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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. -
GLP-1R Modulator
GPCR modulator-1 is a negative allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R). This compound demonstrates key biological activity by modulating receptor signaling, making it valuable for investigating the role of GLP-1R in type 2 diabetes research. GPCR modulator-1 can facilitate studies aimed at understanding metabolic processes and potential therapeutic interventions for diabetes-related complications. -
GLP-1R Agonist
GLP-1R Agonist 4 is a potent agonist of the glucagon-like peptide-1 receptor (GLP-1R), which is crucial for glucose homeostasis and insulin secretion. As a GLP-1R agonist, it mimics the effects of endogenous GLP-1, promoting insulin release in response to elevated blood glucose levels. This compound has significant potential for research applications in diabetes management, particularly in elucidating the mechanisms of GLP-1 signaling and its therapeutic implications. -
GLP-2 Receptor Agonist
Elsiglutide is a selective GLP-2 receptor agonist that functions as a GLP-2 analogue. It promotes intestinal cell proliferation and decreases apoptosis, demonstrating utility in gastrointestinal research. Additionally, Elsiglutide has been shown to mitigate diarrhea induced by Lapatinib in preclinical rodent models, making it a potential candidate for studies focused on enhancing gut health and managing drug side effects. -
GLP-1 Receptor Antagonist
Exendin (5-39) is a selective glucagon-like peptide 1 (GLP-1) receptor antagonist. This compound has been shown to effectively ameliorate memory impairment in β-amyloid protein-treated rodents, making it a valuable tool for studying cognitive decline and neurodegenerative diseases. Its ability to modulate GLP-1 signaling pathways positions Exendin (5-39) as a useful reagent in research focused on metabolic disorders and brain function. -
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. -
GLP-1/Gastrine Agonist
ZP3022 is a dual agonist of glucagon-like peptide-1 (GLP-1) and gastrin, demonstrating significant potential in improving glycemic control. This compound has been shown to effectively increase β-cell mass, promote β-cell proliferation, and enhance pancreatic islet function. ZP3022 is a valuable tool for research in anti-diabetic therapies and the exploration of metabolic regulation. -
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. -
GLP-1R Agonist
GLP-1R agonist 9 is a potent agonist of the glucagon-like peptide-1 receptor (GLP-1R), demonstrating EC50 values of 1.1 nM and 11 nM in CHO GLP-1R Clone H6 and CHO GLP-1R Clone C6, respectively. This compound exhibits significant biological activity in stimulating insulin secretion, making it a valuable tool in diabetes research. Its efficacy in modulating GLP-1R offers potential applications in studying metabolic disorders and developing therapeutic agents for glucose regulation. -
GLP-1 Receptor Agonist
Cochinchinenin C is a nonpolypeptide agonist of the glucagon-like peptide-1 (GLP-1) receptor. This compound exhibits significant biological activity in stimulating insulin secretion and inhibiting glucagon release, making it a valuable tool for diabetes research. Its ability to modulate glucose homeostasis positions Cochinchinenin C as a potential candidate for therapeutic applications in metabolic disorders. -
GLP-1 Receptor Agonist
PF-06954522 citrate is an orally active agonist of the GLP-1 receptor. It plays a significant role in regulating glucose metabolism and promoting insulin secretion, making it a valuable tool for investigating type 2 diabetes mellitus. This compound is particularly relevant for studying the mechanisms underlying glucose homeostasis and potential therapeutic strategies for diabetic conditions. -
LSN3318839 Stereoisomer
(S,R)-LSN3318839 is a stereoisomer of LSN3318839, functioning as a positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R). This compound enhances insulin secretion and exhibits hypoglycemic effects, making it a valuable reagent for research into diabetes and metabolic disorders. Its oral bioactivity positions it as a promising candidate for studies focused on glucose homeostasis andtherapeutic interventions. -
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. -
GLP-1R Agonist
DA-302168S is a selective agonist of the glucagon-like peptide-1 receptor (GLP-1R), exhibiting an EC50 value of 1.32 nM. This compound effectively stimulates insulin secretion and demonstrates hypoglycemic effects while decreasing food intake. DA-302168S primarily targets GLP-1R in primates and humans, with minimal activity observed in rodent and canine models. It is a valuable tool for research in type 2 diabetes and obesity. -
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. -
GLP-1 R Agonist
GLP-1 receptor agonist 8 is a potent agonist targeting the glucagon-like peptide-1 receptor (GLP-1 R). This compound demonstrates significant biological activity in promoting insulin secretion and regulating appetite, making it relevant for research applications in diabetes, obesity, and nonalcoholic fatty liver disease (NAFLD). Its pharmacological properties provide valuable insights into metabolic disorders and potential therapeutic strategies. -
GLP-1 Analogue
A8SGLP-1 is an orally active GLP-1 analogue with a serine substitution at position 8. This compound demonstrates key biological activity by effectively reducing blood glucose levels in db/db mouse models while maintaining endogenous GLP-1 function. A8SGLP-1 is designed for research applications in diabetes and metabolic disorder studies, providing valuable insights into GLP-1 receptor modulation and therapeutic potential. -
GLP-1R Agonist
GLP-1R agonist 7 is a potent agonist of the glucagon-like peptide-1 receptor (GLP-1R), characterized by an EC50 of 0.67 µM. This compound plays a significant role in modulating glucose metabolism and is instrumental in diabetes research. Its ability to stimulate insulin secretion and inhibit glucagon release makes it a valuable tool for investigating therapeutic approaches to metabolic disorders. -
Peptide
Exendin-4 (3-39) is a peptide that functions as a selective agonist for the Glucagon-like peptide-1 receptor (GLP-1r). This truncated variant of Exendin-4 is missing the first two amino acids, while retaining its bioactivity. Exendin-4 (3-39) is primarily employed in research exploring metabolic diseases, diabetes, and the hypothalamic-pituitary-adrenal (HPA) axis. Its structural modifications allow for investigations into receptor interactions and signaling pathways related to GLP-1r. -
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. -
GLP-1R Agonist
GLP-1R agonist 6 is a potent agonist of the GLP-1 receptor, exhibiting an EC50 of 0.15 nM for human GLP-1R. This compound demonstrates significant biological activity in promoting insulin secretion and glucose homeostasis, making it a valuable tool for research in diabetes and metabolic disorders. Its efficacy in activating GLP-1R positions it as a key reagent for exploring therapeutic strategies targeting glucose regulation and appetite control. -
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. -
GLP-1R Agonist
GLP-1R agonist 8 is a highly potent agonist of the glucagon-like peptide-1 receptor (GLP-1R), exhibiting an EC50 of less than 2 nM. This compound is instrumental in stimulating insulin secretion and regulating glucose homeostasis, making it a valuable tool in diabetes research and therapeutic development. Its efficacy in enhancing GLP-1R activity underscores its potential for studying metabolic diseases and investigating the physiological roles of GLP-1 signaling pathways. -
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. -
GIP/GLP-1 dual receptor Agonist
GIP/GLP-1 dual receptor agonist-1 is an agonist targeting both GIP and GLP-1 receptors. It exhibits significant biological activity in modulating glucose metabolism and promoting insulin secretion. This reagent is instrumental in research focused on metabolic disorders, particularly non-alcoholic steatohepatitis (NASH) and non-alcoholic fatty liver disease (NAFLD). -
GLP-1R Agonist
GLP-1R Agonist 1 is a potent agonist targeting the glucagon-like peptide-1 receptor (GLP-1R). Acting as an imidazole derivative, this compound promotes insulin secretion while inhibiting glucagon release, making it a valuable tool in diabetes research. Its mechanism of action supports the investigation of therapies aimed at managing blood glucose levels and enhancing glycemic control. -
GLP-1 Receptor Agonist
TT-OAD2 free base is a non-peptide agonist of the glucagon-like peptide-1 (GLP-1) receptor, exhibiting an EC50 of 5 nM. This compound demonstrates significant potential in the treatment of diabetes by enhancing insulin secretion and regulating blood glucose levels. Its applications extend to research investigating GLP-1 signaling pathways and the development of novel therapeutic strategies for metabolic disorders. -
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. -
GLP-1R Agonist
GLP-1R agonist 31 is a potent glucagon-like peptide-1 receptor (GLP-1R) agonist. This compound exhibits significant activity in enhancing insulin secretion and promoting glucose-dependent effects, making it valuable in diabetes research. It can be utilized in studies related to metabolic disorders and the development of GLP-1-based therapies. -
GLP-1R Agonist
GLP-1R Agonist 5 is a highly potent agonist of the GLP-1 receptor, exhibiting an EC50 of less than 10 nM. This compound demonstrates significant biological activity in promoting insulin secretion and aiding in glucose homeostasis. It is a valuable tool for research applications focused on metabolic disorders, diabetes, and related therapeutic targets. -
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. -
Stable Isotope
GLP-1 receptor agonist 17-d3 is a deuterium-labeled compound that targets the GLP-1 receptor, serving as a critical tool in the study of GLP-1 receptor activation. This isotopically enriched agonist plays a significant role in the investigation of cardiovascular and metabolic diseases, providing insights into GLP-1 signaling pathways and their therapeutic implications. Its unique labeling allows for enhanced tracking and identification in biological assays, facilitating advanced research in the field of metabolic health. -
GCGR Antagonist
GCGR Antagonist 3 targets the glucagon receptor (GCGR) and functions as a potent antagonist. This compound plays a critical role in diabetes research by inhibiting glucagon signaling, which may aid in the investigation of glucose homeostasis and metabolic disorders. Its application in preclinical studies offers valuable insights into potential therapeutic strategies for diabetes management. -
Glucagon Receptor Antagonist
[Des-His1,Glu9] Glucagon is a potent antagonist of the glucagon receptor, effectively inhibiting glucagon's biological activity. This peptide enhances glucose-stimulated insulin secretion from pancreatic islet cells, making it a valuable tool for studying insulin regulation. [Des-His1,Glu9] Glucagon is particularly relevant in diabetes research, aiding in the exploration of therapeutic strategies targeting glucose homeostasis and pancreatic function. -
GLP-1R Agonist
GLP-1R agonist 32 is a potent and selective agonist of the GLP-1 receptor, demonstrating an EC50 of 0.017 nM. Its mechanism involves the stimulation of cAMP production, which enhances insulin secretion, suppresses glucagon release, and slows gastric emptying. This compound holds significant promise for investigating therapeutic strategies in type 2 diabetes, obesity, and associated metabolic disorders. -
Glucagon Receptor Antagonist
Glucagon receptor antagonist-9 is a potent antagonist of the glucagon receptor, exhibiting a pIC50 of 7.000. This compound effectively inhibits glucagon signaling, which plays a critical role in glucose metabolism and homeostasis. Its application in research includes the study of metabolic disorders, diabetes, and potential therapeutic strategies targeting glucagon pathways. -
Glucagon receptor antagonist inactive control
Glucagon receptor antagonist inactive control is a compound designed to serve as a structural analog to the glucagon receptor (GCGR) antagonist, but it lacks the active antagonistic properties against GCGR. This inactive control compound is ideal for use in experiments aimed at elucidating the mechanisms associated with GCGR-mediated signaling pathways, providing a valuable comparison to active antagonists in research settings. Its application helps ensure accurate interpretation of results in studies related to glucagon receptor function. -
Glucagon Receptor Antagonist
Glucagon receptor antagonist-11 is a selective antagonist of the glucagon receptor with a pIC50 of 6.677. This compound plays a critical role in studies related to glucose homeostasis and insulin sensitivity, making it a valuable tool for exploring metabolic disorders. Its inhibitory effect on glucagon signaling can be leveraged in research focused on diabetes, obesity, and related metabolic diseases. -
hGCGR Antagonist
SCH 900822 is a potent and selective antagonist of the human glucagon receptor (hGCGR). By inhibiting the binding of glucagon to its receptor, it effectively reduces hepatic glycogenolysis and gluconeogenesis, leading to decreased blood glucose production. This compound is primarily utilized in research related to type 2 diabetes, providing insights into potential therapeutic interventions for managing hyperglycemia. -
GCGR Antagonist
LGD-6972 sodium is a selective antagonist of the glucagon receptor (GCGR), exhibiting oral bioavailability. This compound demonstrates significant potential in the research of type 2 diabetes by modulating glucose metabolism and insulin sensitivity. Its application in studying glucagon-mediated pathways underscores its importance in metabolic disease research. -
GLP-1R Agonist
Danuglipron tromethamine is an orally active glucagon-like peptide-1 receptor (GLP-1R) agonist. This compound exhibits significant biological activity in promoting insulin secretion and suppressing glucagon release, making it a valuable tool for research in type 2 diabetes. Its mechanism of action supports investigations into glucose metabolism and potential therapeutic approaches for managing diabetes-related conditions. -
Glucagon Receptor Antagonist
Glucagon receptor antagonist-10 is a selective antagonist of the glucagon receptor, exhibiting a pIC50 of 7.154. This compound is valuable in investigating the regulation of glucose homeostasis and its implications in metabolic disorders. It serves as a useful tool for researchers studying the pathways involved in glucagon signaling and potential therapeutic approaches to diabetes management. -
GHS-R1a Inverse Agonist
AZ-GHS-38 is an orally active inverse agonist of the growth hormone secretagogue receptor 1a (GHS-R1a), exhibiting an IC50 of 6.7 nM. This compound effectively reduces food intake in wild-type mice, making it a valuable tool for anti-obesity research. Its central nervous system penetration facilitates investigations into the modulation of appetite and energy homeostasis. -
Growth Hormone Secretagogue
L-739943 is a potent, orally active growth hormone (GH) secretagogue that functions by stimulating GH release. With an ED50 value of 1 nM, L-739943 has demonstrated effectiveness in promoting GH secretion in beagle dogs. This compound is useful for investigating GH-related therapeutic applications and understanding GH-mediated physiological processes. -
GHSR Antagonist
YIL781 hydrochloride is a potent antagonist of the ghrelin receptor (GHSR). This compound has been shown to significantly improve glucose homeostasis in rat models, demonstrating its potential in metabolic research. YIL781 hydrochloride effectively inhibits the calcium response triggered by ghrelin, with pIC50 values of 7.90 and 8.27, indicating robust bioactivity in a research context.

