Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
GHS-R1a Antagonist
Cortistatin-8 (CST-8; PCFWKTCK) is a synthetic analogue of the neuropeptide cortistatin that acts as an antagonist of the ghrelin receptor (GHS-R1a). This compound counteracts the effects of ghrelin on gastric acid secretion and influences growth hormone release from somatotroph cells. With no binding affinity for somatostatin receptors (SST-R), Cortistatin-8 is specifically designed for research applications investigating the modulation of ghrelin signaling both in vitro and in vivo. -
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. -
ASM Inhibitor
KARI 201 hydrochloride is a selective inhibitor of acid sphingomyelinase (ASM) with a competitive mechanism of action, exhibiting an IC50 of 338.3 nM. This compound is capable of penetrating the blood-brain barrier and has demonstrated potential in improving neuropathological features associated with Alzheimer's disease. KARI 201 hydrochloride serves as a valuable tool for research applications focused on neurodegenerative disorders and the modulation of sphingolipid metabolism. -
Growth Hormone Secretagogue Agonist
L-692429 is a benzolactam derivative functioning as a nonpeptidyl growth hormone secretagogue (GHS) agonist. It exhibits biological activity by binding to G protein-coupled receptors with a Ki of 63 nM, facilitating the release of growth hormone. This compound is useful in research applications focused on growth hormone regulation and metabolism. -
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. -
GHS-R1a Agonist
L-692585 is a highly potent nonpeptidyl agonist of the growth hormone secretagogue receptor 1a (GHS-R1a), characterized by a Ki value of 0.8 nM. This compound directly stimulates somatotropes, leading to the release of growth hormone (GH). L-692585 is valuable for research into growth hormone regulation and its implications in metabolic disorders and growth deficiencies. -
Isomer of GSK1614343
(αR,8aS)-GSK1614343 is an isomer of GSK1614343, acting as a potent antagonist of growth hormone secretagogues type 1a (GHS1a) receptors. This compound effectively modulates the GH secretagogue pathway, making it valuable for research focused on obesity, metabolism, and growth-related disorders. Its distinct isomeric configuration provides unique properties for investigations into receptor biology and therapeutic target validation. -
Neuropeptide Hormone
Somatostatin-25 is a naturally occurring neuropeptide hormone that primarily inhibits the secretion of growth hormone. This regulatory activity plays a crucial role in various physiological processes, including the modulation of endocrine functions and gastrointestinal activities. It is widely utilized in research to investigate growth hormone regulation and its implications in disorders related to endocrine signaling. -
GHRHR Activator
Human growth hormone-releasing factor (GHRH) is a hypothalamic polypeptide that activates the growth hormone-releasing hormone receptor (GHRHR) in the anterior pituitary. Its primary mechanism involves stimulating the production and secretion of growth hormone (GH), which is critical for various physiological processes including growth and metabolism. This reagent is valuable for research applications focused on endocrinology, developmental biology, and metabolic disorders. -
GRF Superagonist
(D-Ala2)-GRF (1-29) amide (human) is a superagonist of Growth Hormone-Releasing Factor (GRF), demonstrating approximately 50 times the GH-releasing potency compared to GRF (1-29) in both pig and rat models. This compound is essential for studies focused on growth hormone modulation, metabolic research, and endocrine system regulation. Its enhanced activity makes it a valuable tool for exploring the physiological roles of growth hormone in various biological 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. -
GHS1a Antagonist
GSK1614343 is a selective antagonist of growth hormone secretagogues type 1a (GHS1a) receptors. It effectively inhibits the calcium response induced by ghrelin, exhibiting a pIC50 value of 7.90. This compound serves as a valuable tool for exploring the physiological roles of the ghrelin signaling pathway in various research applications, particularly in rodent models. -
GHRH Analog
[His1,Nle27] GHRF (1-32), amide, human is a potent analog of growth hormone-releasing hormone (GHRH) that primarily targets the growth hormone secretagogue receptor (GHRHR). This compound exhibits strong receptor affinity, making it a valuable tool in research applications focused on growth hormone regulation and related metabolic processes. Its use may enhance studies related to pituitary function and endocrine signaling pathways. -
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.
