogluconate dehydrogenase in vitro and demonstrates antiviral properties against SARS-CoV-2 and Influenza viruses. This compound is particularly useful in researching autoimmune encephalomyelitis (EAE) and in developing strategies for asthma attack prevention. -
Dopamine Receptor Antagonist
Levosulpiride is a selective antagonist of dopamine D2 receptors, classified as an atypical antipsychotic agent within the benzamide family. This compound is primarily used in the investigation of its effects on psychotic disorders and gastrointestinal conditions due to its ability to modulate dopaminergic activity. Researchers utilize Levosulpiride to study its therapeutic potential in conditions such as schizophrenia and to explore its impact on gastrointestinal motility. -
5-HT2C Receptor Agonist
CP-809101 hydrochloride is a highly selective agonist of the 5-HT2C receptor, exhibiting pEC50 values of 9.96 for the human 5-HT2C receptor, along with lower activity at 5-HT2B and 5-HT2A receptors. This compound has been shown to inhibit conditioned avoidance responses in rodent models and effectively antagonizes PCP- and d-amphetamine-induced hyperactivity. Additionally, CP-809101 hydrochloride demonstrates potential in reducing food and nicotine dependence, making it a valuable tool for research in psychopharmacology and addiction studies. -
Adrenergic Receptor Antagonist
Dibenamine is an alpha-adrenergic receptor antagonist that inhibits both basal and histamine-stimulated gastric acid secretion. Its primary pharmacological activity renders it useful in studying conditions characterized by excessive gastric acid production. Additionally, Dibenamine can be employed in research concerning adrenergic signaling pathways and their impact on gastric physiology. -
Histamine Receptor Antagonist
Doxylamine succinate is a first-generation antihistamine that acts as an H1 receptor antagonist. This compound exhibits key biological activity as an effective sedative and hypnotic agent, making it valuable in sleep disorder research. Additionally, it possesses local analgesic properties, providing potential applications in studies related to pain management and sleep regulation. -
Histamine H1 Receptor Antagonist
Epinastine hydrochloride is a selective histamine H1 receptor antagonist and mast cell stabilizer. It exhibits high affinity for neuronal octopamine receptors, with inhibitory constants of Ki = 2 nM in locusts and Ki = 1.1 nM in honeybees. This compound effectively inhibits inflammatory mediators such as TARC, IL-8, and IL-4, and enhances anti-colon cancer immunity while reducing scratching behavior and vascular permeability induced by Substance P. Epinastine hydrochloride is valuable for research in allergic diseases and related inflammatory conditions. -
Antihistamine Agent
Hydroxyzine dihydrochloride is an antihistamine agent that primarily functions as a histamine H1-receptor antagonist and serotonin antagonist. It exhibits anxiolytic properties, making it a valuable tool for research into generalized anxiety disorder and related conditions. This compound can also be utilized in studies involving sedation and allergic reactions due to its diverse pharmacological effects. -
Histamine Receptor Inhibitor
Levodropropizine is a selective histamine receptor inhibitor primarily used as a peripheral antitussive agent. Its mechanism of action involves the suppression of cough reflexes through its interaction with histamine receptors, making it effective in treating cough associated with colds and allergies. Levodropropizine is noted for its good tolerance profile, facilitating its use in various research applications focused on respiratory physiology and pharmacology. -
5-HT Receptor Modulator
Lurasidone Hydrochloride is a potent antagonist of both dopamine D2 and 5-HT7 receptors, exhibiting IC50 values of 1.68 nM and 0.495 nM, respectively. Additionally, it acts as a partial agonist at the 5-HT1A receptor with an IC50 of 6.75 nM. This compound is utilized in research focused on neuropharmacology and the treatment of psychiatric disorders, such as schizophrenia and bipolar disorder. Its selective modulation of serotonin and dopamine receptors makes it a valuable tool for investigating neurochemical pathways and therapeutic interventions. -
5-HT(1B/1D) Receptor Agonist
Naratriptan hydrochloride is a selective agonist for the 5-HT1B and 5-HT1D receptors. It effectively induces vasoconstriction of cranial arteries through these receptor pathways, demonstrating an EC50 value of 0.11 μM in dog basilar artery models. Additionally, Naratriptan hydrochloride exhibits the ability to inhibit trigeminal nerve-mediated dural neurogenic plasma extravasation and mitigate sterile inflammation. This compound is primarily utilized in research focused on acute migraine, particularly in the investigation of cranial vascular and neuroinflammatory mechanisms. -
Histamine H1 Antagonist
Pemirolast potassium is a histamine H1 antagonist with antiallergic properties. It effectively mitigates hypersensitivity reactions associated with Paclitaxel and demonstrates potential applications in studies related to bronchial asthma and conjunctivitis. This compound is valuable for researchers focusing on allergic responses and treatment mechanisms in respiratory and ocular conditions. -
Dopamine Receptors Blocker
Trifluoperazine dihydrochloride is a dopamine receptor antagonist, primarily used in the study of schizophrenia. This compound demonstrates significant activity as an α1-adrenergic receptor blocker and acts as a potent inhibitor of NUPR1, exhibiting anticancer properties. Additionally, it functions as a calmodulin inhibitor and has been shown to inhibit P-glycoprotein, impacting multidrug resistance. Trifluoperazine dihydrochloride is also recognized for its reversible inhibition of influenza virus morphogenesis, making it valuable for various research applications in neuropharmacology and virology. -
5-HT3 Receptor Antagonist
VUF10166 is a potent 5-HT3 receptor antagonist, exhibiting high affinity with Ki values of 0.04 nM for the 5-HT3A subtype and 22 nM for the 5-HT3AB subtype. This compound effectively inhibits 5-HT-induced responses at these receptors at nanomolar concentrations. Additionally, at elevated concentrations, VUF10166 demonstrates partial agonistic activity at the 5-HT3 receptor, with an EC50 of 5.2 μM. Its unique pharmacological profile makes it a valuable tool for research in neurobiology and gastrointestinal pharmacology. -
5-HT3 Receptor Antagonist
Ramosetron Hydrochloride is a potent 5-HT3 receptor antagonist. It exhibits key biological activity in alleviating symptoms of dysphoria, activity interference, and food avoidance. This compound shows promise for research applications targeting irritable bowel syndrome with diarrhea, making it a valuable tool for studies in gastrointestinal disorders.
