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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. -
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. -
GHSR Antagonist
JMV 2959 is an antagonist of the growth hormone secretagogue receptor type 1a (GHS-R1a), exhibiting an IC50 value of 32 nM. This compound is utilized in research aimed at elucidating the roles of GHS-R1a in growth hormone regulation and metabolic processes. Its potent inhibitory activity makes it a valuable tool for studies related to obesity, metabolic disorders, and the endocrine system. -
GHSR Agonist
Macimorelin acetate is a growth hormone secretagogue receptor (GHSR) agonist that acts orally to stimulate growth hormone (GH) release. This compound is utilized in research related to adult growth hormone deficiency (AGHD) and cancer anorexia-cachexia syndrome (CACS). Its ability to promote GH release makes it a valuable tool for investigating conditions associated with altered GH levels. -
GHSR Antagonist
JMV 2959 hydrochloride is a selective antagonist of the growth hormone secretagogue receptor 1a (GHS-R1a), exhibiting an IC50 of 32±3 nM in LLC-PK1 cellular assays. This compound is valuable for studies investigating the modulation of growth hormone release and its implications in metabolic disorders, obesity, and appetite regulation. Its efficacy as a GHS-R1a antagonist makes it a potent tool for exploring the signaling pathways associated with this receptor. -
Anti-aging Agent, GHSR Activator
Emoghrelin is a ghrelin receptor (GHSR) activator that promotes growth hormone secretion, making it a valuable anti-aging agent. Isolated from the traditional medicinal plant Heshouwu (Polygonum multiflorum), Emoghrelin's mechanism supports various biological activities tied to growth and regeneration processes. This compound is of particular interest in aging research and studies focused on metabolic regulation and endocrine functions. -
GHSR Inverse Agonist
PF-04628935 is a potent inverse agonist of the ghrelin receptor (GHSR) with a reported IC50 of 4.6 nM. It demonstrates oral bioavailability of 43% in rat models and effectively penetrates the blood-brain barrier. This compound is valuable for research applications focused on stress and anxiety, providing insights into the role of ghrelin signaling in these physiological processes. -
GHSR Agonist
Relamorelin is a potent agonist of the growth hormone secretagogue receptor (GHSR), specifically targeting the GHS-1a receptor with a Ki of 0.42 nM. This pentapeptide ghrelin analog exhibits the ability to enhance growth hormone secretion and facilitate gastric emptying. Relamorelin is valuable for research applications in understanding and treating conditions such as cachexia, gastroparesis, and gastrointestinal dysmobility disorders. -
GHSR Agonist
Relamorelin acetate is a selective agonist for the growth hormone secretagogue receptor (GHSR), exhibiting a Ki value of 0.42 nM for the GHS-1a receptor. This pentapeptide ghrelin analog effectively increases growth hormone levels and enhances gastric emptying. Utilized in research, Relamorelin acetate shows promise for addressing conditions such as cachexia, gastroparesis, and various gastric or intestinal dysmotility disorders. -
GHSR Agonist
Ghrelin receptor full agonist-2 (compound 12j) is a potent agonist of the ghrelin receptor (GHSR), facilitating enhanced signaling through this target. This compound demonstrates significant biological activity associated with ghrelin's roles in appetite regulation, energy homeostasis, and growth hormone secretion. Its applications extend to studies investigating metabolic disorders, neuroendocrine functions, and potential therapeutic strategies in obesity and related conditions. -
GHSR Agonist
GSK894490A is a non-peptide agonist of the growth hormone secretagogue receptor (GHSR). It elicits biological activity by enhancing ghrelin signaling, thereby promoting growth hormone release. This compound is valuable for research focused on metabolic regulation, appetite modulation, and potential therapeutic targets for growth hormone-related disorders. -
GHSR Agonist
BMS-604992 free base is a selective agonist of the growth hormone secretagogue receptor (GHSR). It exhibits high-affinity binding with an inhibition constant (Ki) of 2.3 nM and potent functional activity, characterized by an EC50 value of 0.4 nM. This compound has been shown to effectively stimulate food intake in rodent models, making it a valuable tool for research in the fields of appetite regulation and metabolic disorders. -
GHSR1a Agonist
PF-6870961 is a selective inverse agonist of the growth hormone secretagogue receptor 1a (GHSR1a). It demonstrates Ki values of 73.6 nM for human GHSR, 239 nM for rat GHSR, and 217 nM for canine GHSR. This compound effectively inhibits constitutive GHSR1a-induced inositol phosphate accumulation with an IC50 of 300 nM and also blocks β-arrestin mobilization with an IC50 of 1.10 nM. PF-6870961 serves as a valuable tool in research focused on GHSR signaling pathways and their physiological roles. -
GHSR
GHRF, mouse is a peptide composed of 44 amino acids that acts as a growth hormone-releasing factor primarily targeting GHSR. This reagent stimulates the release and synthesis of growth hormone, playing a crucial role in growth regulation and metabolic functions. It is widely utilized in research applications focusing on endocrinology, growth disorders, and the mechanisms of hormone action. -
GHSR
Obestatin (rat) is a 23-amino acid peptide encoded by the Ghrelin gene that primarily targets the G-protein coupled receptor 39 (GHSR). It plays a critical role in regulating food intake, inhibiting jejunal contractions, and promoting weight management. Additionally, obestatin exhibits anti-inflammatory, cardioprotective, and antioxidant properties, making it a valuable reagent for research in metabolic disorders and cardiovascular health. -
GHSR Agonist
BMS-604992 is a selective, orally active agonist of the growth hormone secretagogue receptor (GHSR). It exhibits high-affinity binding with a Ki of 2.3 nM and demonstrates potent functional activity with an EC50 of 0.4 nM. This compound has been shown to effectively stimulate food intake in rodent models, making it valuable for research in appetite regulation and metabolic studies. -
GHSR1a Agonist
PF-6870961 hydrochloride is a potent inverse agonist of GHSR1a, exhibiting Ki values of 73.6 nM for human GHSR, 239 nM for rat GHSR, and 217 nM for dog GHSR. It effectively inhibits GHSR1a-induced inositol phosphate (IP) accumulation with an IC50 of 300 nM and demonstrates a strong inhibition of constitutive GHSR1a β-arrestin mobilization with an IC50 of 1.10 nM. This compound is relevant for research applications exploring the physiological roles of GHSR1a in metabolic and neuroendocrine processes. -
GHSR Agonist
Macimorelin is a potent GHSR agonist that serves as a growth hormone secretagogue. It effectively stimulates the release of growth hormone, making it a valuable tool in the investigation of adult growth hormone deficiency (AGHD) and cancer anorexia-cachexia syndrome (CACS). This compound is instrumental in research aimed at understanding the physiological roles of growth hormone and its potential therapeutic applications in these conditions. -
GHSR Agonist
BMS-604992 dihydrochloride is a selective agonist of the growth hormone secretagogue receptor (GHSR), exhibiting high-affinity binding with a Ki of 2.3 nM and potent functional activity with an EC50 of 0.4 nM. This small-molecule compound has been shown to stimulate food intake in rodent models, making it a valuable tool for studies related to appetite regulation and metabolic disorders. Its distinctive mechanism and efficacy position BMS-604992 dihydrochloride as an important reagent for research in endocrinology and neurobiology. -
GHSR
JMV 3002 is a potent antagonist of the growth hormone secretagogue receptor (GHSR). It exhibits significant biological activity by inhibiting hexarelin-stimulated food intake in rat models, achieving up to 98% reduction at a dose of 80 μg/kg. JMV 3002 does not induce release of growth hormone on its own, nor does it inhibit hexarelin-stimulated growth hormone secretion in infant rats at a dose of 160 μg/kg. This compound is valuable for research focused on energy homeostasis and the regulation of appetite. -
GHSR-1a Agonist
GHSR-1a agonist-1 is a potent agonist of the human growth hormone secretagogue receptor 1a (GHSR-1a), exhibiting an EC50 value of 0.49 nM. This compound effectively stimulates the release of endogenous growth hormone, making it valuable for investigating growth and developmental processes. In preclinical studies, oral administration at a dosage as low as 0.1 mg/kg led to significant increases in body weight and length in 4-week-old rats, supporting its potential applications in addressing growth and development retardation in pediatric research. -
GHSR Inverse Agonist
KwFwLL-NH2 is a hexapeptide that functions as an inverse agonist at the growth hormone secretagogue receptor (GHSR). This compound demonstrates moderate potency with an EC50 of 45.6 nM, making it a valuable tool for investigating the role of ghrelin signaling in various biological processes. It is applicable in research focused on appetite regulation, metabolic disorders, and potential therapeutic interventions targeting the ghrelin pathway. -
GLP-1R Agonist
Lotiglipron is an orally active GLP-1 receptor agonist that plays a crucial role in enhancing glucose-dependent insulin secretion and reducing appetite. This compound is primarily utilized in research related to Type 2 diabetes mellitus (T2DM) and metabolic disorders, demonstrating significant effects on glycemic control and weight management. Its unique mechanism makes Lotiglipron a valuable tool for studying potential therapeutic strategies in diabetes treatment. -
Semaglutide Intermediate
tBuO-Ste-Glu(AEEA-AEEA-OH)-OtBu is a key intermediate in the synthesis of Semaglutide, a glucagon-like peptide 1 receptor (GLP-1R) agonist. This compound is essential for facilitating the development of therapeutics targeting GLP-1R, which plays a crucial role in glucose metabolism and appetite regulation. Research applications include the study of metabolic disorders and the development of obesity and diabetes treatments. -
GLP-1R Agonist
Aleniglipron is a potent glucagon-like peptide-1 receptor (GLP-1R) agonist that exhibits an EC50 value of less than 0.1 nM in human-derived beta (HDB) cell lines through cAMP stimulation assays. This compound selectively activates the Gαs-cAMP signaling pathway of GLP-1R, avoiding β-arrestin recruitment. Aleniglipron is demonstrated to enhance insulin release, improve glucose clearance, reduce food intake, and promote weight loss. It serves as a valuable tool in research focused on type 2 diabetes and obesity. -
GLP-1 Analog
GLP-1 (7-36), amide, biotin labeled is a biotinylated analog of human Glucagon-Like Peptide 1, specifically comprising the C-terminal region. This compound serves as a valuable tool for studying GLP-1 receptor interactions and signaling pathways. It is commonly utilized in research applications focused on metabolic disorders, diabetes, and obesity, providing insights into peptide hormone functions and their implications in therapeutic development. -
GPCR Agonist
Tryptophan-cholic acid (Trp-CA) serves as an agonist for the orphan G protein-coupled receptor MRGPRE, exhibiting an EC50 of 9.6 μM. This compound facilitates the secretion of glucagon-like peptide GLP-1, improving glucose tolerance in diabetic mouse models. Although Trp-CA is orally effective, its poor absorption and inability to cross the blood-brain barrier limit its systemic application. Its primary research applications focus on understanding mechanisms in type 2 diabetes (T2D) and investigating treatments for insulin secretion and hepatic steatosis associated with high-fat diets. -
GLP-1R PAM
V-0219 is an orally active positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R). This compound enhances GLP-1R signaling, making it a valuable tool for studying therapeutic strategies in obesity-associated diabetes and related metabolic disorders. Its mechanism of action offers potential insights into the modulation of glucose homeostasis and appetite regulation. -
GLP-1R Modulator
LSN3160440 is an allosteric modulator of the GLP-1 receptor (GLP-1R) that enhances protein-protein interactions, effectively functioning as a molecular glue. By stabilizing the binding of inactive GLP-1 (9-36) NH2 to GLP-1R, it facilitates receptor activation and downstream signaling. This compound is valuable in studying metabolic disorders and diabetes-related research, providing insights into GLP-1R modulation and its therapeutic potential. -
Antioxidant Agent
Cinnamtannin A2, a tetrameric procyanidin, functions as a potent antioxidant agent. It has been shown to enhance GLP-1 levels and stimulate insulin secretion in murine models. Additionally, Cinnamtannin A2 upregulates the expression of corticotropin-releasing hormone and demonstrates significant anti-diabetic and nephroprotective effects, making it valuable for research in metabolic and renal health. -
GLP-1 Receptor Agonist
Albiglutide fragment is a GLP-1 receptor agonist that corresponds to a biologically active form of the GLP-1 (7-36) analog. This peptide plays a crucial role in modulating glucose metabolism by stimulating insulin secretion and reducing glycosylated hemoglobin (A1C) levels, making it a valuable tool in type 2 diabetes (T2D) research. Its unique structure, derived from a DPP-4 resistant GLP-1 dimer fused with the human albumin gene, enhances its stability and provides insights into long-acting therapeutic options for diabetes management. -
GLP-1 Receptor Agonist
(4S)-GLP-1 receptor agonist 14 is a potent agonist targeting the GLP-1 receptor, exhibiting an EC50 of ≤ 20 nM. This compound is effective in stimulating insulin secretion and has applications in the study of diabetes, obesity, and metabolic disorders. Additionally, it may provide insights into cardiovascular diseases, liver diseases, and nonalcoholic steatohepatitis (NASH), making it a valuable tool for researchers investigating GLP-1 receptor-related pathways. -
GLP-1 Agonist
GLP-1R agonist 10 is a potent GLP-1 receptor agonist, exhibiting an EC50 of 0.051 nM. This compound stimulates insulin secretion in a glucose-dependent manner, thereby enhancing glucose homeostasis. It is primarily utilized in research applications focused on metabolic disorders, diabetes treatment, and the mechanistic study of GLP-1 signaling pathways. -
GLP-1 Agonist
GLP-1 receptor agonist 7 is a highly effective agonist targeting the glucagon-like peptide-1 (GLP-1) receptor. This compound stimulates cAMP production via GLP-1R activation with an EC50 of ≤ 0.2 nM. GLP-1 receptor agonist 7 is valuable for research applications related to metabolic disorders, particularly type 2 diabetes, facilitating the investigation of GLP-1-mediated pathways and potential therapeutic interventions. -
GLP-1 Receptor Agonist
GLP-1 receptor agonist 11 is a selective agonist of the glucagon-like peptide-1 (GLP-1) receptor. This compound demonstrates significant biological activity in stimulating insulin secretion and inhibiting glucagon release, making it a valuable tool in diabetes research. Additionally, GLP-1 receptor agonist 11 may be applied in studies related to non-alcoholic fatty liver disease, offering insights into metabolic regulation and potential therapeutic strategies. -
GLP-1 Antagonist
Exendin(9-39) amide acetate is a potent glucagon-like peptide-1 (GLP-1) antagonist that selectively competes with endogenous GLP-1 for the GLP-1 receptor (GLP-1R). By inhibiting GLP-1 signaling, it counteracts the physiological effects associated with elevated GLP-1 levels. This reagent is particularly valuable for research into postbariatric hypoglycemia (PBH) and other metabolic disorders where GLP-1 modulation is critical. -
GLP-1 Activator
3-Deoxyglucosone is a GLP-1 activator that plays a critical role in the Maillard reaction and the polyol pathway. This reactive intermediate interacts with protein amino groups to produce advanced glycation end products (AGEs), particularly imidazolone, the most specific AGE for 3-Deoxyglucosone. Additionally, it enhances GLP-1 secretion in the presence of low glucose levels, positioning it as a valuable biomarker for diabetes research. -
GLP Receptor Agonist
GLP-1 receptor agonist 14 is a potent agonist of the glucagon-like peptide-1 (GLP-1) receptor. This compound demonstrates significant biological activity in promoting insulin secretion and enhancing glucose-dependent insulin release, making it a valuable tool for research in diabetes and metabolic disorders. Its unique properties facilitate investigations into GLP-1 signaling pathways and therapeutic strategies for metabolic diseases. -
GLP-1R PAM
V-0219 hydrochloride is a positive allosteric modulator (PAM) of the glucagon-like peptide-1 receptor (GLP-1R). This compound has demonstrated oral bioactivity and is pertinent in the study of obesity-associated diabetes. Its ability to enhance GLP-1R signaling makes it a valuable tool for research into metabolic disorders and therapeutic interventions targeting glucose homeostasis. -
GLP-1 Receptor Agonist
GLP-1 Receptor Agonist 10 is a potent agonist of the glucagon-like peptide-1 (GLP-1) receptor. It has demonstrated the ability to inhibit food intake and reduce glucose excursions in mice, making it a valuable tool for investigating metabolic disorders. This compound is particularly relevant for research applications focused on type 2 diabetes (T2DM) and obesity, providing insights into potential therapeutic strategies for these conditions.

