Catalog No.
Product Name
Application
Product Information
Citations
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DPPIV Inhibitor
K579 is a potent dipeptidyl peptidase IV (DPPIV) inhibitor that exhibits oral bioactivity. This compound effectively mitigates blood glucose elevation by increasing plasma insulin levels and enhancing the active forms of glucagon-like peptide-1 (GLP-1). K579 is suitable for research applications focused on diabetes and glucose metabolism regulation. -
DPP-4 Inhibitor
(2S,4R)-Teneligliptin is a selective inhibitor of dipeptidyl peptidase IV (DPP-4). By enhancing the plasma concentration of active glucagon-like peptide-1 (GLP-1), it promotes insulin secretion in response to elevated blood glucose levels, demonstrating significant hypoglycemic activity. This compound holds promise for research applications focused on type 2 diabetes management and related metabolic disorders. -
Dipeptidyl Peptidase Inhibitor
Retagliptin hydrochloride is an effective inhibitor of dipeptidyl peptidase-4 (DPP-4), a key enzyme in glucose metabolism. This compound enhances glycemic control in type 2 diabetes by prolonging the action of incretin hormones, including glucagon-like peptide-1 (GLP-1). It is utilized in research applications focused on metabolic disorders and the regulation of insulin secretion. -
DPP4 Inhibitor
Cetagliptin is an orally active dipeptidyl peptidase 4 (DPP-4) inhibitor that also engages CYP2D6 with an IC50 value of 6 µM. By inhibiting DPP-4, cetagliptin effectively reduces the degradation of glucagon-like peptide-1 (GLP-1), contributing to the regulation of postprandial blood glucose levels. This compound is primarily utilized in type 2 diabetes mellitus research, making it a valuable tool for studying glucose homeostasis and metabolic responses. -
DPP-4 Inhibitor
DPP-4-IN-18 is a potent and selective Dipeptidyl Peptidase-4 (DPP-4) inhibitor with an IC50 of 27 nM. By inhibiting DPP-4, this compound prevents the degradation of glucagon-like peptide 1 (GLP-1), leading to increased levels of active GLP-1. DPP-4-IN-18 is primarily utilized in research focused on type 2 diabetes and related metabolic disorders. -
Serine Aminopeptidase
Dipeptidyl Peptidase IV, Porcine Kidney is a serine aminopeptidase that plays a vital role in glucose metabolism. This enzyme specifically hydrolyzes gastric inhibitory peptide (GIP) and glucagon-like peptide-1 (GLP-1), which are key incretins involved in insulin release regulation. Its biological activity makes it a valuable tool for research in diabetes, metabolism, and related endocrine functions. -
DPP-IV Inhibitor
Gosogliptin hydrochloride is a selective, competitive inhibitor of DPP-IV, an enzyme crucial for the degradation of incretin peptides such as GLP-1 and glucose-dependent insulinotropic polypeptide. This compound exhibits rapid and reversible inhibition of plasma DPP-4 activity, leading to enhanced insulin secretion and improved glucose tolerance. Gosogliptin hydrochloride is primarily utilized in research focused on diabetes and metabolic disorders, providing valuable insights into glucose regulation and insulin dynamics. -
DPP-4 Inhibitor
DPP-4-IN-10 is a potent DPP-4 inhibitor that acts to prevent the degradation of glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP). By inhibiting DPP-4, this compound may enhance glycemic control in individuals with type 2 diabetes mellitus (T2DM). Its oral bioavailability makes it suitable for pharmacological studies focused on glucose metabolism and diabetes management. -
DPP-IV Inhibitor
ASP8497 is a competitive inhibitor of dipeptidyl peptidase IV (DPP-IV), which plays a critical role in glucose metabolism. This compound effectively reduces blood glucose levels and elevates plasma active GLP-1 and insulin concentrations without inducing hypoglycemia in fasted normal mice. ASP8497 is suitable for research applications focused on antihyperglycemic mechanisms and glucose regulation. -
DPP-IV Inhibitor
Carmegliptin is a potent and orally active DPP-IV inhibitor, demonstrating an IC50 value of 6.8 nM for human DPP-IV. By binding to the S1 pocket of DPP-IV, it effectively inhibits the degradation of GLP-1, leading to increased plasma insulin levels, improved glucose tolerance, and alleviation of hyperglycemia. Carmegliptin serves as a substrate for human P-glycoprotein without inhibiting the transporter, exhibiting low in vitro cell permeability. This compound is valuable for research focused on type 2 diabetes and non-insulin-dependent diabetes mellitus. -
DPP-4 Inhibitor
16-Hydroxycleroda-3,13-dien-15,16-olide is a potent dipeptidyl peptidase 4 (DPP-4) inhibitor, targeting the serine protease class of enzymes. This clerodane diterpene demonstrates key biological activities, including the down-regulation of lipopolysaccharide (LPS)-induced ERK phosphorylation in myocytes and inhibition of glucagon-like peptide-1 (GLP-1) induced protein kinase A (PKA) expression. Additionally, it exhibits hypolipidemic, hepatoprotective, and hypoglycemic effects, making it a valuable compound for research in metabolic and cardiovascular diseases. -
DPP-IV Inhibitor
Carmegliptin hydrochloride is a potent DPP-IV inhibitor, exhibiting a human DPP-IV IC50 of 6.8 nM. By binding to the S1 pocket of DPP-IV, it prevents the degradation of GLP-1, leading to increased plasma insulin levels, improved glucose tolerance, and relief from hyperglycemia. This compound can serve as a valuable reagent for research into type 2 diabetes and non-insulin-dependent diabetes mellitus, providing insights into GLP-1 modulation and its effects on metabolic regulation. -
DPP-IV Inhibitor
TS-021 is a selective, orally active, reversible DPP-IV inhibitor with long-lasting effects. It demonstrates significant selectivity against DPP-8 and DPP-9, exceeding 600-fold and 1,200-fold, respectively, as well as a greater than 15,000-fold selectivity over other peptidases. With an IC50 value of 5.34 nM for DPP-IV inhibition in human plasma, TS-021 is effective in enhancing active GLP-1 levels and exhibits potent antihyperglycemic activity, making it valuable for research in diabetes and metabolic disorders. -
GLP-1/Amylin Agonist
Zenagamtide is a GLP-1 and amylin receptor agonist that acts as a triple agonist also targeting the calcitonin receptor. It is a peptide comprising 68 amino acids and is capable of crossing the blood-brain barrier, making it effective in modulating appetite and reducing energy intake. Research suggests that Zenagamtide may lead to improvements in body weight, waist circumference, glycated hemoglobin, and lipid profiles, while also enhancing insulin sensitivity and ameliorating features of metabolic dysfunction-associated steatotic liver disease (MASLD). Its biological activity makes it valuable for investigating conditions related to overweight, obesity, and insulin resistance. -
GLP-1R Agonist
CT-996 is an orally active GLP-1 receptor (GLP-1R) agonist with an EC50 of 0.49 nM, modulating glucose metabolism through its effects on β-arrestin recruitment and receptor internalization. This compound significantly lowers postprandial blood glucose levels in mice engineered to express human GLP-1 receptors and enhances glucose-stimulated insulin secretion (GSIS) in obese monkey models during intravenous glucose challenges. CT-996 serves as a valuable tool for research focused on type 2 diabetes and obesity. -
Exenatide Impurity
(D-Asn28)-Exenatide is an impurity of Exenatide, which functions as a long-acting agonist of the glucagon-like peptide-1 receptor. This compound may be used in research applications focusing on peptide synthesis, quality control, and pharmacological studies involving GLP-1 receptor pathways. Its significance lies in understanding the properties and effects of Exenatide-related compounds. -
M1 Muscarinic Agonist
McN-A-343 is a selective M1 muscarinic agonist that enhances muscarinic transmission in sympathetic ganglia. This compound significantly inhibits muscarine-induced catecholamine secretion in isolated perfused rat adrenal glands and plays a role in neuronal firing regulation. Additionally, McN-A-343 activates enteroendocrine L cells to promote the release of glucagon-like peptide 1 (GLP-1) and modulates α-melanocyte stimulating hormone (α-MSH) secretion from the pituitary gland. Its capacity to reduce colonic inflammation and oxidative stress makes McN-A-343 a valuable tool for studying ulcerative colitis. -
GPR120 Agonist
GPR120 Agonist 5 is a selective agonist for the GPR120 receptor, exhibiting an EC50 of 1.2 μM. This compound enhances the secretion of glucagon-like peptide-1 (GLP-1) through its interaction with GPR120, leading to increased insulin production and decreased blood glucose levels. Additionally, GPR120 Agonist 5 demonstrates anti-inflammatory properties, making it a valuable tool for studies focused on metabolic disorders, obesity, insulin resistance, and type 2 diabetes. This reagent is essential for investigating the biological functions and therapeutic potential of GPR120 in relevant disease models. -
GPR40 Full Agonist
AM-6226 is a potent full agonist of the G protein-coupled receptor 40 (GPR40), exhibiting an EC50 of 0.12 μM. This compound effectively activates GPR40 receptors on pancreatic β cells and enteroendocrine L cells, promoting insulin secretion in a glucose-dependent manner while enhancing the release of incretin hormones like GLP-1 and GIP. AM-6226 is valuable for research into metabolic diseases, particularly diabetes, due to its potential to mitigate hypoglycemia risks. -
GPR40 Agonist
GPR40 Agonist 7 is a potent and orally active agonist of the G protein-coupled receptor GPR40. This compound enhances insulin and GLP-1 secretion, demonstrating notable hypoglycemic effects in vivo, with an effective dose (ED50) of 0.58 mg/kg. It serves as a valuable research tool for studying glucose metabolism and related metabolic disorders. -
GPR40 Agonist
BMS-986118 is a selective agonist of GPR40, exhibiting potent biological activity with an EC50 of 0.07 µM. This compound enhances insulin secretion and stimulates GLP-1 release, leading to significant reductions in plasma glucose levels in acute animal models. BMS-986118 is valuable for research in diabetes and metabolic disorders, providing insights into the regulation of glucose homeostasis. -
GPR120 Agonist
LXT34 is a potent agonist of the GPR120 receptor, demonstrating significant anti-inflammatory activity. This compound enhances GLP-1 production in the gastrointestinal tract and ameliorates insulin resistance in both macrophages and pancreatic cells. LXT34 is applicable in studies related to inflammatory diseases, including type 2 diabetes, obesity, and non-alcoholic fatty liver disease. -
GPR40 Agonist
LY2881835 is a selective agonist of the G protein-coupled receptor 40 (GPR40), demonstrating potent activity in promoting the secretion of insulin and GLP-1, while effectively lowering glucose levels in a dose-dependent manner. This compound shows promise for research applications related to type 2 diabetes mellitus. Additionally, LY2881835 features an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) for click chemistry experiments. -
Anti-diabete Agent
Hyocholic acid is a bile acid primarily found in porcine sources, demonstrating significant anti-diabetic properties. Its mechanism involves promoting GLP-1 secretion through activation of TGR5 and inhibition of FXR in enteroendocrine cells. This compound has potential applications in research aimed at understanding and treating type 2 diabetes and related metabolic disorders. -
TGR5 Agonist
Cholic acid 7-sulfate is a selective agonist for the TGR5 receptor with an EC50 of 0.17 μM. This compound enhances GLP-1 secretion in enteroendocrine L cells, leading to improved glucose tolerance through TGR5 activation. Additionally, as an endogenous ligand for MHC class I-related protein (MR1), it supports the survival of mucosal-associated invariant T (MAIT) cells and influences their development and function by modulating homeostatic gene expression. Cholic acid 7-sulfate is valuable in studies related to diabetes and MAIT cell-mediated immune regulation. -
TGR5 Activator
WB403 is a potent TGR5 activator with an EC50 of 5.5 μM for human TGR5. It enhances downstream signaling pathways associated with glucose metabolism, notably promoting GLP-1 secretion, improving glucose tolerance, and lowering fasting and postprandial blood glucose levels as well as HbA1c in murine models of type 2 diabetes. Additionally, WB403 contributes to increased pancreatic β-cell mass and the restoration of the islet cell distribution. This compound is valuable for studying mechanisms and therapeutic strategies in type 2 diabetes research. -
Stable Isotope
Cholic acid 7-sulfate-d4 is a deuterium-labeled derivative of cholic acid 7-sulfate, a selective agonist for the TGR5 receptor with an EC50 of 0.17 μM. This compound plays a crucial role in stimulating GLP-1 secretion and enhancing glucose tolerance through its action on enteroendocrine L cells. Additionally, cholic acid 7-sulfate-d4 serves as an endogenous ligand for MHC class I-related protein (MR1), influencing the development and function of mucosal-associated invariant T cells (MAIT). It is primarily utilized in research focused on diabetes and immune regulation related to MAIT cells. -
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. -
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. -
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. -
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. -
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.
