Catalog No.
Product Name
Application
Product Information
Citations
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GRK6 Inhibitor
GRK6-IN-5 is a selective inhibitor of G protein-coupled receptor kinase 6 (GRK6), exhibiting an IC50 of 4.48 μM. This compound is instrumental for investigating its role in hematological malignancies, inflammation-related conditions, and autoimmune disorders. Researchers can utilize GRK6-IN-5 to elucidate the biochemical pathways influenced by GRK6, potentially leading to therapeutic advancements in these diseases. -
GRK5 Inhibitor
GRK5-IN-5 is a selective inhibitor of G protein-coupled receptor kinase 5 (GRK5), demonstrating an IC50 of 0.03 μM. This compound also exhibits activity against GRK2 and GRK6, with IC50 values of 2.2 μM and 0.036 μM, respectively. GRK5-IN-5 is known for its potent activity in inhibiting myocardial hypertrophy and reducing non-myocardial cell proliferation. It effectively suppresses the upregulation of hypertrophy markers Nppa and Nppb, thereby preventing pathological remodeling of cardiac tissue. This reagent is valuable for investigating mechanisms underlying cardiac hypertrophy. -
G Protein-coupled Receptor 40 Agonist
DS-1558 is an orally bioavailable small molecule that acts as an agonist for G Protein-coupled Receptor 40 (GPR40). It enhances glucose-stimulated insulin secretion mediated by glucagon-like peptide-1 (GLP-1) and amplifies the insulinogenic response to intravenous glucose in normal Sprague Dawley rats. This compound is a valuable tool for researching mechanisms underlying type 2 diabetes and developing potential 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. -
GLP-1R Agonist
GLP-1R Agonist 2 is a potent agonist of the glucagon-like peptide-1 receptor (GLP-1R), functioning through the formation of hydrogen bonds with key residues Tyr42, Cys71, and Ser84. This compound demonstrates significant biological activity in stimulating insulin secretion and inhibiting glucagon release, making it a valuable tool for research into metabolic disorders such as type 2 diabetes and obesity. Its mechanism of action positions it as an important candidate for the development of therapeutics targeting these conditions. -
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. -
GLP-1 Receptor Antagonist
GLP-1(9-36)amide is a potent antagonist of the glucagon-like peptide-1 (GLP-1) receptor, generated from the enzymatic action of dipeptidyl peptidase-4 (DPP-4) on GLP-1(7-36)amide. This peptide plays a crucial role in glucose metabolism and insulin signaling and is utilized in research aimed at understanding metabolic disorders and the role of GLP-1 in obesity and diabetic conditions. The study of GLP-1(9-36)amide can provide insights into receptor regulation and potential therapeutic strategies for GLP-1 related pathologies. -
GLP-1R/GLP-2R Agonist
Dapiglutide is a dual agonist targeting the glucagon-like peptide-1 receptor (GLP-1R) and glucagon-like peptide-2 receptor (GLP-2R). This long-acting compound has been shown to mitigate intestinal dysfunction in mouse models of short bowel syndrome and exhibits significant anti-obesity properties. Dapiglutide is valuable for research into metabolic disorders and the therapeutic potential of GLP-1/GLP-2 receptor modulation. -
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 Receptor Agonist
TT-OAD2 is a non-peptide agonist of the glucagon-like peptide-1 (GLP-1) receptor, exhibiting a potent EC50 of 5 nM. This compound plays a significant role in enhancing glucose-dependent insulin secretion and may be utilized in the treatment of diabetes. Its selective activity makes it a valuable tool for studying GLP-1 receptor signaling pathways and their implications in metabolic disorders. -
GLP-1R Agonist
Orforglipron hemicalcium hydrate is a calcium salt hydrate derivative of Orforglipron, functioning as a GLP-1 receptor (GLP-1R) agonist. This compound demonstrates significant biological activity in enhancing insulin secretion and lowering blood glucose levels, making it a pivotal candidate for research in type 2 diabetes treatment. Its oral bioavailability and receptor selectivity support various studies aimed at understanding the therapeutic potential of GLP-1R modulation in metabolic disorders. -
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. -
GLP-2 Receptor Partial Agonist
GLP-2(3-33) is a partial agonist of the GLP-2 receptor, generated through the enzymatic action of dipeptidylpeptidase IV (DPPIV). It exhibits biological activity with an EC50 of 5.8 nM, making it a valuable tool for research into gastrointestinal physiology and potential therapeutic applications in metabolic disorders. Its role in modulating the GLP-2 receptor provides insight into gut hormone signaling and its effects on intestinal growth and function. -
Antioxidant
GLP-1(28-36)amide is a C-terminal nonapeptide derived from the cleavage of GLP-1 by neutral endopeptidase. This compound functions primarily as an antioxidant, targeting mitochondria and inhibiting mitochondrial permeability transition (MPT). GLP-1(28-36)amide exhibits significant anti-diabetic properties and offers cardioprotective effects, making it valuable in research focused on metabolic and cardiovascular diseases. -
Fragment Of Dulaglutide
GLP-1 moiety from Dulaglutide is a 31-amino acid fragment that acts as a glucagon-like peptide 1 (GLP-1) receptor agonist. This compound plays a crucial role in regulating glucose metabolism and insulin secretion, making it pertinent for research applications related to diabetes and myocardial injury. Its therapeutic potential is significant in studying metabolic disorders and cardiovascular health. -
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. -
Pentapeptide
GLP-1(32-36)amide is a pentapeptide derived from the C terminus of the glucoregulatory hormone GLP-1. This compound has been shown to inhibit weight gain and positively influence whole-body glucose metabolism in diabetic mouse models. It serves as a valuable tool for studying metabolic disorders and potential therapeutic strategies for diabetes management. -
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. -
GLP-1 Receptor Agonist
GLP-1R Agonist 17 is a potent agonist of the GLP-1 receptor, demonstrating strong activation of this target. This compound exhibits significant biological activity related to the modulation of glucose metabolism and appetite regulation. Its primary applications include research into cardiovascular metabolic diseases, making it a valuable tool for studying therapeutic interventions in diabetes and obesity. -
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. -
Anti-GLP1R Antibody
Gulgafafusp alfa is a human IgG2κ antibody that selectively targets the glucagon-like peptide 1 receptor (GLP1R). This antibody plays a critical role in research related to metabolic disorders, diabetes, and obesity by modulating GLP1R activity. Its ability to engage GLP1R provides valuable insights into the receptor's role in glucose homeostasis and appetite regulation. -
GLP-1 Receptor Agonist
PF-06954522 is an orally active agonist of the GLP-1 receptor, primarily targeting this receptor to modulate glucose homeostasis. Its biological activity makes it a valuable tool for researching type 2 diabetes mellitus and assessing the potential therapeutic effects on glycemic control and weight management. This compound is instrumental for studies aimed at understanding GLP-1 signaling pathways and related metabolic disorders. -
GLP-1R Agonist
Pegsebrenatide (NLY01) is a GLP-1 receptor agonist known for its ability to penetrate the blood-brain barrier. This compound demonstrates significant neuroprotective properties by alleviating retinal inflammation and preventing neuronal death associated with ocular hypertension. In preclinical models, Pegsebrenatide effectively delays the onset of experimental autoimmune encephalomyelitis and reduces its severity, while also inhibiting the formation of neurotoxic A1 reactive astrocytes. Its applications extend to research focused on glaucoma, Parkinson's disease, and multiple sclerosis. -
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. -
Enterostatin Hormone
(Ser8)-GLP-1 (7-36) amide, human is an entero-insulinotropic hormone derived from glucagonogen, specifically a cleavage product of GLP-1 (1-36) amide. This peptide plays a crucial role in stimulating glucose-dependent insulin secretion from pancreatic β-cells and modulates gastrointestinal motility and secretion. Its biological activity makes it a valuable reagent for research focused on metabolic disorders, diabetes, and gastrointestinal physiology. -
GLP-1 Peptides
GLP-1 (1-36) amide (human, rat) is a molecular variant of the glucagon-like peptide 1 (GLP-1) family. This peptide demonstrates the ability to stimulate [14C]aminopyrine accumulation in enzymatically dispersed rat parietal cells, indicating its role in gut hormone regulation. It is useful for research applications focused on metabolic disorders, glucose homeostasis, and appetite suppression, providing insights into obesity and diabetes mechanisms. -
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. -
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.
