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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. -
A1 Adenosine Receptor Agonist
CCPA (2-Chloro-N6-cyclopentyladenosine) is a highly selective agonist for A1 adenosine receptors, demonstrating a Ki value of 0.4 nM. This compound effectively inhibits adenylate cyclase, with an IC50 of 33 nM. CCPA is relevant in studies investigating anti-seizure and cardioprotective effects, making it a valuable tool for research related to seizures and myocardial infarction. -
NF-κB Expression Reducer, ERK 1/2 Activator, Beta-Adrenergic Receptor Modulator, Calcium Channel Inhibitor
Eupatorin is a flavonoid that functions primarily as an NF-κB expression reducer and an ERK 1/2 activator, while also modulating beta-adrenergic receptors and inhibiting calcium channels. It demonstrates significant antiproliferative and vasodilatory effects, inducing apoptosis and causing G2/M phase cell cycle arrest, alongside reactive oxygen species (ROS) production. Eupatorin has been shown to impact inflammatory mediators and calcium signaling pathways, making it relevant for research in breast cancer, hypertension, and leukemia. Metabolized by CYP1A1 and other CYP1 enzymes, Eupatorin yields bioactive metabolites that maintain antiproliferative properties. -
Adrenergic Receptor Antagonist
Aaptamine is an alkaloid derived from the marine sponge Aaptos suberitoides, functioning primarily as a competitive antagonist of the α-adrenergic receptor. This compound exhibits significant cytotoxicity against tumor cells, inducing apoptosis and cell cycle arrest while promoting p21 expression through a p53-independent mechanism. Aaptamine also demonstrates a variety of biological activities, including anti-tumor, antioxidant, antibacterial, and analgesic effects, making it a valuable tool for cancer research and therapeutic applications. -
α-1A Adrenergic Receptor Agonist
Dabuzalgron is a selective α-1A adrenergic receptor agonist primarily utilized for the treatment of urinary incontinence. This compound exhibits key biological activity by enhancing bladder function, thereby mitigating symptoms associated with overactive bladder. Additionally, Dabuzalgron has been shown to provide protection against Doxorubicin-induced cardiotoxicity through the preservation of mitochondrial function, making it relevant in cardiovascular research. -
S1PR1 Antagonist
W146 TFA is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1), exhibiting an EC50 value of 398 nM. This compound is instrumental in studying the role of S1PR1 in various biological processes, including immune modulation and cardiovascular function. W146 TFA is valuable for research applications involving cytokine signaling and cellular proliferation pathways. -
ICMT Inhibitor
UCM-1336 is a potent inhibitor of Isoprenylcysteine Carboxyl Methyltransferase (ICMT), exhibiting an IC50 of 2 μM. This compound effectively induces mislocalization of endogenous Ras, resulting in decreased Ras activation. UCM-1336 has shown the ability to trigger cell death through autophagy and apoptosis, making it a valuable tool for research in cancer biology and signal transduction pathways. -
5-HT2/D1/D2 Antagonist
Olanzapine-d3 is a deuterated form of olanzapine, targeting multiple receptors, including serotonin receptors 5-HT2A, 5-HT2C, and dopamine receptors D1 to D4. This selective and orally active monoaminergic antagonist exhibits high affinity binding with Ki values ranging from 4 to 57 nM for relevant targets. It is primarily utilized in research related to psychopharmacology and the treatment of schizophrenia and bipolar disorder, enabling detailed pharmacokinetic studies and investigation of receptor interactions. -
mGlu1 Antagonist
LY456236 is a selective, non-competitive antagonist of the metabotropic glutamate receptor 1 (mGlu1), exhibiting an IC50 of 0.145 μM for the inhibition of phosphatidylinositol hydrolysis. Additionally, it demonstrates inhibitory activity against EGFR with an IC50 of 0.918 μM. By targeting the MAPK pathway, LY456236 effectively blocks cell proliferation and reverses the anti-apoptotic effects of DHPG. This reagent is suitable for investigations in epilepsy and related neurological research. -
GLP-1R Agonist/GIPR Antagonist
Maridebart cafraglutide is a novel peptide-antibody conjugate that serves as a GLP-1 receptor agonist and GIP receptor antagonist. This compound exhibits potent agonistic activity against GLP-1 receptors across species, with EC50 values of 24.4 pM for human, 5.7 pM for cynomolgus monkey, 2.4 pM for rat, and 123 pM for mouse. Additionally, it shows antagonistic effects on GIP receptors with IC50 values of 46.4 nM in human, 26.5 nM in cynomolgus monkey, and 822.3 nM in rat models. Maridebart cafraglutide is primarily used for investigating mechanisms of obesity and type 2 diabetes. -
GIP/GLP-1 Agonist
Ribupatide is a dual agonist targeting both gastric inhibitory polypeptide (GIP) and glucagon-like peptide 1 (GLP-1) receptors. It exhibits significant antidiabetic activity, making it a valuable compound for research applications focused on metabolic disorders and diabetes management. Its dual mechanism may provide insights into the intricate regulation of glucose metabolism. -
GIP/GLP-1 Agnonist
Relsipatide is a dual agonist of the gastric inhibitory polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. This compound demonstrates significant potential in enhancing insulin secretion and reducing glucagon levels, making it a valuable tool in antidiabetic research. Its unique mechanism of action may contribute to improved glycemic control and metabolic regulation in diabetes studies. -
PEGylated Exenatide
Visepegenatide is a PEGylated form of Exenatide, primarily targeting GLP-1 receptors to enhance insulin secretion and improve beta-cell function. This compound demonstrates significant activity in reducing hyperglycemia and managing insulin resistance. Visepegenatide is a valuable tool for research focused on type 2 diabetes and related metabolic disorders. -
GIP/GLP Agonist
Enicepatide is a dual agonist for the gastric inhibitory polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. This compound is primarily investigated for its antidiabetic properties, contributing to glucose metabolism regulation and insulin secretion enhancement. Research applications include exploring its potential role in treating metabolic disorders and obesity-related conditions. -
GIP/GLP-1 Agonist
Astepatide is a dual agonist of the gastric inhibitory peptide (GIP) receptor and glucagon-like peptide-1 (GLP-1) receptor, which primarily influences glucose metabolism and insulin secretion. This compound demonstrates significant anti-diabetic activity, making it a valuable tool for research related to diabetes and metabolic disorders. Astepatide can aid in exploring mechanisms of action and therapeutic potential for obesity and type 2 diabetes. -
Anti-diabete Agent
Glyceollin III is a soybean-derived glyceollin that functions as an anti-diabetic agent. It enhances insulin-stimulated glucose uptake and promotes the secretion of glucagon-like peptide-1 (GLP-1). This compound is valuable for research focused on type 2 diabetes and its metabolic effects. -
H1 receptor Antagonist
R 58639 is a selective histamine H1 receptor antagonist. It demonstrates significant biological activity in the modulation of allergic responses and cognitive processes. This compound is primarily utilized in research focusing on the pathophysiology and treatment of gastric ulcers, providing insights into the role of H1 receptor signaling in gastrointestinal biology. -
Histamine H2 Receptor Agonist
Betazole hydrochloride is a pyrazole derivative that acts as a histamine H2 receptor agonist. This compound stimulates gastric acid secretion and significantly elevates common bile duct pressure. Betazole is primarily utilized as a diagnostic agent, known as histalog, to assess gastric acid secretory capacity. -
Antihistamine
Diphenhydramine is a first-generation antihistamine that functions primarily as a histamine H1-receptor antagonist. It exhibits anti-cholinergic properties, allowing it to effectively alleviate allergic symptoms. This compound is capable of crossing the blood-brain barrier, making it valuable in neurological studies and research focused on central nervous system effects. Its diverse applications also include exploration in pharmacology and behavioral research involving sedative effects. -
Serotonin Receptor Antagonist
Trazodone is a triazolopyridine derivative that primarily functions as a serotonin receptor antagonist and reuptake inhibitor. It exhibits significant antidepressant and sleep-inducing activities, making it valuable in the study of mood disorders and insomnia. Additionally, Trazodone demonstrates antagonistic effects on α1- and α2-adrenergic receptors as well as histamine H1 receptors, while displaying minimal anticholinergic activity. -
Histamine 1 Receptor Blocker
Ketotifen is an orally active second-generation noncompetitive antagonist of the histamine H1 receptor, known for its role as a mast cell stabilizer. It exhibits significant biological activity by inhibiting 6-phosphogluconate dehydrogenase in vitro and displays antiviral properties against SARS-CoV-2 and the Influenza virus. Ketotifen is applicable in research focused on autoimmune encephalomyelitis (EAE) and contributes to studies aimed at preventing asthma attacks. -
Histamine Receptor Antagonist
Levocetirizine is a third-generation peripheral histamine H1-receptor antagonist. As the R-enantiomer of Cetirizine, it demonstrates a higher binding affinity for the H1 receptor compared to its S counterpart. Levocetirizine is primarily utilized in the management of allergic rhinitis and chronic idiopathic urticaria, providing effective relief from allergy-related symptoms. Its efficacy makes it a valuable tool in related pharmacological research. -
H1R-H4R Agonist
Amthamine dihydrobromide is an agonist of the histamine receptors H1R to H4R. This compound has been shown to induce liver congestion and necrosis of hepatocytes, providing a valuable model for studying the hepatotoxic effects associated with H1R-H4R activation. It is suitable for research applications focused on the roles of these receptors in liver function and pathology. -
Anti-histamine
Chlorpheniramine is an H1 antihistamine that primarily targets histamine receptors to alleviate symptoms associated with allergic reactions. It exhibits significant efficacy in reducing peripheral and central histamine-induced effects, making it a valuable tool in the study of allergic diseases and related pathophysiological processes. This compound is widely utilized in research applications focusing on allergy management and pharmacological interventions.

