Catalog No.
Product Name
Application
Product Information
Citations
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CXCR4 Antagonist
Burixafor hydrobromide is a potent CXCR4 antagonist with a pIC50 of 7.4, effectively inhibiting the binding of CXCL12 to the CXCR4 receptor. This compound antagonizes CXCL12-induced recruitment of Gαᵢ and β-arrestin2, thereby obstructing the downstream Gαᵢ-mediated inhibition of cAMP signaling. Burixafor hydrobromide is utilized in research for mobilizing CD34+ hematopoietic stem/progenitor cells from the bone marrow to peripheral blood, making it valuable in studies related to autologous hematopoietic stem cell transplantation. -
hD4 Receptor Antagonist
L 741742 hydrochloride is a highly selective antagonist of the human D4 dopamine receptor, exhibiting a Ki value of 3.5 nM for the D4 receptor while demonstrating much lower affinity for D3 and D2 receptors. This compound disrupts signaling pathways associated with PDGFRβ, ERK1/2, and mTOR, and impairs autophagic processes by affecting lysosomal function. Biologically, it induces G0/G1 cell-cycle arrest and apoptosis in various cell types and promotes neuronal differentiation in human neural stem cells. L 741742 hydrochloride is particularly relevant for research on schizophrenia and glioblastoma, demonstrating efficacy against glioblastoma neural stem cells and enhancing the effects of Temozolomide in vitro. -
mGluR2 Negative Allosteric Modulator
mG2N001 is a negative allosteric modulator of the metabotropic glutamate receptor mGluR2, exhibiting an IC50 of 93 nM and a binding affinity (Ki) of 63 nM. This compound demonstrates significant biological activity by modulating glutamatergic signaling pathways, making it valuable for neurological research. Additionally, its radioisotope [11C]mG2N001 is suitable for PET imaging, providing high brain heterogeneity and penetration, allowing for selective accumulation in mGluR2-rich regions, which enhances imaging contrast in neurobiological studies. -
mGluR5 Antagonist
AZD-2066 hydrochloride is a selective antagonist of the metabotropic glutamate receptor 5 (mGluR5) with the ability to penetrate the blood-brain barrier. This compound activates the brain-derived neurotrophic factor (BDNF) and trkB signaling pathway, making it relevant for research into neuropathic pain, major depressive disorder, and gastroesophageal reflux disease. AZD-2066 hydrochloride serves as a valuable tool for investigating the therapeutic potential of mGluR5 modulation in these conditions. -
H1 Receptor Blocker
(R)-(+)-Dimethindene maleate is a selective H1 receptor antagonist, displaying significant antihistaminic activity. It is utilized in research to study allergic responses and histamine-mediated mechanisms in various biological models, including porcine studies. This compound serves as a valuable tool for exploring the effects of histamine signaling and the therapeutic potential of H1 receptor blockade. -
βH Inhibitor AND H1 Receptor Antagonist
Desmethylastemizole is a β-hematin (βH) inhibitor and a Histamine H1 receptor antagonist. It exhibits potent antiplasmodium activity against Plasmodium falciparum, with IC50 values of 0.12, 0.11, and 0.06 μM for the Pf3D7, PfDd2, and PfItG strains, respectively. Additionally, Desmethylastemizole effectively blocks hERG K+ channels and inhibits histone-lysine N-methyltransferase EZH2 activity. This compound is relevant for research in long QT syndrome and malaria. -
H4/H1 Receptor Antagonist
H4R Antagonist 3 is a selective histamine H4 and H1 receptor antagonist with an EC50 of ≤10 mM. This compound is valuable for investigating the mechanisms underlying inflammatory, autoimmune, allergic, and ocular diseases. Its ability to modulate histamine receptor activity makes it a useful tool for research applications focused on these conditions. -
Histamine H3 Receptor Antagonist
Proxyfan is a potent antagonist of the histamine H3 receptor, exhibiting Ki values of 2.9 nM and 2.7 nM for rat and human H3 receptors, respectively. This compound demonstrates over 1000-fold selectivity for the H3 receptor compared to other histamine receptors. Proxyfan is useful in research applications focused on neurological disorders, cognitive enhancement, and sleep regulation, making it a valuable tool for studying histaminergic signaling pathways. -
Histamine H3 Receptor Antagonist
PF-03654764 is a potent and selective antagonist of the histamine H3 receptor, demonstrating Ki values of 1.2 nM for human H3 and 7.9 nM for rat H3 in whole cell assays. This compound exhibits significant potential in research applications related to allergies, particularly in the treatment of allergic rhinitis when combined with other antihistamines. Its oral bioactivity provides a valuable tool for investigating the role of histamine signaling in various physiological and pathological processes. -
Histamine H1 Receptor Antagonist
Diphenylpyraline is a potent histamine H1 receptor antagonist. This compound exhibits anticholinergic and antiallergic properties, making it effective as an orally active antihistamine. Diphenylpyraline is applicable in research focused on allergic conditions, including rhinitis and hay fever, as well as pruritic skin disorders. -
Histamine H1 Receptor Antagonist/5-Lipoxygenase Inhibitor
UCB-35440 is an orally active antagonist of the histamine H1 receptor and a selective inhibitor of 5-lipoxygenase. It demonstrates significant inhibition of leukotriene B4 (LTB4) formation in human whole blood, as well as a reduction in polymorphonuclear cell infiltration in mouse models. UCB-35440 also effectively inhibits histamine-induced bronchoconstriction and alleviates skin inflammation in guinea pig studies. This compound is suitable for research applications related to asthma and inflammatory skin conditions. -
Stable Isotope
Promethazine-d4 hydrochloride is a deuterated form of Promethazine hydrochloride, a first-generation antihistamine that primarily functions as a strong antagonist of the H1 receptor. It also exhibits moderate antagonistic activity at mACh receptors, alongside a moderate affinity for 5-HT2A, 5-HT2C, D2, and α1-adrenergic receptors. This stable isotope is useful for tracing studies, pharmacokinetic research, and metabolite identification in biological samples. -
Histamine Receptor Inverse Agonist
Mianserin-d3 is a deuterium-labeled form of Mianserin, primarily acting as an H1 receptor inverse agonist. It has demonstrated biological activity by activating κ-opioid and octopamine receptors, while also promoting ERK1/2 and CREB phosphorylation. Mianserin-d3 is valuable for investigating neurological disorders, including depression and epilepsy, and may influence social and exploratory behavior as well as electroconvulsive thresholds. -
Histamine H2 Receptor Antagonist
Cimetidine sulfoxide is a sulfoxide metabolite of the histamine H2 receptor antagonist Cimetidine. This compound demonstrates inhibitory activity at the H2 receptors, making it relevant for research applications involving gastric acid secretion and gastrointestinal disorders. Cimetidine sulfoxide may hold potential for exploring treatment options in peptic ulcer disease and upper gastrointestinal hemorrhage. -
anti-Allergic Agent
Setastine is an orally effective, non-sedative antihistamine that primarily targets H1 histamine receptors. It exhibits significant blocking properties, making it suitable for research applications related to allergies and rhinitis. Its long-acting effects further enhance its potential in exploring various allergic responses in scientific studies. -
Histamine H1 Antagonist
Noberastine is a potent antagonist of the Histamine H1 receptor, exhibiting significant peripheral antihistamine activity. This compound is primarily utilized in research focused on allergic responses and histamine-related disorders. Its ability to effectively inhibit H1 receptor activity makes it a valuable tool for studies investigating antihistaminic properties and related therapeutic applications. -
H4 Receptor Agonist
4-Methylhistamine hydrochloride is a highly selective agonist for the histamine H4 receptor (H4R), exhibiting a Ki value of 50 nM and over 100-fold selectivity compared to other histamine receptor subtypes. With a pEC50 of 7.4, it effectively activates H4R, making it a valuable tool for research in cancer, inflammation, and immunology. Applications include studies related to lung cancer and skin inflammatory conditions, providing insights into H4R-mediated pathways in these areas. -
Histamine Receptor Antagonist
Pimethixene is a potent antagonist of multiple receptor types, primarily functioning as a histamine receptor antagonist. It demonstrates significant activity against serotonin receptors (5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C), dopamine receptors (D2, D4), and muscarinic receptors (M1, M2), with reported pKis of 7.63 to 10.44. This pharmacological profile positions pimethixene as an effective agent for migraine management and offers valuable insights for research into antihistaminic and antiserotonergic therapies. -
Histamine Receptor Antagonist
SUN 1334H is a potent, orally active, and highly selective H1 receptor antagonist, exhibiting a Ki value of 9.7 nM. This compound effectively inhibits histamine-induced signaling, making it valuable for research on allergic responses and related conditions. Its specificity and potency make it suitable for studies investigating the role of H1 receptors in various biological systems. -
Histamine 3 Receptor Inverse Agonist
Samelisant free base is a selective inverse agonist of the histamine H3 receptor (H3R) that exhibits high binding affinity (Ki values of 8.7 nM for human H3R and 9.8 nM for rat H3R). It demonstrates effective brain penetration and oral bioavailability, making it a valuable tool in the study of sleep-related disorders. Research applications include exploring the mechanisms underlying sleep regulation and potential therapeutic interventions for insomnia and other sleep disturbances. -
Histamine H2 Receptor Antagonist
Cimetidine hydrochloride is a potent histamine H2 receptor antagonist with an inhibition constant (Ki) of 0.6 μM. It serves as an effective gastric acid reducer and is widely utilized in research pertaining to duodenal and gastric ulcers. Additionally, Cimetidine hydrochloride exhibits notable anti-cancer and anti-inflammatory properties, making it relevant for various therapeutic investigations. -
Histamine Receptor Antagonist
Adriforant is a selective 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. It effectively inhibits the actions of histamine, making it a valuable tool for studying the role of H4 receptors in various biological processes. This compound is particularly relevant for research in immunology, allergy, and inflammation, providing insights into potential therapeutic applications targeting histamine-mediated pathways. -
Histamine Receptor
Alcaftadine carboxylic acid selectively targets histamine H1 and H2 receptors, exhibiting broad-spectrum antihistaminic properties. This compound demonstrates significant efficacy in modulating immune cell recruitment and stabilizing mast cells, contributing to its therapeutic effects. Alcaftadine carboxylic acid effectively alleviates ocular itching associated with allergic conjunctivitis, showing superior performance compared to placebo and comparable efficacy to olopatadine 0.01%. This makes it a valuable candidate for research on allergy-related conditions and immune response modulation. -
Histamine 1 Receptor Antagonist
Acrivastine-d7 is a deuterated derivative of Acrivastine, targeting the histamine H1 receptor as an antagonist. It exhibits potent antihistaminic activity, making it valuable in studying allergic reactions and histamine-related pathways. This reagent can be utilized in pharmacokinetic studies and metabolic research involving H1 receptor interactions. -
H1 Histamine Receptor Antagonist
Thonzylamine hydrochloride is an orally active H1 histamine receptor antagonist. It exhibits significant antihistaminic and antianaphylactic properties, making it valuable for investigating hypersensitivity diseases, nasal congestion, allergic conjunctivitis, and other allergic conditions. This compound is a useful tool for researchers studying the mechanisms underlying allergic responses and evaluating potential therapeutic interventions. -
Histamine Receptor Antagonist
A-331440 is a selective antagonist of the histamine H3 receptor, which plays a critical role in the regulation of neurotransmitter release through inhibition at presynaptic sites. In preclinical studies with mice subjected to a high-fat diet, A-331440 demonstrated significant dose-dependent effects on body weight and fat loss. At a dosage of 5 mg/kg, it effectively reduced body weight akin to dexfenfluramine, while a 15 mg/kg dose led to substantial reductions in body fat and enhanced insulin tolerance, resembling the metabolic profile of mice on a low-fat diet. These results indicate A-331440's potential as an antiobesity agent by influencing histaminergic pathways related to appetite control and metabolic processes. -
H1-Antihistamine
Sequifenadine is an H1-antihistamine that effectively inhibits histamine action at the H1 receptor. This compound exhibits anti-inflammatory properties and is instrumental in the research of inflammatory eye diseases associated with allergic symptoms. Its ability to mitigate allergic responses makes it a valuable tool for studying the underlying mechanisms of allergies and related ocular conditions. -
H3R Inverse Agonist
H3R antagonist 1 is an inverse agonist of the histamine receptor 3 (H3R). This compound promotes the upregulation of myelin-associated glycoprotein (MAG) and myelin basic protein (MBP) in differentiating oligodendrocytes, which is crucial for myelination processes. H3R antagonist 1 is applicable in research focused on multiple sclerosis and related demyelinating disorders, providing insight into oligodendrocyte differentiation and myelin repair mechanisms. -
Antihistamine/anticholinergic Agent
Chlorphenoxamine hydrochloride is an antihistamine and anticholinergic agent that functions as a GPCR antagonist. It exhibits potent antiviral activity against lethal viral pathogens, including SARS-CoV, MERS-CoV, and Ebola virus, with reported IC50 values of 1.1 μM against Ebola virus and 6.2 μM against Marburg virus. This compound is utilized in research related to allergic conditions, urticaria, viral infections, and the treatment of Parkinson’s disease. -
Antihistamine/Anti-5-HT Agent
Dimethothiazine mesylate is an orally active tricyclic antihistamine and anti-5-HT agent that exhibits significant activity against decerebrate rigidity, demonstrating minimal sedative and soporific effects. This compound effectively reduces or eliminates the influence of both static and dynamic fusimotor activity on muscle spindles in decerebrate models. Dimethothiazine mesylate is relevant for research applications related to hemicrania and spasticity. -
Histamine Receptor
Aplysamine-1 is a potent antagonist of the histamine H3 receptor. This compound demonstrates significant modulation of neurotransmitter release and offers valuable insights into histamine signaling pathways. Aplysamine-1 is utilized in research exploring its potential therapeutic applications for neurological disorders and conditions related to histamine dysregulation. -
Stable Isotope
Asenapine-13C,d3 is a stable isotope-labeled form of Asenapine, a novel atypical antipsychotic. This compound acts primarily as an antagonist of serotonin, dopamine, adrenoceptors, and histamine receptors, demonstrating a range of pKi values indicative of strong binding affinity. Asenapine-13C,d3 is valuable for pharmacokinetic studies and metabolic research related to schizophrenia and bipolar disorder, providing insights into drug behavior in biological systems. -
Histamine H3 Receptor Antagonist
GT-2016 is a potent and selective antagonist of the histamine H3 receptor, exhibiting a Ki value of 43.8 nM. This compound demonstrates high selectivity for the H3 receptor over H1 and H2 receptors and is inactive against histamine methyltransferase. GT-2016 is valuable for research into neurological disorders and sleep regulation, providing insights into histaminergic signaling pathways. -
Antihistamine
Dioxopromethazine hydrochloride is a potent antihistamine that functions primarily by blocking H1 histamine receptors. It exhibits significant activity in mitigating asthmatic symptoms and is frequently utilized in research focused on allergic responses and respiratory disorders. This compound's ability to alleviate histamine-mediated effects makes it a valuable tool in the study of inflammatory pathways and therapeutic interventions. -
Antihistamine
Talastine is a potent H1-antihistamine that effectively blocks the action of histamine at H1 receptor sites. This compound is utilized in research to study allergic responses and related conditions, and may induce allergic exanthema in experimental models. Its mechanism highlights its potential role in exploring antihistamine therapies and allergy-related pharmacology. -
H1 Receptor Antagonist
Promethazine-d4 is a deuterated form of promethazine, functioning primarily as an H1 receptor antagonist. This compound exhibits antihistamine, sedative, antiemetic, anticholinergic, and anti-motion sickness activities. It is widely utilized in research applications focused on histamine-related disorders and the pharmacological study of sedation and motion sickness. -
Isomer of Dropropizine
(+)-Dropropizine is an isomer of Dropropizine that functions as an orally active histamine receptor inhibitor, exhibiting notable anti-allergic properties. This compound has been shown to alleviate cough by modulating neuropeptides associated with the cough reflex and by interfering with the activation of peripheral sensory nerve endings. (+)-Dropropizine holds potential for research focused on addressing dry coughs linked to various respiratory diseases. -
Dopamine Receptor Agonist
Proterguride is a potent agonist of dopamine receptors, demonstrating significant potential in modulating dopaminergic signaling. Additionally, it exhibits antagonistic activity at the histamine H(1) receptor and alpha(1)-adrenoceptor, while also partially activating serotonergic 5-HT2A/B receptors. This compound is valuable for research focused on neurological diseases, including Parkinson's disease, providing insights into dopaminergic mechanisms and receptor interactions. -
PAF/Histamine Antagonist
Sch-40338 is a dual antagonist targeting platelet-activating factor (PAF) and histamine, exhibiting an IC50 of 0.59 μM in PAF-induced platelet aggregation and a Ki of 5.4 μM for histamine H₁ receptor binding. This compound is valuable for investigating the mechanisms underlying allergic diseases, offering insights into the modulation of inflammatory responses and platelet activation pathways. Sch-40338 serves as a useful tool for researchers exploring therapeutic strategies in allergen-mediated conditions. -
Antihistamine
Phenindamine is a first-generation antihistamine that primarily targets the H1 receptor. It exhibits significant anticholinergic and sedative effects, making it useful in alleviating allergic symptoms such as rhinitis and urticaria. This compound is often utilized in pharmacological studies to explore its effects on the central nervous system and its potential role in addressing respiratory conditions associated with allergic responses. -
Antihistamine
Cinnarizine-d8 is a deuterium-labeled derivative of Cinnarizine, which operates primarily as an antihistamine and calcium channel blocker. This compound has been utilized in pharmacological research to elucidate the mechanisms of action and metabolic pathways of antihistamines. Its isotopic labeling enhances analytical sensitivity in studies involving pharmacokinetics and pharmacodynamics. -
Histamine H3 Antagonist
Carcinine dihydrochloride is a selective histamine H3 receptor antagonist with a Ki value of 0.2939 μM. It demonstrates notable biological activities, including reducing histamine content, exhibiting antioxidant properties, and providing neuroprotective effects. Additionally, Carcinine dihydrochloride shows a positive inotropic effect and has potential to lower blood sugar and lipid levels. This compound is applicable in research related to inflammation, neurological disorders, cardiovascular health, and metabolic diseases, including retinal damage, seizures, and diabetes. -
Histamine-release Inhibitor
Panaxydiol is a histamine-release inhibitor that effectively suppresses histamine secretion in biological systems. This compound features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating the formation of diverse chemical linkages. Its unique properties make Panaxydiol a valuable reagent for researchers involved in chemical biology, drug discovery, and the development of innovative therapeutic strategies. -
5-HT Receptor Agonist
8 Hydroxy PIPAT oxalate is a selective agonist of the 5-HT1A receptor. This compound activates serotonergic signaling pathways, promoting the degranulation of enteric mast cells and enhancing spontaneous histamine release in both guinea pig and human intestinal preparations. Its ability to modulate histamine release suggests potential applications in understanding and addressing functional gastrointestinal disorders, including irritable bowel syndrome. -
Histamine Receptor Agonist
Methimepip dihydrobromide is a potent and selective agonist of the histamine H3 receptor, exhibiting an EC50 of 0.316 nM. This compound is useful for investigating the role of H3 receptors in various physiological processes and could be valuable in research related to neurological disorders, sleep regulation, and appetite control. Its specificity and strength make it an essential tool in pharmacological studies of histamine signaling pathways. -
D2/H1 Antagonist
Norzine dimalate, a potent antagonist of dopamine D2 and histamine H1 receptors, exhibits significant anti-emetic and antipsychotic properties. Additionally, it acts as a selective ABCC1 activator, contributing to the reduction of amyloid-β load in murine models. Its diverse biological activities make Norzine dimalate a valuable reagent for research in neuropharmacology and Alzheimer's disease studies. -
Histamine H3 Receptor Agonist
Immethridine dihydrobromide is a selective agonist of the histamine H3 receptor (H3R) and demonstrates 300-fold selectivity for H3R over the H4 receptor, with no binding affinity for H1 or H2 receptors. This compound is valuable for research applications related to experimental autoimmune encephalomyelitis (EAE), providing insights into the role of H3R in neuroinflammatory conditions. Its specific targeting of H3R makes it a significant tool for investigating therapeutic approaches in neurological disorders. -
H3R Antagonist
H3R Antagonist 6 is a potent antagonist of the Histamine receptor 3 (H3R), exhibiting an IC50 of 5.6 nM. This compound, when labeled with 18F, demonstrates high radiochemical yield and molar activity, alongside moderate brain uptake, albeit with some off-target binding to the Sigma-1 receptor. H3R Antagonist 6 serves as a valuable PET radioligand for positron emission tomography imaging, facilitating research into central nervous system (CNS) disorders. -
Stable Isotope
Benztropine-d3 mesylate is a deuterium-labeled form of the centrally acting anticholinergic agent, Benztropine mesylate. This compound is primarily utilized in Parkinson's disease research and exhibits anti-histaminic properties alongside its function as a dopamine reuptake inhibitor. Additionally, Benztropine mesylate acts as an allosteric antagonist at the human D2 dopamine receptor and demonstrates effects against cancer stem cells (CSCs), making it valuable for studies in both neuropharmacology and oncology. -
Histamine H3 Receptor Modulator
Cipralisant maleate is a selective histamine H3 receptor modulator, exhibiting both antagonistic activity in vivo and agonistic effects in vitro. With a high affinity demonstrated by a pKi of 9.9 and a Ki of 0.47 nM for the rat histamine H3 receptor, this compound shows potential applications in attention-deficit hyperactivity disorder research. Additionally, Cipralisant maleate serves as a click chemistry reagent due to its alkyne group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules.
