GPCR/G Protein

Items 5001-5050 of 5455

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  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. 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).
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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