Catalog No.
Product Name
Application
Product Information
Citations
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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. -
A2A Receptor/HDAC Inhibitor
IHCH-3064 is a dual-target compound that inhibits the Adenosine A2A Receptor and histone deacetylase (HDAC). It demonstrates potent binding affinity for the A2A receptor (Ki = 2.2 nM) and selectively inhibits HDAC1 with an IC50 of 80.2 nM. This compound exhibits significant antiproliferative activity against various tumor cell lines in vitro, making it a valuable tool for tumor immunotherapy research applications. -
Dopamine D2/D3 Agonist
Piribedil maleate is a potent agonist of dopamine D2 and D3 receptors, with additional activity as an α2-adrenoceptor antagonist. It has been shown to inhibit MLL1 methyltransferase activity with an EC50 of 0.18 μM. Piribedil maleate is of interest for research applications related to Parkinson’s disease, circulatory disorders, and various cancers. -
Dopamine D2/D3 Agonist
Piribedil hydrochloride is a potent agonist of dopamine D2 and D3 receptors, serving as a valuable tool for investigating dopaminergic signaling pathways. In addition to its agonistic activity, it acts as an antagonist at α2-adrenoceptors and inhibits MLL1 methyltransferase with an EC50 of 0.18 μM. This compound is primarily utilized in research related to Parkinson's disease, circulatory disorders, and certain types of cancer, making it an important reagent for studies focused on neurodegeneration and tumor biology. -
Dopamine D2/D3 Agonist
Piribedil dihydrochloride is a potent dopamine D2 and D3 agonist, also functioning as an antagonist at α2-adrenoceptors. This compound exhibits inhibitory activity on MLL1 methyltransferase with an EC50 of 0.18 μM. It is primarily utilized in research focused on Parkinson's disease, circulatory disorders, and various types of cancers. -
Histamine N-Methyltransferase Inhibitor
SKF 91488 dihydrochloride is a potent, noncompetitive inhibitor of histamine N-methyltransferase, exhibiting a Ki value of 0.9 μM. This compound effectively blocks the metabolism of histamine, leading to elevated concentrations of histamine in biological systems. SKF 91488 dihydrochloride plays a significant role in research focusing on infection, inflammation, and cardiovascular diseases, including studies on Mycoplasma pneumonia and hemorrhagic hypotension. Its influence on blood pressure and bronchoconstriction further underscores its utility in exploring related pathophysiological mechanisms. -
Stable Isotope
Dopamine-d5 hydrochloride is a deuterium-labeled analogue of dopamine, a catecholamine neurotransmitter primarily synthesized in the substantia nigra, ventral tegmental area, and hypothalamus. This compound retains the essential biological functions of dopamine, including its interaction with D2 dopamine receptors, which mediates the endocytosis of VEGFR2, a key process in angiogenesis. Dopamine-d5 hydrochloride is valuable for research applications involving neurotransmitter dynamics, neuropharmacology, and angiogenic pathways. -
Antipsychotic Agent
Penfluridol is a potent, long-acting antipsychotic agent that primarily targets D2-like dopamine receptors. It exhibits significant anti-inflammatory properties by inhibiting TNFα-induced NF-κB activation and demonstrates efficacy in models of arthritis and colitis. Additionally, Penfluridol acts as a Ca2+-calmodulin inhibitor, inducing apoptosis and autophagy in various cellular contexts. This compound is utilized in research focusing on chronic schizophrenia, acute psychosis, Tourette syndrome, autoimmune diseases, and it also shows antibacterial activity against E. faecalis with a minimum inhibitory concentration of 7.81 μg/ml. -
Dopamine Receptor Antagonist
Perphenazine is a potent dopamine receptor antagonist, specifically targeting D2 and D3 receptors with Ki values of 0.56 nM and 0.43 nM, respectively, while also interacting with the 5-HT2A receptor and the Alpha-1A adrenergic receptor. This compound demonstrates inhibitory effects on cancer cell proliferation and promotes apoptosis. Perphenazine is valuable for research into psychiatric disorders, cancer biology, and inflammatory processes. -
H1 Receptor Antagonist
Pheniramine maleate is a first-generation histamine H1 receptor antagonist that primarily targets the central nervous system to produce sedative and hypnotic effects. In addition to its antihistaminic activity, Pheniramine maleate exhibits antitumor properties by inducing apoptosis in leukemia cells. It also demonstrates effectiveness as a local agent to alleviate pain and provide antipruritic effects in various applications. -
5-HT4 Agonist
Prucalopride succinate is a selective 5-HT4 receptor agonist known for its high affinity for human 5-HT4a and 4b receptors, with pKis of 8.6 and 8.1, respectively. This compound enhances intestinal motility and promotes regeneration of the enteric nervous system, making it relevant for research in chronic constipation and pseudo-intestinal obstruction. Additionally, Prucalopride succinate exhibits anticancer properties by inhibiting the PI3K/AKT/mTOR signaling pathway, thereby facilitating its application in cancer studies. -
Antibiotic
Adenoregulin, also known as Dermaseptin b2, is an antimicrobial peptide antibiotic that targets a broad spectrum of microorganisms. It exhibits activity against both Gram-negative and Gram-positive bacteria, as well as yeast and fungi. Additionally, Adenoregulin enhances the binding of agonists to the A1 adenosine receptor, making it valuable for research applications in microbiology and pharmacology. -
CXCR Inhibitor
Corydalmine, a CXCR inhibitor, demonstrates significant antifungal activity by inhibiting spore germination in various plant pathogenic and saprophytic fungi. Additionally, it serves as an oral analgesic agent, exhibiting potent analgesic effects. Corydalmine has been shown to alleviate Vincristine-induced neuropathic pain in murine models through the inhibition of the NF-κB-dependent CXCL1/CXCR2 signaling pathway, making it a valuable tool for pain research and therapeutic applications. -
CXCR Inhibitor
Corydalmine hydrochloride is a potent CXCR inhibitor that demonstrates significant biological activity by inhibiting spore germination in certain plant pathogenic and saprophytic fungi. Additionally, it exhibits notable analgesic properties, effectively alleviating Vincristine-induced neuropathic pain in murine models. This effect is mediated through the inhibition of the NF-κB-dependent CXCL1/CXCR2 signaling pathway, highlighting its potential applications in pain management research and fungal inhibition studies. -
Stable Isotope
Anandamide-d8 is a deuterated form of the endocannabinoid Anandamide, primarily known for its interaction with cannabinoid receptors CB1 and CB2. This compound modulates various neuronal and immune functions and can also engage additional receptors, including PPARs, TRPV1, and GPR18/GPR55. Anandamide-d8 exhibits potential anti-fungal and anti-inflammatory properties, making it valuable for research applications in fields such as neurodegenerative diseases, including Alzheimer's disease, and inflammatory conditions like ulcerative colitis. -
PARP-1 Inhibitor
Benzo[c][1,8]naphthyridin-6(5H)-one is a potent inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1) and aurora kinase A, exhibiting IC50 values of 0.311 μM and 5.5 μM, respectively. This compound demonstrates low micromolar affinity for human adenosine receptors AR A1 and hA2A, with Ki values of 4.6 and 4.8 μM. Due to its mechanistic action, Benzo[c][1,8]naphthyridin-6(5H)-one is valuable for research applications targeting DNA repair pathways and cancer therapies. -
Histamine H2-Receptor Antagonist
Ranitidine hydrochloride is a selective histamine H2-receptor antagonist that effectively inhibits gastric secretion. It demonstrates significant antagonism of histamine-induced cardiac and uterine responses in isolated animal models, with pA2 values of 7.2 and 6.95, respectively. Additionally, ranitidine hydrochloride has been shown to inhibit the development and metastasis of breast tumors in murine models, indicating its potential utility in cancer research. -
5-HT1 Agonist
Rizatriptan benzoate is a selective agonist of the 5-HT1B and 5-HT1D serotonin receptors. It exhibits vasoconstrictive properties that affect peripheral blood flow and effectively penetrates the blood-brain barrier, thereby inhibiting pain neurotransmission within the central nervous system. This compound is primarily utilized in research focused on migraine pathophysiology and the modulation of serotonergic signaling. -
5-HT1 Receptor Agonist
Sumatriptan succinate is a selective agonist for the 5-HT1 receptor subtype, notably demonstrating IC50 values of 7.3 nM, 9.3 nM, and 17.8 nM for the 5-HT1D, 5-HT1B, and 5-HT1F receptors, respectively. This compound is primarily utilized in the study of migraine pathophysiology and therapeutics, providing insights into serotonin modulation during migraine attacks. Its pharmacological profile makes it an essential reagent for research investigating the efficacy of triptans in headache relief. -
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. -
PDE3/PDE4/PDE5/HRH1 Inhibitor
Fenspiride hydrochloride is a non-steroidal anti-inflammatory agent and an antagonist of the H1-histamine receptor. It selectively inhibits phosphodiesterase activities, including PDE3, PDE4, and PDE5, with -log IC50 values of 3.44, 4.16, and approximately 3.8, respectively. This compound is valuable for research applications focused on respiratory diseases, highlighting its potential in therapeutic investigations and the modulation of inflammatory responses. -
Histamine Receptor Antagonist
Mepyramine maleate is a potent antagonist of the histamine H1 receptor, exhibiting a Kd of 0.8 nM for H1, alongside Kd values of 5200 nM and >3000 nM for H2 and H3 receptors, respectively. With a pKd value of 9.4 for the H1 receptor, this first-generation antihistamine is valuable for studies focused on allergic responses and the role of histamine in various physiological processes. It is widely used in pharmacological research to explore histamine-mediated signaling and potential therapeutic applications in allergy and inflammation. -
5-HT Receptor Antagonist
Trimipramine maleate is a selective 5-HT receptor antagonist that effectively crosses the blood-brain barrier. It demonstrates significant binding affinity with pKi values of 6.39, 8.10, and 4.66 for the 5-HT1C, 5-HT2, and 5-HT1A receptors, respectively. Additionally, Trimipramine maleate acts as an inhibitor of human noradrenaline transporter (hNAT), serotonin transporter (hSERT), and organic cation transporters (hOCT1, hOCT2), with IC50 values of 4.99 μM, 2.11 μM, and 3.72 μM, and 8.00 μM, respectively. Its unique pharmacological profile also indicates potential applications in vascular activity and anxiety treatment research.
