Catalog No.
Product Name
Application
Product Information
Citations
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5-HT3 Serotonin Receptor Agonist
Amanozine is a potent agonist of the 5-HT3 serotonin receptor, playing a critical role in mediating serotonin signaling within the nervous system. This compound exhibits potential therapeutic applications in the study of various neurological disorders, making it a valuable tool for research in psychopharmacology and neuropharmacology. Its ability to influence serotonin receptor activity could provide insights into the mechanisms underlying mood regulation and anxiety. -
5-HT4 Receptor Antagonist
GR125487 sulfamate is a selective antagonist of the 5-HT4 receptor, which plays a significant role in various cognitive and gastrointestinal functions. This compound effectively inhibits cognitive enhancement, making it valuable for researching memory disorders, mood disorders, gastrointestinal dysfunctions, and urinary tract issues. Its oral bioactivity allows for convenient administration in preclinical studies. -
5-HT(1B/1D) Receptor Agonist
Naratriptan-d3 hydrochloride is a selective agonist of the 5-HT1B/1D receptors. This deuterium-labeled derivative exhibits effective vasoconstrictive properties on cranial arteries through activation of these receptors, with an EC50 value of 0.11 μM observed in dog basilar arteries. Additionally, it is known to inhibit trigeminal nerve-mediated dural neurogenic plasma extravasation and mitigate sterile inflammation. Naratriptan-d3 hydrochloride is primarily utilized in research focusing on acute migraine, particularly related to cranial vascular dynamics and neuroinflammatory responses. -
5-HT2A/D2 Antagonist
Blonanserin dihydrochloride is a potent antagonist of the 5-HT2A and dopamine D2 receptors, exhibiting Ki values of 0.812 nM and 0.142 nM, respectively. This compound is primarily utilized as an atypical antipsychotic agent and is relevant for research focused on extrapyramidal symptoms, sedation levels, and hypotensive effects. Its pharmacological profile makes it a valuable tool in the study of neuropsychiatric disorders and related therapeutic interventions. -
5-HT2 Receptor Agonist
CYB210010 is a long-acting agonist of the serotonin 5-HT2 receptors, specifically targeting the 5-HT2A and 5-HT2C subtypes (EC50: 4.1 nM and 7.3 nM, respectively). This compound is orally bioavailable and capable of penetrating the central nervous system, leading to a notable head twitch response (HTR) without the development of behavioral tolerance following chronic administration. Its selectivity and consistent biological activity make CYB210010 a valuable tool for research into the roles of serotonin receptors in various neuropsychiatric conditions. -
5-HT1F Receptor Agonist
LY334370 hydrochloride is a highly selective agonist of the 5-HT1F receptor, demonstrating a binding affinity with a Kd value of 0.446 nM. This compound exhibits noteworthy anti-migraine activity, making it valuable for research in migraine pathophysiology and treatment exploration. Its mechanism of action highlights the therapeutic potential of targeting the serotonergic system in neurological disorders. -
Stable Isotope
Paliperidone-d4 is the deuterated form of Paliperidone, a major active metabolite of Risperidone, acting as a dopamine D2 antagonist and 5-HT2A antagonist. This compound also exhibits antagonistic properties at alpha-1 and alpha-2 adrenergic receptors as well as H1-histaminergic receptors. Paliperidone's primary application is in the treatment of schizophrenia, making it valuable for pharmacological research and development of antipsychotic therapies. -
5-HT Deamination Inhibitor
RS 2232 is a competitive inhibitor of 5-hydroxytryptamine (5-HT) deamination, demonstrating a Ki of 0.054 μM. This compound selectively and reversibly inhibits type A monoamine oxidase, making it a valuable tool in neurological research. RS 2232 is utilized to gain insights into the role of serotonin metabolism in various brain functions and disorders. -
D2 Receptor Binder
Mosapramine is a D2 receptor binder that acts as an antipsychotic agent and is a metabolite of Clocapramine. It selectively binds to striatal dopamine D2 receptors and frontal lobe 5-HT2 receptors, exhibiting a D2/5-HT2 receptor occupancy ratio of 7.4. This compound induces characteristic neuropharmacological effects in rat models, including extrapyramidal symptoms, hyperprolactinemia, and increased salivation, while displaying a lower incidence of weight loss. Mosapramine is valuable for research applications related to schizophrenia and its underlying mechanisms. -
5-HT6 Receptor Agonist
ST1936 is a selective agonist of the 5-HT6 receptor, exhibiting nanomolar affinity with a Ki value of 13 nM for human 5-HT6 receptors. It also demonstrates notable selectivity across related serotonin receptors, with Ki values of 168 nM for 5-HT7 and 245 nM for 5-HT2B. Additionally, ST1936 has moderate affinity for human and rat α2 adrenergic receptors, with a Ki of 300 nM. This compound is valuable for neuroscience research, particularly in studies related to cognitive function and mood disorders. -
5-HT2 Antagonist
Spiramide is a potent and selective antagonist of the 5-HT2 receptor and dopamine D2 receptor, demonstrating Ki values of 2 nM and 3 nM, respectively. It exhibits over 2000-fold selectivity for the 5-HT2 receptor compared to the 5-HT1C receptor (Ki = 4300 nM). Due to its pharmacological properties, Spiramide is valuable for research applications in the fields of neuropharmacology and the study of antipsychotic mechanisms. -
5-HT2 Receptor Antagonist
(S)-Mirtazapine is a stereoselective antagonist of the 5-HT2 receptor, showing significant pronociceptive effects in animal models of acute thermal nociception. This S(+)-enantiomer exhibits distinct pharmacological properties, contributing to its potential applications in pain research and neuropharmacology. Additionally, (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2, which may influence its therapeutic efficacy and safety profile. -
Serotonin/Dopamine Receptor Modulator
Brexpiprazole S-oxide is the primary metabolite of the atypical antipsychotic Brexpiprazole, functioning as a serotonin and dopamine receptor modulator. It exhibits partial agonism at the human 5-HT1A receptor and antagonism at the 5-HT2A receptor, with affinities (Ki) of 0.12 nM and 0.47 nM, respectively, and a potent partial agonist effect at the dopamine receptor (Ki = 0.3 nM). This compound is utilized in research focused on neuropharmacology, psychopharmacology, and the modulation of serotonergic and dopaminergic signaling pathways. -
5-HT6/5-HT2A Antagonist
Landipirdine is a potent antagonist of the 5-HT6 and 5-HT2A receptors. This orally active compound is primarily investigated for its potential therapeutic effects in the context of Parkinson's disease. Its mechanism of action provides a valuable tool for researchers exploring receptor interactions and neuropharmacology related to neurodegenerative conditions. -
5HT4 Receptor Agonist
Renzapride is a full agonist of the 5-HT4 receptor, exhibiting a Ki value of 115 nM. Additionally, it acts as an antagonist at both the 5-HT2b and 5-HT3 receptors. This compound is primarily utilized in research focusing on constipation-predominant irritable bowel syndrome (C-IBS), making it valuable for exploring therapeutic interventions in gastrointestinal disorders. -
5-HT1A Receptor Agonist
Lauroscholtzine, also known as N-Methyllaurotetanine, acts as an agonist of the 5-HT1A receptor. This natural alkaloid is known for its modulatory effects on serotonergic signaling, making it a valuable tool for studying the role of serotonin in various physiological processes. Its biological activity is relevant for research into neuropharmacology, particularly in the context of anxiety and depression-related disorders. -
5-HT Receptor Antagonist
Seganserin is a potent orally active antagonist of the 5-HT receptor, exhibiting a plasma half-life of 26.1 ± 12.9 hours. This compound plays a crucial role in neurological research, offering insights into serotonin-mediated pathways and their implications in various neuropsychiatric conditions. Its selectivity for the 5-HT receptor makes it a valuable tool for exploring serotonin receptor signaling and pharmacology. -
5-HT Receptor Antagonist
Dolasetron Mesylate hydrate is a serotonin 5-HT3 receptor antagonist that primarily functions by blocking the action of serotonin at these receptors. This compound is widely utilized in research focused on understanding and mitigating chemotherapy-induced nausea and vomiting. Its efficacy in targeting the 5-HT3 receptor makes it a valuable tool in pharmacological studies related to antiemetic therapy. -
5-HT Receptor Control
2C-B-FLY hydrochloride is a selective 5-HT receptor agonist, functioning primarily on the serotonin receptor system. This compound exhibits significant hallucinogenic properties, making it valuable for research into psychoactive mechanisms and the modulation of serotonergic pathways. Its unique structure as a dihydrodifuran analog of 4-bromo-2,5-dimethoxyphenethylamine (2C-B) enhances its potential applications in behavioral and neuropharmacological studies. -
Vasopressin Receptor Agonist
Argipressin acetate is a potent vasopressin receptor agonist, primarily targeting the V1, V2, and V3 receptors. It exhibits high affinity for the V1 receptor, with a dissociation constant (Kd) of 1.31 nM in A7r5 rat aortic smooth muscle cells. This compound is valuable for research applications exploring vascular physiology, fluid balance, and the modulation of blood pressure. -
Stable Isotope
Thioridazine-d3 hydrochloride is a deuterium-labeled derivative of Thioridazine, an antagonist of dopamine receptor D2 family proteins. It demonstrates significant anti-psychotic and anti-anxiety effects while also inhibiting the PI3K-Akt-mTOR signaling pathway, contributing to anti-angiogenic activity. Additionally, Thioridazine exhibits antiproliferative properties and induces apoptosis in various cancer cell types, with particular efficacy against cancer stem cells (CSCs). This stable isotope is valuable for pharmacokinetic studies and elucidating mechanisms of action in related research applications. -
ETA/ETB Antagonist
Macitentan-d4 is a deuterated analog of the dual ETA and ETB endothelin receptor antagonist, Macitentan. This compound exhibits significant biological activity by blocking the effects of endothelin-1, which is implicated in conditions such as pulmonary arterial hypertension (PAH) and idiopathic pulmonary fibrosis (IPF). Macitentan-d4 serves as a valuable tool for research into the underlying mechanisms of endothelin signaling and its role in cardiovascular and pulmonary disorders. -
Endocannabinoid
Arachidonoyl ethanolamide phosphate functions as an endogenous ligand for cannabinoid receptors, primarily targeting the CB1 subtype in the central nervous system and the CB2 subtype in peripheral immune cells. This compound is involved in modulating various physiological processes, including pain perception, mood regulation, and immune response. Its unique action profile makes it useful for research in neurobiology and immunology, particularly in studies focusing on the endocannabinoid system and its implications in various diseases. -
Stable Isotope
N-(Phenylacetyl-d5)glycine is a deuterated form of phenylacetylglycine, functioning as a stable isotope. This compound serves as a gut microbial metabolite that can activate the beta-2 adrenergic receptor (β2AR). Its biological activity includes providing protective effects against cardiac injury induced by ischemia and reperfusion, making it valuable for research in cardiac health and metabolic studies. -
Stable Isotope
D-Mannitol-13C6 is a stable isotope-labeled form of D-Mannitol, targeting metabolic pathways through its role as an osmotic agent. This compound is utilized in various research applications, including studies on calcium and magnesium absorption, cecal fermentation, and the modulation of insulin sensitivity. D-Mannitol has been shown to promote the browning of white adipose tissue by activating the β3-adrenergic receptor, which can lead to enhanced thermogenesis and potential reductions in blood glucose levels. Additionally, it is employed in plant cell culture to maintain osmotic balance and protect cellular integrity. -
Stable Isotope
D-Mannitol-13C is a stable isotope-labeled derivative of D-Mannitol. This compound serves as a valuable osmotic diuretic and is utilized in various research applications, including the study of calcium and magnesium absorption and retention through cecal fermentation. D-Mannitol is known to promote brown adipose tissue formation, enhance insulin sensitivity, and lower blood glucose levels by activating the β3-adrenergic receptor, leading to the conversion of white fat cells into brown fat cells. Additionally, it is employed to maintain osmotic pressure in plant cell cultures, aiding in cellular protection during physiological manipulation. -
Stable Isotope
Perphenazine-d4 is a deuterated derivative of Perphenazine, a typical antipsychotic agent primarily inhibiting the 5-HT2A receptor, alpha-1A adrenergic receptor, dopamine receptor D2/D3, D2L receptor, and histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively. This stable isotope is valuable for pharmacokinetic studies, allowing for the precise tracking of Perphenazine metabolism and distribution in biological systems. Perphenazine-d4 is essential for researchers focusing on neuropharmacology and drug interaction studies involving antipsychotic medications. -
Antihistamine Agent
Meclizine is an antihistamine that reversibly inhibits the binding of histamine to H1 receptors, making it effective as an anti-motion sickness agent. As a piperazine derivative, it can cross the blood-brain barrier, enabling its use in neurological research. Additionally, Meclizine acts as an agonist for the mouse constitutive androstane receptor (CAR) and serves as an inverse agonist for the human equivalent. This compound is also relevant for studying polyglutamine (polyQ) toxicity disorders, including Huntington's disease. -
Stable Isotope
D-Mannitol-2-13C is a stable isotope-labeled derivative of D-Mannitol. This 13C-labeled compound plays a critical role in metabolic studies, particularly in understanding carbohydrate metabolism and energy homeostasis. D-Mannitol serves as an osmotic diuretic, promotes the absorption of minerals, enhances brown adipose tissue formation, and demonstrates potential for reducing blood glucose levels through β3-adrenergic receptor activation. It is frequently employed in cell culture applications to maintain osmotic pressure and protect cells, particularly when cell walls are compromised. -
Antihistamine Agent
Meclizine dihydrochloride monohydrate is an antihistamine that reversibly inhibits histamine interactions at the H1 receptor. As a member of the piperazine class of H1 antagonists, it is primarily utilized as an effective anti-motion sickness agent. This compound also demonstrates the ability to cross the blood-brain barrier and functions as an agonist for the mouse constitutive androstane receptor (CAR), while acting as an inverse agonist for the human CAR. It has applications in research focusing on polyQ toxicity disorders, including Huntington's disease. -
Somatostatin Receptor Agonist
Octreotide dihydrochloride is a synthetic octapeptide that acts as an agonist for somatostatin receptors, primarily targeting subtypes 2, 3, and 5. By increasing Gi protein activity, it effectively reduces intracellular cAMP levels, contributing to its antitumor effects. Octreotide dihydrochloride is utilized in research applications related to apoptosis and is particularly relevant in studies of acromegaly and other disorders associated with aberrant somatostatin signaling. -
A1 Adenosine Teceptors Agonist
CCPA hemihydrate is a highly selective agonist of the A1 adenosine receptors, exhibiting a Ki value of 0.4 nM. It demonstrates preferential binding to the A1 receptor over the A2 receptor, with a Ki of 3900 nM. As a purine nucleoside analog, CCPA hemihydrate has demonstrated broad antitumor activity, particularly in the context of indolent lymphoid malignancies. Its anticancer effects are mediated through mechanisms such as inhibition of DNA synthesis and induction of apoptosis, making it valuable for research applications in cancer therapy. -
S1P1 Receptor Agonist
(S)-FTY-720 Vinylphosphonate is a chiral phosphonate analogue of Fingolimod that functions as an S1P1 receptor agonist. It demonstrates significant biological activity, activating the S1P1 receptor with an EC50 of 75 nM and effectively inhibiting Camptothecin-induced apoptosis in IEC-6 cells. This reagent is relevant for research into autoimmune diseases, providing insights into therapeutic mechanisms and potential interventions. -
mGlu1 Antagonist
LY456236 free base is a selective, non-competitive antagonist of the metabotropic glutamate receptor 1 (mGlu1), showing an IC50 for phosphatidylinositol hydrolysis of 0.145 μM. Additionally, it inhibits epidermal growth factor receptor (EGFR) activity with an IC50 of 0.918 μM. This compound effectively blocks cell proliferation by targeting the MAPK signaling pathway, counteracting the anti-apoptotic effects of DHPG. LY456236 free base is a valuable tool for research into epilepsy and other neurological disorders. -
Stable Isotope
Cyproheptadine-d3 is a deuterium-labeled derivative of the antihistamine Cyproheptadine, serving as a stable isotope for research applications. It primarily acts as a serotonin and histamine receptor antagonist, making it useful in studies investigating receptor interactions and pharmacokinetics. This reagent is valuable for tracing and quantifying Cyproheptadine in various biological samples, facilitating research in pharmacology and toxicology. -
β2AR Activator
Phenylacetylglycine is a gut microbial metabolite that acts as a β2-adrenergic receptor (β2AR) activator. It has demonstrated protective effects against cardiac injury resulting from ischemia/reperfusion. This compound is significant for research into cardiovascular health and the role of microbiota in modulating cardiac responses. -
Dopaminergic Neurotoxin
MPTP (1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine) is a potent dopaminergic neurotoxin that readily penetrates the blood-brain barrier. It is primarily utilized to create animal models of Parkinson’s Disease, enabling the study of neurodegenerative processes. MPTP acts by converting into MPP+, which induces apoptosis in dopaminergic neurons, serving as a valuable tool for investigating therapeutic strategies and the underlying mechanisms of neurodegeneration. -
Platelet Aggregation Inhibitor
Epoprostenol sodium, a synthetic derivative of prostaglandin I2, primarily acts as a potent inhibitor of platelet aggregation. This compound is widely recognized for its role in the management of pulmonary arterial hypertension (PAH) and is utilized in clinical settings such as pulmonary hypertension and organ transplantation. Its ability to modulate vasodilation and inhibit platelet activation makes it a valuable tool in related biomedical research applications. -
Histamine Release Inhibitor
Alginic acid is a natural polysaccharide recognized for its ability to inhibit histamine release, making it a valuable compound for research into allergic reactions and inflammation. Its remarkable water solubility, film-forming properties, and biodegradability enhance its applicability in various biological studies. Alginic acid has been demonstrated to induce oxidative stress-mediated effects, resulting in hormone secretion disorders, apoptosis, and autophagy in mouse granulosa cells and ovaries. This compound is of particular interest in anti-anaphylactic and anti-inflammatory research applications. -
Stable Isotope
Kynurenic acid-d5 is a deuterium-labeled analog of kynurenic acid, an endogenous metabolite of tryptophan. It acts as a broad-spectrum antagonist of NMDA and glutamate receptors, as well as the α7 nicotinic acetylcholine receptor. Additionally, kynurenic acid-d5 serves as an agonist for GPR35/CXCR8, making it valuable in studies related to neuropharmacology and neurotransmitter signaling pathways. This stable isotope is ideal for tracing and characterization studies in metabolic research. -
LPA2 Receptor Antagonist
H2L5186303 is a potent and selective antagonist of the lysophosphatidic acid receptor 2 (LPA2), exhibiting an IC50 of 9 nM. This compound induces apoptosis and effectively inhibits cell proliferation and motility. Additionally, H2L5186303 demonstrates anti-inflammatory properties, making it a valuable reagent for research involving cancer biology and inflammation pathways. -
mGlu4 Agonist
Cinnabarinic acid primarily functions as an orthosteric agonist of the mGlu4 receptor, selectively engaging with residues within its glutamate binding pocket, and exhibiting no significant activity on other mGlu receptors. As an endogenous metabolite of the kynurenine pathway of tryptophan, cinnabarinic acid plays a role in cell apoptosis. This compound is valuable in research exploring mGlu4 receptor signaling and its implications in neurological disorders. -
5-HT2 Receptor Antagonist
Cyproheptadine is a selective antagonist of the 5-HT2A receptor, exhibiting both antidepressant and antiserotonergic properties. In addition to its central nervous system effects, Cyproheptadine demonstrates antiplatelet and thromboprotective activities. This compound is valuable for research applications focused on thromboembolic disorders, contributing to the understanding of related vascular conditions. -
Dopamine Receptor Antagonist
Flupentixol dihydrochloride is a potent antagonist of D1 and D2 dopamine receptors, demonstrating significant inhibition of PI3Kα with an IC50 of 127 nM. This compound exhibits anti-proliferative effects on cancer cells and promotes apoptosis, making it a valuable tool in oncology research. Additionally, Flupentixol has applications in studies related to schizophrenia, anxiety, and depression, contributing to the understanding of these complex neuropsychiatric disorders. -
PAR2 Antagonist
ENMD-1068 hydrochloride is a selective antagonist of protease-activated receptor 2 (PAR2). This compound effectively reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling pathways. Additionally, ENMD-1068 hydrochloride demonstrates the ability to inhibit the proliferation of endometrial cells and induce apoptosis in epithelial cells associated with lesions. This reagent is valuable for research applications in endometriosis and liver fibrosis. -
σ2 Receptor Agonist
PB28 dihydrochloride is a potent σ2 receptor agonist, exhibiting high affinity with a Ki of 0.68 nM, and also acts as a σ1 antagonist with a Ki of 0.38 nM. This compound demonstrates significant biological activity by inhibiting electrically evoked twitch responses in guinea pig bladder and ileum, with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride has been shown to modulate SARS-CoV-2-human protein-protein interactions, induce caspase-independent apoptosis, and display antitumor effects, making it a valuable tool for research in neuropharmacology and cancer biology. -
H1-histamine/P2X7 Receptor Antagonist
Oxatomide is a dual antagonist of the H1-histamine receptor and the P2X7 receptor, noted for its oral bioavailability. It exhibits significant antihistaminic, antiallergic, and anti-inflammatory properties, making it a valuable compound for the study of allergic diseases. Researchers can utilize Oxatomide to investigate mechanisms of allergy and inflammation, contributing to potential therapeutic advancements. -
PAR-1 Antagonist
Atopaxar is a selective and reversible antagonist of the thrombin receptor protease-activated receptor-1 (PAR-1). By inhibiting PAR-1 signaling, Atopaxar serves as an effective antiplatelet agent, disrupting platelet activation and aggregation. This compound is valuable for research applications related to atherothrombotic diseases, providing insights into the mechanisms of platelet-mediated thrombosis and potential therapeutic interventions. -
Adenosine Receptor Agonist
N6-Benzyladenosine is an adenosine receptor agonist that demonstrates significant cytotoxic activity. It effectively induces apoptosis in cells and arrests the cell cycle at the G0/G1 phase, making it a valuable tool for studying cell proliferation and death. Additionally, N6-Benzyladenosine inhibits Toxoplasma gondii adenosine kinase, providing insights into its potential applications in antiparasitic research and glioma studies. -
CBR1 Inhibitor
Hydroxy-PP-Me is a selective inhibitor of the cannabinoid receptor type 1 (CBR1) with an IC50 of 759 nM. It effectively inhibits serum starvation-induced apoptosis and enhances the cytotoxic effects of chemotherapeutic agents such as Daunorubicin and Arsenic Trioxide (As2O3) on tumor cells. Hydroxy-PP-Me is a valuable tool for cancer research, particularly in the study of leukemia and related malignancies.
