Catalog No.
Product Name
Application
Product Information
Citations
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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. -
H3 Agonist
(R)-(-)-α-Methylhistamine dihydrobromide is a potent and selective agonist of the H3 histamine receptor, exhibiting a Kd of 50.3 nM. This compound has been shown to enhance memory retention and alleviate memory impairment in rat models, making it a valuable tool for research on cognitive function and neuropharmacology. Its ability to penetrate the blood-brain barrier further establishes its utility in neurological studies. -
H1/ H2 Agonist
HTMT dimaleate is a potent agonist of histamine H1 and H2 receptors. It exhibits significantly enhanced activity, being 40,000 times more effective than histamine in mediating H2 receptor effects in natural suppressor cells. This compound is valuable for research focused on immunological responses and histamine receptor signaling pathways. -
Histamine H2 Receptor Antagonist
BMY-25368 hydrochloride is a potent antagonist of the histamine H2 receptor, functioning primarily as a gastric acid secretion inhibitor. By competitively inhibiting gastric secretion stimulated by histamine, it also effectively antagonizes secretion induced by Pentagastrin, Bethanechol, and food intake. This reagent is applicable in research focused on understanding gastric physiology and the modulation of acid secretion. -
Histamine Dehydrogenase
Histamine dehydrogenase, Microorganism (EC 1.4.99) is a homodimeric enzyme that facilitates the oxidative deamination of histamine in conjunction with an electron carrier. This enzyme plays a crucial role in histamine metabolism and its regulation within biological systems. It is applicable in studies related to neurotransmission, immune response, and the mechanisms underlying allergic reactions. Researchers may utilize this enzyme to explore its potential roles in various physiological and pathological processes involving histamine. -
H1 Receptor Antagonist
Dimethindene is a selective histamine H1 receptor antagonist known for its ability to inhibit histamine-mediated processes. This compound has been shown to impair cutaneous wound healing through its antagonistic action. Additionally, Dimethindene is capable of blocking potassium (K+) currents, making it valuable for research applications focused on skin physiology and ion channel modulation. -
Histamine 1 Antagonist
Azelastine is a potent and selective antagonist of the histamine H1 receptor. It demonstrates significant antihistaminic activity, making it valuable for research into allergic rhinitis and asthma. Additionally, Azelastine has potential applications in studying diabetic hyperlipidemia and SARS-CoV-2-related pathophysiology. -
Histamine H2 Receptor Antagonist
Aminopotentidine is a potent antagonist of the histamine H2 receptor, exhibiting KB values of 220 nM for human H2 receptors and 280 nM for guinea pig H2 receptors. This compound is utilized in studying gastric acid secretion and has applications in gastrointestinal research. Additionally, it serves as a valuable precursor for the synthesis of [125I] iodo derivatives, facilitating radiolabeling studies. -
Stable Isotope
(Rac)-Levomepromazine-d3 hydrochloride is a labeled form of the racemic compound Methotrimeprazine, belonging to the phenothiazine class. This reagent exhibits antagonist activity at various neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin, and histamine receptors. It is primarily used as a stable isotope for research applications, enabling in-depth studies of pharmacological interactions and the metabolic pathways of related compounds. -
Histamine Receptor Agonist
LML134 is a highly selective inverse agonist of the Histamine 3 receptor (H3R), demonstrating an impressive affinity with Ki values of 0.3 nM for hH3R cAMP and 12 nM for hH3R binding. This compound exhibits rapid brain penetration, resulting in significant H3R occupancy and a swift disengagement from its target. LML134 holds promise for investigating therapeutic strategies for sleep disorders by modulating histaminergic signaling pathways. -
Antihistamine Agent
Brompheniramine is a selective histamine H1 receptor antagonist primarily utilized as an antihistamine agent. With a Kd of 6.06 nM, it effectively alleviates symptoms of allergic rhinitis. In addition to its antihistaminic properties, brompheniramine exhibits anticholinergic, antidepressant, and anesthetic effects, making it suitable for various research applications related to allergy and inflammation. The compound also interacts with hERG, calcium, and sodium channels, with IC50 values of 0.90 μM, 16.12 μM, and 21.26 μM, respectively. -
Histamine H1 Antagonist
Triprolidine hydrochloride is a potent histamine H1 antagonist that effectively alleviates symptoms associated with allergic conditions. It exhibits properties that provide spinal cord motor and sensory blockade, making it valuable for research applications in allergic rhinitis and other histamine-mediated disorders. This compound facilitates the study of antihistamine effects and their underlying mechanisms in various biological contexts. -
Histamine H4 Receptor Agonist
ST-1006 is a potent agonist of the histamine H4 receptor, characterized by a pKi value of 7.94. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for research into inflammatory processes and related diseases. Its potential applications include studies in immunology and the modulation of allergic responses, providing insights into therapeutic strategies targeting the H4 receptor pathway. -
Histamine H1-Receptor Blocker
Oxomemazine is a phenothiazine-derived antagonist targeting the histamine H1 receptor. It exhibits notable antihistamine and anticholinergic properties, making it useful in research related to cough treatments. Additionally, Oxomemazine demonstrates a selective blockade of the muscarinic M1 receptor with a significant affinity difference compared to the M2 receptor. Studies have shown its protective effects against anaphylactic microshock in guinea pigs, highlighting its potential for further pharmacological investigation. -
H1 Receptor Antagonist
Cetirizine Impurity C dihydrochloride is an impurity of cetirizine, which acts as a selective H1 receptor antagonist. This compound demonstrates significant inhibition of histamine activity, contributing to its use in studies of allergic responses and histamine-mediated disorders. Its characterization is essential for ensuring the purity and efficacy of cetirizine in pharmaceutical formulations and research applications. -
Sigma Receptor Agonist
CB-64D is a dual agonist of sigma receptor 1 and sigma receptor 2, exhibiting Ki values of 16.5 nM and 3063 nM, respectively. It has been shown to induce apoptosis in SK-N-SH cancer cells, highlighting its potential role in cancer research. This compound can serve as a valuable tool for investigating the biological functions of sigma receptors and their implications in various pathologies. -
Stable Isotope
Perphenazine-d6 fumarate is a deuterated derivative of Perphenazine, primarily acting as a dopamine D2 and D3 receptor antagonist with Ki values of 0.56 nM and 0.43 nM, respectively. Additionally, it demonstrates affinity for the 5-HT2A and Alpha-1A adrenergic receptors. This compound exhibits notable biological activities, including the inhibition of cancer cell proliferation and the induction of apoptosis. Perphenazine-d6 fumarate is useful in research addressing mental health disorders, cancer mechanisms, and inflammatory processes. -
Dopamine Receptor Antagonist
Perphenazine dihydrochloride is a potent antagonist of dopamine receptors, primarily targeting D2 and D3 subtypes, with Ki values of 0.56 nM and 0.43 nM, respectively. Additionally, it exhibits activity against 5-HT2A and α1A adrenergic receptors. This compound demonstrates significant biological activity by inhibiting cancer cell proliferation and inducing apoptosis. Perphenazine dihydrochloride is particularly useful in research focused on mental disorders, oncology, and inflammatory processes. -
CB2R Agonist
CB2R agonist 4 is a selective agonist for the cannabinoid receptor 2 (CB2R), exhibiting an EC50 value of 6.9 μM. This compound can induce cellular apoptosis, promote reactive oxygen species (ROS) production, and contribute to protein misfolding. Due to its cytotoxic effects observed in various tumor cell lines, CB2R agonist 4 is a valuable tool for cancer research applications. -
Stable Isotope
D-Mannitol-d is a deuterium-labeled form of D-Mannitol, a polyol with significant applications in both food and pharmaceutical research. It functions primarily as an osmotic diuretic, utilized to alleviate tissue edema, while also promoting the absorption of calcium and magnesium through cecal fermentation. Additionally, D-Mannitol-d is instrumental in studies related to metabolic processes, including the induction of brown fat formation via β3-adrenergic receptor activation, potentially contributing to improved insulin sensitivity and reduced blood glucose levels. Its unique properties make it valuable for maintaining osmotic pressure in plant cell cultures, particularly when cellular integrity is compromised. -
Verapamil Enantiomer
(R)-Verapamil is an enantiomer of the calcium channel blocker Verapamil, primarily acting on sodium channels with an IC50 of 3.19 μM. It exhibits agonistic activity on somatostatin receptor 2 (SSTR2), with an EC50 of 1.3 μM. In preclinical studies, (R)-Verapamil has demonstrated the ability to downregulate TXNIP protein expression and inhibit β-cell apoptosis in diabetic mouse models, contributing to effective blood glucose control. Additionally, it can be utilized as a PET tracer to assess P-glycoprotein function, making it a valuable tool in metabolic and pharmacological research. -
CXCR-4 Inhibitor
SSB-2548 is a selective inhibitor of the chemokine receptor CXCR-4. It has demonstrated significant efficacy in inhibiting the proliferation and migration of acute myeloid leukemia cells, while also promoting apoptosis. Its favorable gastrointestinal absorption profile makes SSB-2548 a valuable tool for investigating the underlying mechanisms of leukemia and exploring potential therapeutic interventions. -
α-1A Adrenergic Receptor Agonist
Dabuzalgron hydrochloride is a selective agonist of the α-1A adrenergic receptor, primarily indicated for the management of urinary incontinence. This compound has demonstrated protective effects against Doxorubicin-induced cardiotoxicity by maintaining mitochondrial integrity and function. Its pharmacological properties make it a valuable tool in research focused on adrenergic signaling and cardiac health. -
5-HT2/D1/D2 Antagonist
Olanzapine hydrochloride is a selective antagonist of serotonin receptors (5-HT2A/2C, 5-HT3) and dopamine receptors (D1, D2). It exhibits high affinity binding to various targets, including H1, muscarinic M1-5, and adrenergic α1 receptors, contributing to its pharmacological profile. This atypical antipsychotic is primarily used in research focusing on neuropharmacology, the treatment of schizophrenia, and mood disorders, providing valuable insights into the modulation of neurotransmitter systems. -
Platelet Aggregation Inhibitor
2'-Hydroxyflavanone is a flavanone that functions as a platelet aggregation inhibitor. It demonstrates significant bioactivity by inhibiting platelet aggregation induced by arachidonic acid and adenosine diphosphate, with IC50 values of 47.8 μM and 147.2 μM, respectively. Additionally, 2'-hydroxyflavanone has been implicated in inhibiting cancer cell proliferation and inducing apoptosis, making it valuable for research in cancer and inflammatory pathways. -
S1P2 Receptor Antagonist
AB1 is a highly selective antagonist of the sphingosine-1-phosphate receptor 2 (S1P2) with an IC50 of 3.5 nM. It effectively inhibits S1P signaling pathways, leading to the suppression of tumor cell migration, angiogenesis, and the expression of the profibrotic mediator CTGF, while promoting apoptosis in cancer cells. This compound demonstrates significant potential for research focused on solid tumors and their microenvironment. -
Stable Isotope
Adenosine-d-1 is a deuterium-labeled derivative of adenosine, an endogenous autacoid that interacts with four G protein-coupled receptors: A1, A2A, A2B, and A3. This stable isotope serves as a valuable tool for studying adenosine's diverse biological functions and its role in various physiological and pathological processes. Applications include pharmacological research, metabolic studies, and the investigation of signal transduction pathways mediated by adenosine receptors. -
Somatostatin Receptor Agonist
Octreotide pamoate is a synthetic octapeptide and a somatostatin receptor agonist that primarily targets subtypes 2, 3, and 5. It enhances Gi protein activity, leading to a reduction in intracellular cAMP levels. Octreotide pamoate exhibits antitumor activity and induces apoptosis, making it valuable for research in conditions such as acromegaly and other diseases related to somatostatin signaling. Its unique pharmacological profile allows for exploration in various therapeutic applications and biological studies. -
Antitumor Somatostatin Analogue
TT-232 TFA is a somatostatin analogue that primarily targets antitumor activity. It has been shown to effectively induce apoptosis in pancreatic tumor cell lines while simultaneously inhibiting tyrosine kinase activity and stimulating tyrosine phosphatase activity in colon tumor cell lines. TT-232 TFA demonstrates strong anti-tumor effects by inhibiting tumor cell proliferation and promoting apoptosis. This compound is valuable for the development of anti-tumor therapeutics and for investigating the mechanisms of apoptosis. -
PAF Antagonist
Pinusolide is a potent antagonist of the platelet-activating factor (PAF) receptor, critically involved in inflammatory responses and cancer progression. This compound has been shown to inhibit tumor cell proliferation and to induce apoptosis, making it a valuable tool in cancer research. Pinusolide's unique mechanism of action provides insights into PAF-related signaling pathways and potential therapeutic strategies. -
Histamine H1 Receptor Antagonist
Meclizine-d8 is a deuterated derivative of Meclizine, functioning primarily as a histamine H1 receptor antagonist. This compound exhibits significant efficacy in alleviating nausea and preventing motion sickness. Additionally, Meclizine serves as an agonist for the mouse constitutive androstane receptor (CAR) while acting as an inverse agonist for the human CAR, making it relevant for studies on receptor modulation and signaling pathways in pharmacology. -
mGluR5 Antagonist
Fenobam hydrate is a selective mGluR5 antagonist with an IC50 of 84 nM, capable of crossing the blood-brain barrier. It exhibits Kd values of 54 nM and 31 nM for rat and human recombinant mGlu5 receptors, respectively. Fenobam hydrate demonstrates anxiolytic properties, inhibits self-administration behavior in rodent models, and induces apoptosis in cancer cells. This compound is valuable for research in neurological disorders, cancer biology, and addiction studies. -
Stable Isotope
D-Mannitol-d2 is a deuterium-labeled derivative of D-Mannitol, primarily used as a stable isotope in various research applications. D-Mannitol is an osmotic diuretic with significant biological activity, promoting calcium and magnesium absorption while reducing tissue edema. Additionally, it has been shown to enhance brown adipocyte formation and improve insulin sensitivity by activating the β3-adrenergic receptor pathway, leading to the conversion of white fat cells into brown fat. This compound is particularly useful in studies involving osmotic pressure regulation and cellular protection in plant and mammalian cell cultures. -
Dopamine D4 Receptor Antagonist
L 741742 is a highly selective antagonist of the dopamine D4 receptor, exhibiting a Ki of 3.5 nM for this target and demonstrating significantly lower affinity for the D2 and D3 receptors. This compound effectively suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, disrupts lysosomal function, and impairs autophagic flux. L 741742 induces G0/G1 cell-cycle arrest and apoptosis, enhances neuronal differentiation in human neural stem cells, and selectively targets the growth of glioblastoma neural stem cells. Its potential therapeutic applications include research in schizophrenia and glioblastoma, with demonstrated synergy when combined with Temozolomide in vitro. -
5-HT Receptor Modulator
1-(1-Naphthyl)piperazine hydrochloride is a potent modulator of the 5-HT receptor system, functioning as an agonist at the 5-HT1A receptor while antagonizing the 5-HT2A receptor. This compound has demonstrated significant biological activity by inducing apoptosis in various cell types. Additionally, it exhibits potential in combatting immunosuppression and preventing photocarcinogenesis, making it a valuable tool for research in neuroscience and cancer studies. -
PAR-1 Antagonist
Atopaxar hydrochloride is a selective and reversible antagonist of protease-activated receptor-1 (PAR-1) that functions primarily as a thrombin receptor inhibitor. This compound demonstrates significant biological activity by inhibiting Janus kinase 1 (JAK1) and JAK2, resulting in JAK-STAT pathway inhibition with an EC50 of 5.90 μM in A549 cells. It has been shown to decrease cell viability (IC50=7.02 μM), induce apoptosis, and arrest the cell cycle at the G1 phase. Atopaxar hydrochloride is valuable in research focused on atherothrombotic diseases and exhibits both antiplatelet and antitumor properties. -
Noradrenergic Reuptake Inhibitor
Maprotiline is a selective noradrenergic reuptake inhibitor that exhibits significant antidepressant activity and also shows promise in antitumor and neuropathic pain relief. It facilitates cancer cell apoptosis through modulation of the ERK signaling pathway and interaction with cellular retinoic acid-binding protein 1 (CRABP1). This compound is valuable for research in mental health disorders, oncology, and pain management. -
5-HT Receptor Modulator
1-(1-Naphthyl)piperazine is a modulator of the 5-HT receptors, functioning as an antagonist at the 5-HT2A receptor and an agonist at the 5-HT1A receptor. It demonstrates a binding affinity for the human 5-HT6 receptor with a Ki value of 120 nM. Additionally, 1-(1-Naphthyl)piperazine has been shown to inhibit forskolin-stimulated adenylate cyclase activity in calf substantia nigra, and it mitigates UV-induced immunosuppression. This compound induces S-phase cell cycle delay and apoptosis while elevating ROS levels, ultimately leading to the inhibition of MNT-1 cell proliferation, making it a valuable tool for melanoma research. -
Dopamine Receptor Antagonist
Flupentixol is an orally active antagonist of D1 and D2 dopamine receptors. This compound exhibits anti-proliferative effects on cancer cells, promoting apoptosis, and has potential applications in the study of schizophrenia, anxiety, and depression. Additionally, Flupentixol has been identified as a new inhibitor of PI3Kα, with an IC50 value of 127 nM, making it a valuable reagent for research in neuropsychiatric disorders and cancer biology. -
Stable Isotope
D-Mannitol-13C,d2 is a stable isotope-labeled form of D-Mannitol, which serves as an osmotic diuretic and explores its role in cellular osmoregulation. D-Mannitol is utilized in various research applications, including the study of calcium and magnesium absorption, as well as promoting brown adipose tissue formation through the activation of β3-adrenergic receptors. It is also valuable in plant cell culture, helping maintain osmotic balance and protecting cells, particularly when cell walls are compromised. This reagent is essential for researchers investigating metabolic pathways, therapeutic interventions, and plant physiology.
