Catalog No.
Product Name
Application
Product Information
Citations
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glucagon receptor antagonist
Glucagon receptor antagonists-1 is a highly potent glucagon receptor antagonist. -
Glucagon receptor antagonist
Glucagon receptor antagonists-2 is a highly potent glucagon receptor antagonist. -
Glucagon receptor antagonist
Glucagon receptor antagonists-3 is a highly potent glucagon receptor antagonist. - Glucagon-Like Peptide 1 (7-36) Amide is a potent glucose-dependent insulinotropic peptide produced by post-translational processing of proglucagon in intestinal L-cells.
- Ying Zhou, .et al. , Adv Biol (Weinh), 2022, Nov 14 PMID: 36373695
- Glucagon is a peptide hormone, produced by alpha cells of the pancreas. It works to raise the concentration of glucose in the bloodstream. Its effect is opposite that of insulin, which lowers the glucose.
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glucagon receptor antagonist
PF-06291874 (Glucagon receptor antagonists-4) is a highly potent and orally active glucagon receptor antagonist. It displays low in vivo clearance in both rats and dogs. -
glucagon receptor antagonist
Adomeglivant is a potent and selective glucagon receptor antagonist that is used in clinical trial for type 2 diabetes mellitus. -
glucagon-like peptide 1 receptor antagonist
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM. -
glucagon-like peptide-1 receptor agonist
Exendin-4 Acetate (Exenatide acetate), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM. -
GLP-1R agonist
PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor agonist (GLP-1R) -
Glucagon receptor agonist
Retatrutide (LY3437943) is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide binds human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide can be used for the research of obesity. -
VPAC2 agonist
Bay 55-9837 is a potent and highly selective agonist of VPAC2, with a Kd of 0.65 nM. Bay 55-9837 may be a useful therapy for the research of type 2 diabetes. -
GLP-2R agonist
Glepaglutide (ZP1848) is a long-acting glucagon-like peptide-2 (GLP-2) analogue and a potent agonist of the GLP-2 receptor (GLP-2R). It enhances intestinal absorption, reduces faecal output, and alleviates small intestinal inflammation. Glepaglutide is a valuable agent for research in inflammatory bowel disease (IBD), including Crohn’s disease. -
GCGR Antagonist
Glucagon receptor antagonist-8 is a selective antagonist of the human glucagon receptor (GCGR) and p38 mitogen-activated protein (MAP) kinase. It exhibits IC50 values of 0.27 μM for GCGR and 0.16 μM for p38 MAP kinase, demonstrating significant inhibitory activity. This compound is applicable in research focused on metabolic disorders, glucose homeostasis, and signaling pathways associated with glucagon activity. -
Glucagon-binding Fluorescent Probe
BD-105 is a glucagon-binding fluorescent probe with a dissociation constant (Ka) of 13.3 μM. This reagent displays significant changes in fluorescence intensity upon binding to glucagon, enabling the visualization of glucagon-secreting cells in various biological contexts. BD-105 selectively labels these cells while avoiding staining of insulin-secreting and non-endocrine control cells. It is an invaluable tool for imaging glucagon in live cells and tissues, facilitating studies in metabolic regulation and endocrine functions. -
GCGR Antagonist
Glucagon receptor antagonist-7 is a potent inhibitor of the human glucagon receptor (hGCGR), demonstrating an IC50 of 181 nM for blocking the binding of 125I-labeled glucagon. With a KDB of 81 nM, it inhibits glucagon-stimulated adenylyl cyclase activity in CHO cells. This compound effectively reduces glucagon-mediated glycogenolysis in human hepatocytes and has been shown to lower blood glucose levels, making it a valuable tool for research in glucose metabolism and diabetes therapeutic strategies. -
GLP-1R/GCGR Agonist
Mazdutide is a long-acting synthetic analog of oxyntomodulin that functions as a dual agonist of the glucagon-like peptide-1 receptor (GLP-1R) and the glucagon receptor (GCGR). By binding to these targets with high affinity (Ki values of 17.7 nM for GCGR and 28.6 nM for GLP-1R in humans), Mazdutide promotes insulin secretion from mouse islets (EC50: 5.2 nM). This compound is primarily utilized in research addressing obesity and type 2 diabetes (T2D) to explore its therapeutic potential and metabolic effects. -
GCGR/GLP-1R Agonist
Survodutide is a potent dual agonist of the glucagon receptor (GCGR) and GLP-1 receptor (GLP-1R), exhibiting EC50 values of 0.52 nM and 0.33 nM, respectively, in CHO-K1 cells. This 29-amino-acid acylated peptide, featuring a C18 fatty acid, demonstrates significant anti-obesity effects through mechanisms that enhance energy expenditure and reduce food intake. Survodutide is valuable for research into metabolic disorders and obesity management. -
GCGR Modulator
LSN3318839 is an orally active positive modulator of the glucagon receptor (GCGR). This compound enhances insulin secretion and exhibits hypoglycemic effects, making it valuable in the study of glucose metabolism and diabetes management. It is suitable for research applications focused on metabolic disorders and endocrine signaling pathways. -
GLP-1/GCGR Agonist
Cotadutide is a potent dual agonist of glucagon-like peptide-1 (GLP-1) and glucagon receptor (GCGR), demonstrating EC50 values of 6.9 pM and 10.2 pM, respectively. This compound effectively promotes weight loss, enhances glycemic control, and alleviates fibrosis. Cotadutide is suitable for research applications focused on obesity and type 2 diabetes (T2D). -
GCGR Agonist
Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist that primarily targets the glucagon receptor (GCGR). It exhibits potent biological activity with an EC50 value of 0.06 nM. This compound is primarily investigated for its therapeutic potential in managing type 2 diabetes, promoting insulin secretion, and regulating glucose metabolism. Research applications include studying metabolic disorders and developing treatments for diabetes-related complications. -
Glucagon Receptor Antagonist
L-168049 is a potent and selective non-competitive antagonist of the glucagon receptor, exhibiting IC50 values of 3.7 nM for human, 63 nM for murine, and 60 nM for canine receptors. This compound serves as a valuable tool for investigating the role of glucagon signaling in metabolic disorders and diabetes research. Its oral bioavailability enhances its utility in various in vivo studies aimed at elucidating glucagon-related pathways. -
GLP-1R/GCGR Agonist
Bamadutide is a potent dual agonist of the glucagon-like peptide-1 receptor (GLP-1R) and the glucagon receptor (GCGR). This compound enhances β-cell function and slows glucose absorption, resulting in improved postprandial blood glucose control. Bamadutide is suitable for research applications focused on metabolic diseases, particularly type 2 diabetes. -
GCGR Modulator
GLP-1R modulator C5 is an allosteric modulator that enhances the binding of GLP-1 to the GLP-1 receptor (GLP-1R) by interacting with a transmembrane site. It exhibits a half-maximal effective concentration (EC50) of 1.59 ± 0.53 μM. This compound is primarily utilized in research focused on diabetes and metabolic disorders, providing valuable insights into GLP-1R signaling pathways and potential therapeutic applications. -
Glucagon Receptor Antagonist
GCGR Antagonist 2 is a furan-2-carbohydrazide that acts as an orally active glucagon receptor antagonist. It shows high binding affinity for the human glucagon receptor (Kd = 2.3 nM) and effectively inhibits the rat glucagon receptor with an IC50 of 0.43 nM. This compound is useful in studies investigating the role of glucagon in metabolic processes, particularly in the inhibition of glucagon-stimulated glycogenolysis. -
GCGR Modulator
GLP-1R modulator L7-028 is an allosteric modulator that enhances the binding of GLP-1 to the GLP-1 receptor (GLP-1R) through a transmembrane site, with an EC50 of 11.01 ± 2.73 μM. This compound is valuable for investigating GLP-1R signaling pathways and its implications in metabolic disorders. Research applications include studies on glucose homeostasis and potential therapeutic strategies for type 2 diabetes and obesity. -
Miniglucagon Agonist
Glucagon (22-29) is a partial agonist of Glucagon (19-29) that targets the glucagon receptor. It is known to specifically inhibit the Ca2+ pump in liver plasma membranes, functioning independently of adenylate cyclase activation. This compound is useful in research applications focused on metabolic regulation and signaling pathways related to glucagon action in hepatocytes. -
Human Glucagon Receptor Antagonist
NNC 92-1687 is a non-peptide competitive antagonist of the human glucagon receptor, exhibiting an IC50 value of 20 μM and a Ki of 9.1 μM. This compound is valuable in the investigation of type 2 diabetes, facilitating research into glucagon signaling pathways and potential therapeutic interventions. Its role in receptor modulation can aid in understanding glucose homeostasis and diabetes-related metabolic processes. -
GCGR Modulator
GLP-1R modulator C16 functions as an allosteric modulator by enhancing the binding affinity of GLP-1 to the GLP-1 receptor (GLP-1R) through a transmembrane site, exhibiting an EC50 of 8.43 ± 3.82 μM. This compound is significant for research on glucose homeostasis and diabetes, enabling studies on GLP-1R signaling pathways and therapeutic applications for metabolic disorders. Its modulation potential aids in understanding GLP-1R pharmacology and its implications in drug development. -
GCGR Agonist
Glucagon-like peptide 1 (1-37), human is a potent agonist of the glucagon receptor (GCGR). This peptide plays a critical role in glucose metabolism and insulin signaling, making it valuable for research in diabetes and metabolic disorders. Its biological activity includes enhancing insulin secretion, inhibiting glucagon release, and promoting satiety, which are important for studies on obesity and diabetes therapies. -
GLP-1R/GCGR Agonist
Pemvidutide is a dual agonist of GLP-1 receptor (GLP-1R) and glucagon receptor (GCGR), exhibiting significant effectiveness in promoting weight loss and reducing liver fat as well as serum lipids. It is primarily utilized in research focusing on non-alcoholic steatohepatitis (NASH) and obesity, making it a valuable tool for understanding metabolic disorders and developing therapeutic strategies. -
Glucagon Receptor Antagonist
Des-His1,Glu9-Glucagon amide is a highly effective peptide antagonist of the glucagon receptor, exhibiting a pA2 of 7.2. This compound plays a significant role in investigating the mechanisms underlying diabetes pathogenesis, making it a valuable tool for research in metabolic disorders. Its ability to modulate glucagon activity allows for deeper insights into glucose regulation and related diseases. -
Glucagon receptor Antagonist
Skyrin is a glucagon receptor antagonist derived from an anthraquinone compound found in almond fruit. This compound selectively inhibits glucagon receptor activity, demonstrating significant potential in regulating glucose metabolism. Research indicates that Skyrin effectively inhibits the growth of tumor cells, making it a valuable tool for studies focused on cancer biology and metabolic disorders. -
GCGR Antagonist
Glucagon receptor antagonist-5 is a selective antagonist for the glucagon receptor (GCGR), exhibiting a Ki value of 32 nM, indicative of its potent inhibitory activity. This indazole-based compound demonstrates significant oral bioavailability, making it a promising candidate for therapeutic intervention in type 2 diabetes mellitus (T2DM). Its mechanism of action highlights its potential in regulating glucose metabolism and insulin sensitivity, making it valuable for research into diabetes-related pathways. -
Glucagon Analog
Dasiglucagon is a human glucagon analog that primarily targets the glucagon receptor. It effectively increases plasma glucose levels, making it a valuable tool in the study of hypoglycemia. This compound is particularly relevant for research focused on glucose metabolism and the physiological responses to low blood sugar conditions. -
GCGR Control
(D-His1)-Exenatide is a characterized impurity of Exenatide, which primarily targets the glucagon receptor (GCGR). This reagent is of interest for studies involving glucagon signaling pathways and metabolic regulation. Its use in research applications can help elucidate the role of glucagon in glucose homeostasis and diabetes-related pathologies. -
GCGR Antagonist
MK-3577 is an orally effective glucagon receptor (GCGR) antagonist that inhibits glucagon signaling, leading to reduced hepatic glucose production and decreased blood glucose levels. This compound is particularly valuable in diabetes research, facilitating studies on glucose metabolism and the management of hyperglycemia. Pharmacokinetic studies in domestic cats demonstrate peak plasma concentrations occurring 3 to 4 hours post-administration, with a half-life of approximately 15 hours, highlighting its potential for sustained therapeutic effects. -
GCGR Antisense Oligonucleotide
ISIS 449884 is a 2'-O-methoxyethyl antisense oligonucleotide that targets the glucagon receptor gene (GCGR). It effectively reduces hepatic glucose output and lowers blood glucose levels, making it a valuable tool for studying type 2 diabetes mellitus (T2DM). This compound is instrumental for researchers investigating the molecular mechanisms underlying glucose metabolism and diabetes pathophysiology. -
GCGR Agonist
GLP-1 receptor agonist 3 (compound (R)-4A-1) serves as a potent agonist of the glucagon-like peptide-1 (GLP-1) receptor, making it a valuable tool in diabetes research. This compound exhibits EC50 values of 1.1 nM and 13 nM in Clone H6 and Clone C6 cell line assays, respectively, demonstrating its efficacy in stimulating GLP-1 receptor activity. Its application in studying metabolic disorders and potential therapeutic strategies for diabetes highlights its significance in the field of endocrinology. -
GCGR Agonist
Neuropeptide Y, porcine, is a peptide found in porcine brain that acts as a GCGR agonist. This compound is known for its ability to inhibit secretin-stimulated pancreatic secretion, making it a valuable tool for studying pancreatic function and regulation. Its applications extend to research on energy homeostasis, appetite regulation, and potential therapeutic interventions in metabolic disorders. -
Modified Glucagon
(Met(O)27)-Glucagon (1-29) is a modified form of glucagon that selectively targets hepatic receptors. This analog retains maximum glucose-synthesizing activity comparable to native glucagon in rat hepatocytes; however, it exhibits reduced potency. The modification at methionine-27 indicates its significance in receptor binding dynamics, making it an essential reagent for studies related to metabolic regulation and glucagon receptor interactions. -
Glucagon Receptor Antagonist
BAY-27-9955 is an orally active non-peptide antagonist of the glucagon receptor. This compound competitively inhibits glucagon binding to the human glucagon receptor with an IC50 of 110 nM. BAY-27-9955 is primarily utilized in research focusing on type 2 diabetes, facilitating studies on metabolic regulation and glucose homeostasis. -
GCGR Agonist
GLP-1 receptor agonist 4 is a glucagon-like peptide-1 receptor (GLP-1R) agonist that serves as an effective activator of the GLP-1 receptor, exhibiting an EC50 of 64.5 nM. This compound plays a significant role in enhancing insulin secretion and promoting glucose homeostasis. GLP-1 receptor agonist 4 is primarily utilized in research focused on diabetes treatment and related metabolic disorders.
