Catalog No.
Product Name
Application
Product Information
Citations
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GLP-1 Receptor Agonist
GLP-1R Agonist 13 is a selective agonist of the GLP-1 receptor, which plays a crucial role in glucose metabolism and appetite regulation. This compound exhibits potent biological activity by enhancing insulin secretion and inhibiting glucagon release, making it a valuable tool for diabetes research. Its application extends to studying metabolic disorders and evaluating potential therapeutic strategies for conditions such as type 2 diabetes and obesity. -
Glucagon Peptide
(Asp28)-Glucagon (1-29) is a modified form of the glucagon peptide, where aspartic acid (Asp) has been introduced at position 28 to enhance its aqueous solubility in physiological pH buffers. This structural optimization preserves the biological activity characteristic of glucagon. It serves as a valuable reagent for research applications that investigate glucagon's role in glucose metabolism, diabetes, and other metabolic disorders in human, rat, and porcine models. -
GLP-1 Agonist
GLP-1 Receptor Agonist 16 is a potent agonist of the GLP-1 receptor, primarily involved in regulating glucose metabolism and appetite. This compound demonstrates significant biological activity in modulating insulin secretion and promoting weight loss. It is particularly valuable in research focused on diabetes, obesity, and nonalcoholic steatohepatitis-related conditions. -
GLP-1R Agonist
GLP-1R agonist 30 is a highly selective and orally active agonist of the glucagon-like peptide-1 receptor (GLP-1R), demonstrating an EC50 of 0.048 nM. It displays significant selectivity with EC50 values greater than 20 μM for GLP-2 receptor, GIP receptor, and glucagon receptor. This compound enhances cAMP signaling while minimizing hERG inhibition, indicating favorable safety profiles. It effectively improves glucose tolerance and promotes insulin secretion in B-hGLP1R knock-in mouse models, making it a valuable tool for research applications in diabetes and metabolic disorders. -
GLP-1R/GIPR Agonist
Brenipatide is a dual agonist of the glucagon-like peptide-1 (GLP-1) receptor and the gastric inhibitory polypeptide (GIP) receptor. It is primarily utilized in researching metabolic disorders, obesity, and diabetes, demonstrating significant potential in enhancing insulin secretion and promoting weight loss. This compound is essential for studies investigating the pathways and mechanisms involved in glucose homeostasis and energy balance. -
GLP-1 Receptor Agonit
Utreglutide is a potent glucagon-like peptide-1 (GLP-1) receptor agonist that plays a significant role in the regulation of glucose metabolism. This compound not only aids in lowering blood pressure and blood lipid levels but also contributes to weight reduction and enhances cardiovascular health. Utreglutide is particularly valuable in research focusing on type 2 diabetes and obesity-related conditions, facilitating a deeper understanding of metabolic disorders. -
GLP-1R Agonist
CHU-128 is a selective GLP-1 receptor (GLP-1R) agonist that effectively activates the Gs/cAMP signaling pathway. This compound is characterized by its strong signal specificity, as it does not engage the Gq/calcium signaling pathway, ERK phosphorylation, or recruit β-inhibitory proteins. CHU-128 is suitable for research applications focused on type 2 diabetes and related metabolic disorders. -
GLP-1 Receptor Positive Allosteric Modulator
GLP-1R agonist 39 is a potent positive allosteric modulator of the GLP-1 receptor. This compound enhances the activity of the GLP-1 receptor, making it valuable for studies related to obesity and type 2 diabetes. Its application in research enables the exploration of therapeutic strategies aimed at metabolic disorders. -
GLP-1R Agonist
GLP-1R agonist 38 is a selective agonist of the glucagon-like peptide-1 receptor (GLP-1R). This compound exhibits significant biological activity in enhancing insulin secretion, suppressing glucagon release, and promoting weight reduction, making it a valuable tool for studying metabolic disorders. It is applicable in research related to type II diabetes mellitus (T2DM), obesity, and non-alcoholic fatty liver disease (NASH). -
GLP-1 Receptor Agonist
GLP-1 Receptor Agonist 18 is a potent GLP-1 receptor agonist with an EC50 of 0.22 nM. This compound demonstrates significant biological activity by lowering blood glucose levels and promoting weight loss, making it valuable for diabetes research. Its efficacy in modulating GLP-1 receptor signaling positions it as a useful tool for investigating therapeutic strategies in metabolic disorders. -
GLP-1R Agonist
GLP-1R agonist 26 is a potent agonist of the glucagon-like peptide-1 receptor (GLP-1R), exhibiting an EC50 of less than 10 nM. This compound plays a crucial role in enhancing insulin secretion, promoting weight loss, and exhibiting cardioprotective effects. It is primarily utilized in research focused on metabolic disorders, diabetes, and obesity treatment. -
GLP-1R Agonist
GLP-1R agonist 29 is a potent agonist of the GLP-1 receptor, effectively stimulating cAMP production with an EC50 value of 0.018 nM. This compound demonstrates favorable pharmacokinetic properties, evidenced by a robust body exposure reflected in an AUC0-∞,sc of 77688 ng·h/mL. It serves as a valuable tool for research applications related to metabolic disorders and diabetes, allowing for exploration of GLP-1R signaling pathways. -
GLP-1R Agonist
GLP-1R Agonist 25 is a selective agonist for the glucagon-like peptide-1 receptor (GLP-1R), exhibiting an EC50 value of 0.167 nM. This compound plays a crucial role in stimulating insulin secretion and regulating glucose metabolism, making it a valuable tool for research focused on type II diabetes and related metabolic disorders. Its potent biological activity supports the exploration of therapeutic strategies aimed at improving glycemic control. -
GPR120 Agonist
AZ13581837 is a potent GPR120 agonist, demonstrating human and mouse EC50 values of 5.2 nM and 4.3 nM, respectively. This compound activates Gαq, Gαs, and β-arrestin signaling pathways, effectively reducing cAMP levels, stimulating GLP-1 secretion, promoting glucose lowering, and enhancing insulin secretion. AZ13581837 is valuable for research related to type 2 diabetes, providing insights into potential therapeutic strategies targeting metabolic disorders. -
GPR119 Agonist
AS1269574 is a potent agonist of GPR119, exhibiting an EC50 of 2.5 μM in HEK293 cells expressing the human receptor. This compound activates TRPA1 cation channels, thereby facilitating the secretion of glucagon-like peptide-1 (GLP-1). Notably, AS1269574 induces glucose-dependent insulin secretion from pancreatic β-cells exclusively under high-glucose conditions, making it a valuable tool for research into type 2 diabetes. -
GPR119 Agonist
K-833 is a potent GPR119 agonist with EC50 values of 39.8 nM in humans, 100 nM in mice, 75.4 nM in rats, and 12.6 nM in dogs. This compound enhances GLP-1 secretion and exhibits a synergistic effect on GLP-1 levels when administered alongside AM-5262 in acute gut peptide secretion assays in mice. K-833 is suitable for research focusing on weight loss and metabolic regulation. -
H1R Antagonist
Fexofenadine Impurity F is a derivative of Fexofenadine, primarily acting as a histamine H1 receptor (H1R) antagonist. This compound exhibits biological activity associated with anti-allergic properties, making it relevant in the study of allergic reactions and potential therapeutic interventions for conditions such as seasonal allergic rhinitis and chronic idiopathic urticaria. It serves as a useful reagent for research in drug development and impurity profiling. -
Active Metabolite of Cannabinol
11-Hydroxy cannabinol is an active metabolite of Cannabinol, primarily targeting cannabinoid receptors in the endocannabinoid system. This compound exhibits biological activity that may influence numerous physiological processes, including pain modulation and anti-inflammatory effects. It is utilized in preclinical research to explore therapeutic applications related to cannabinoid signaling pathways and their potential impact on various health conditions. -
Xylazine Metabolite
2,6-Dimethylphenylthiourea is a metabolite of xylazine, an established α2-adrenergic agonist. This compound serves as a valuable tool in pharmacological research, specifically in studies examining the metabolic pathways of xylazine and its effects on α2-adrenergic receptors. It provides insights into its pharmacokinetics and potential physiological implications. -
Adenosine A2A Receptor Inhibitor
4-Desmethyl Istradefylline is a selective adenosine A2A receptor antagonist, serving as a significant metabolite of Istradefylline. With a Ki of 2.2 nM, it demonstrates potent inhibition of the A2A receptor, making it relevant for exploring therapeutic strategies in Parkinson's disease and related neurological disorders. Its oral bioactivity allows for convenience in in vivo research applications targeting adenosine signaling pathways. -
Stable Isotope
Quetiapine Sulfoxide-d8 is a deuterated analog of Quetiapine sulfoxide, a primary metabolite of the second-generation antipsychotic Quetiapine. This compound acts as a 5-HT receptor agonist and dopamine receptor antagonist, playing a critical role in the pharmacokinetic studies of Quetiapine metabolism. Quetiapine Sulfoxide-d8 is commonly utilized in research applications involving drug metabolism, pharmacology, and analytical chemistry, particularly in the development and validation of quantitation methods in biological samples. -
Pergolide Metabolite
Pergolide sulfone is a metabolite of Pergolide, primarily acting as a dopamine receptor agonist. This compound exhibits significant dopaminergic activity, making it relevant for research into Parkinson's disease and other neurological disorders. Pergolide sulfone can be utilized in studies investigating the pharmacological profiles of dopamine receptor interactions and their implications in neurodegenerative conditions. -
Drug Derivative
(±)-p-Fluoro pseudoephedrine hydrochloride is a drug derivative associated with the pharmacological activity of pseudoephedrine. This compound exhibits decongestant properties, primarily functioning as a sympathomimetic agent that influences adrenergic receptors. Its biological activity is employed in studies related to respiratory distress, providing valuable insights into drug metabolism and therapeutic efficacy in treatments for nasal congestion. -
MMB-CHMICA Metabolite
MMB-ICA is a metabolite of MMB-CHMICA, primarily targeting the cannabinoid receptor system. This compound demonstrates significant biological activity in modulating receptor signaling pathways, making it valuable for research in cannabinoid pharmacology. MMB-ICA is utilized in studies investigating the therapeutic potential of cannabinoids and their metabolic pathways. -
PB-22 Metabolite
PB-22 N-(5-Hydroxypentyl)-3-carboxyindole metabolite is a primary metabolite of the cannabinoid PB-22. This compound exhibits biological activity through its interaction with the endocannabinoid system, influencing cannabinoid receptor signaling pathways. It is utilized in research to explore the metabolic pathways of synthetic cannabinoids and their pharmacological effects in various biological systems. -
Drug Metabolite
Reduced Haloperidol, a primary metabolite of Haloperidol, functions as a dopamine receptor antagonist. It exhibits significant antipsychotic activity, primarily utilized in research related to schizophrenia and other psychotic disorders. This compound is instrumental in studies investigating the modulation of neurotransmitter systems, aiding in the reduction of hallucinations and delusions associated with these conditions. -
Clonidine Metabolite
4-Hydroxyclonidine is a metabolite of Clonidine, primarily functioning as an alpha-2 adrenergic agonist. It exhibits comparable potency to Clonidine in displacing labeled Clonidine from specific antibodies. This compound is of significant interest in pharmacological research, particularly in studies examining adrenergic receptor interactions and the metabolic pathways of antihypertensive agents. -
Propranolol Active Metabolite
Norpropranolol hydrochloride is the active metabolite of Propranolol, primarily targeting beta-adrenergic receptors. It exhibits significant cardiovascular effects, including the reduction of heart rate and blood pressure. This compound is used in research applications focused on studying cardiovascular pharmacology and the modulation of stress response pathways. -
Bufuralol Metabolite
4-Hydroxybufuralol is a primary metabolite of Bufuralol, known for its significant role in pharmacokinetics. It exhibits interactions with beta-adrenergic receptors, contributing to cardiovascular research applications. This compound is essential for studies focused on drug metabolism and the pharmacological effects of beta-blockers. -
PB-22 Metabolite
PB-22 N-(4-Hydroxypentyl)-3-carboxyindole metabolite is a significant metabolite of the synthetic cannabinoid PB-22. This compound interacts primarily with cannabinoid receptors, influencing cannabinoid signaling pathways. It is valuable for research applications focused on studying the metabolism and pharmacological effects of cannabinoids, as well as providing insights into potential therapeutic uses and regulatory impacts associated with cannabinoid exposure. -
Alprenolol Metabolite
4-Hydroxyalprenolol is a metabolite of the β-receptor blocker Alprenolol, known for its role in modulating adrenergic signaling. This compound exhibits biological activity related to cardiovascular function and may be utilized in research focused on the pharmacokinetics and pharmacodynamics of β-blockers. Its analysis can provide insights into the metabolism of therapeutic agents and their effects on β-adrenergic receptors. -
MMB-CHMICA Metabolite
AB-INACA is a metabolite of the synthetic cannabinoid AB-CHMINACA, acting primarily on the cannabinoid receptors. This compound has been utilized in research to investigate synthetic cannabinoid metabolism and receptor interaction dynamics. Its biological activity provides valuable insights into the pharmacological pathways of synthetic cannabinoids, making it a useful tool for toxicological studies and drug metabolism research. -
5-HT Metabolite
5-Hydroxy NMT oxalate is a metabolite of serotonin (5-HT) that functions as a neuromodulator. This compound has been implicated in various neurophysiological processes and is associated with cocaine addiction, as elevated plasma levels have been observed in affected individuals. Its utility in research extends to the study of serotonergic signaling pathways and addiction-related behaviors. -
Platelet Aggregation Inhibitor
U-51605 is a platelet aggregation inhibitor that targets thromboxane synthesis. It also functions as a prostaglandin I2 synthase inhibitor and has been shown to block retinal vasodilation responses induced by nitric oxide donors like NOR3. This reagent is valuable for research applications focusing on cardiovascular health and vascular biology. -
S1P₁ Agonist
PPI-4955 is a selective agonist of the sphingosine-1-phosphate receptor subtype 1 (S1P₁), displaying an EC50 of 1.62 nM. Its active phosphorylated form, PPI-4955-P, demonstrates exceptional receptor selectivity, with IC50 values of 0.23 nM for hS1P₁, 2000 nM for hS1P₃, 6.5 nM for hS1P₄, and 184 nM for hS1P₅. This compound significantly enhances in vivo phosphorylation efficiency, leading to lymphocyte reduction and a potential decrease in cardiovascular risk. PPI-4955 is applicable for research in immunomodulation and cardiovascular studies. -
A2B Receptor Antagonist
PSB-603 is a potent and highly selective antagonist of the A2B adenosine receptor, exhibiting a Ki value of 0.553 nM. This compound demonstrates minimal affinity for human and rat A1, A2A, and human A3 receptors at concentrations up to 10 μM. PSB-603 is primarily utilized in research exploring adenosine receptor signaling pathways and their implications in various physiological and pathological processes. -
Adenosine A3 Receptor Antagonist
MRS 1523 is a selective antagonist of the adenosine A3 receptor, demonstrating Ki values of 18.9 nM and 113 nM for human and rat A3 receptors, respectively. It exhibits significant selectivity with 140-fold and 18-fold greater affinity for the A3 receptor over A1 and A2A receptors in rat models. MRS 1523 has been shown to produce an antihyperalgesic effect by blocking N-type calcium channels and inhibiting action potentials in isolated rat dorsal root ganglion (DRG) neurons, making it valuable for research in pain mechanisms and receptor activity. -
A2B Adenosine Receptor Antagonist
PSB-1115 is a selective antagonist of the A2B adenosine receptor, providing a valuable tool for investigating adenosine signaling pathways. It effectively inhibits the contraction induced by 2,4,6-trinitrobenzenesulfonic acid (TNBS) in response to acetylcholine (ACh). This compound is relevant for research in inflammation, smooth muscle function, and potential therapeutic interventions targeting adenosine receptors. -
A3 Adenosine Receptor Antagonist
DPTN dihydrochloride is a potent and selective antagonist of the A3 adenosine receptor (A3AR), exhibiting Ki values of 1.65 nM for human, 9.61 nM for mouse, and 8.53 nM for rat receptors. This compound is valuable for research applications investigating the physiological roles of A3AR in various biological processes, including immunomodulation and tumor growth regulation. DPTN's selectivity makes it an important tool for studies aimed at elucidating the therapeutic potential of A3AR modulation in human and animal models. -
A3 Receptor Antagonist
MRS1220 is a highly potent and selective antagonist of the human A3 adenosine receptor (hA3AR), exhibiting a Ki value of 0.59 nM. This compound is of significant interest for research related to diseases of the central nervous system and has demonstrated the ability to reduce glioblastoma tumor size and inhibit angiogenesis in vivo. Its distinct action on the A3 receptor makes it a valuable tool for studying mechanisms associated with neuroprotection and tumor biology. -
GPCRs/Adenosine Modulator
SCH-202676 hydrobromide is an allosteric modulator targeting G protein-coupled receptors (GPCRs), specifically the adenosine receptor. This compound demonstrates notable antiviral activity and effectively inhibits the 3CLpro enzyme in a time-dependent manner, with an IC50 value of 0.655 μM. Its unique mechanism makes it a valuable reagent for research applications focused on GPCR modulation and antiviral studies. -
Adenosine Receptor Activator
Adenosine-2'-monophosphate (2'-AMP) functions primarily as an adenosine receptor activator. This compound is metabolized to extracellular adenosine through the extracellular 2’,3’-cAMP-adenosine pathway, playing a crucial role in modulating immune responses. Research indicates that 2'-AMP inhibits lipopolysaccharide (LPS)-induced production of TNF-α and CXCL10 via activation of the A2A receptor, making it a valuable tool in studies of inflammation and immune regulation. -
Adenosine Receptor Antagonist
7-Methylxanthine is a non-selective adenosine receptor antagonist that serves as an orally active methyl derivative of xanthine. This compound has demonstrated key biological activities, including anti-myopia effects, making it valuable for research in visual function and ocular health. Additionally, 7-Methylxanthine is a component of human urinary calculi, highlighting its relevance in studies related to purine metabolism and urolithiasis. -
A2A Receptor Antagonist
Inupadenant is a potent and selective antagonist of the A2A adenosine receptor, primarily utilized for its immunomodulatory effects. This compound enhances the humoral immune response and exhibits promising anti-tumor activity, making it a valuable tool in cancer research and immune response studies. Notably, Inupadenant does not penetrate the blood-brain barrier, which may limit its central nervous system effects. -
A2A Inverse Agonist
Sipagladenant is an orally active inverse agonist of the adenosine A2A receptor. It is primarily utilized in research related to frontal lobe dysfunction, offering insights into the modulation of adenosine signaling pathways. This compound may be useful in elucidating the role of A2A receptors in various neurological conditions. -
A1 Adenosine Receptor Antagonist
PSB36 is a selective antagonist of the A1 adenosine receptor, exhibiting a Ki of 0.12 nM and Kd of 0.7 nM. This compound has demonstrated efficacy in reducing formalin- and carrageenan-induced edema in murine models, alongside a decrease in pain-related behaviors without causing local paw effects. Furthermore, PSB36 prolongs the action potential duration (APD90) of rat and human atria, enhances frequency-dependent atrial effective refractory period (ERP), raises diastolic thresholds, and mitigates the duration of atrial fibrillation episodes. PSB36 is applicable in research investigating inflammatory pain, hyperalgesia, edema, and atrial fibrillation. -
Adenosine A2A Receptor Antagonist
(E)-8-(3-Chlorostyryl)caffeine is a selective antagonist of the adenosine A2A receptor, which plays a significant role in neuronal signaling. In addition to its primary action, this compound also inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM through a mechanism independent of its effects on the A2A receptor. Due to its dual activity, (E)-8-(3-Chlorostyryl)caffeine is of particular interest in research related to Parkinson's disease and other neurological disorders. -
A2AAR Agonist
UK-432097 is a highly potent and selective agonist of the A2A adenosine receptor (A2AAR), exhibiting a pKi of 8.4 for human A2AAR. This compound demonstrates significant anti-inflammatory and anti-aggregatory properties, making it a valuable tool for studying inflammatory pathways. UK-432097 is particularly relevant for research applications related to chronic obstructive pulmonary disease (COPD) and other conditions influenced by A2A receptor signaling. -
A2BAR Antagonist
ISAM-140 is a potent and selective antagonist of the A2B adenosine receptor, exhibiting a Ki of 3.49 nM. This compound is valuable for research applications focused on adenosine signaling pathways and their role in various physiological processes. Its high specificity makes it an essential tool for studying the therapeutic potential of A2B receptor modulation in disease models. -
Adenosine Receptor Agonist
(-)-N6-Phenylisopropyl adenosine is a selective agonist for the A1 adenosine receptor. This compound effectively inhibits K+-induced Ca2+ uptake with an IC50 of 0.5 µM. It has been shown to protect against ischemia-induced ventricular arrhythmias and atrial fibrillation, while also exacerbating symptoms associated with ethanol withdrawal. Additionally, (-)-N6-phenylisopropyl adenosine exhibits notable analgesic properties, making it a valuable tool for research in cardiovascular and pain-related studies.
