GPCR/G Protein

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  1. GLP-1R Modulator

    LSN3160440 is an allosteric modulator of the GLP-1 receptor (GLP-1R) that enhances protein-protein interactions, effectively functioning as a molecular glue. By stabilizing the binding of inactive GLP-1 (9-36) NH2 to GLP-1R, it facilitates receptor activation and downstream signaling. This compound is valuable in studying metabolic disorders and diabetes-related research, providing insights into GLP-1R modulation and its therapeutic potential.
  2. Antioxidant Agent

    Cinnamtannin A2, a tetrameric procyanidin, functions as a potent antioxidant agent. It has been shown to enhance GLP-1 levels and stimulate insulin secretion in murine models. Additionally, Cinnamtannin A2 upregulates the expression of corticotropin-releasing hormone and demonstrates significant anti-diabetic and nephroprotective effects, making it valuable for research in metabolic and renal health.
  3. GLP-1 Receptor Agonist

    Albiglutide fragment is a GLP-1 receptor agonist that corresponds to a biologically active form of the GLP-1 (7-36) analog. This peptide plays a crucial role in modulating glucose metabolism by stimulating insulin secretion and reducing glycosylated hemoglobin (A1C) levels, making it a valuable tool in type 2 diabetes (T2D) research. Its unique structure, derived from a DPP-4 resistant GLP-1 dimer fused with the human albumin gene, enhances its stability and provides insights into long-acting therapeutic options for diabetes management.
  4. GLP-1 Receptor Agonist

    (4S)-GLP-1 receptor agonist 14 is a potent agonist targeting the GLP-1 receptor, exhibiting an EC50 of ≤ 20 nM. This compound is effective in stimulating insulin secretion and has applications in the study of diabetes, obesity, and metabolic disorders. Additionally, it may provide insights into cardiovascular diseases, liver diseases, and nonalcoholic steatohepatitis (NASH), making it a valuable tool for researchers investigating GLP-1 receptor-related pathways.
  5. GLP-1 Agonist

    GLP-1R agonist 10 is a potent GLP-1 receptor agonist, exhibiting an EC50 of 0.051 nM. This compound stimulates insulin secretion in a glucose-dependent manner, thereby enhancing glucose homeostasis. It is primarily utilized in research applications focused on metabolic disorders, diabetes treatment, and the mechanistic study of GLP-1 signaling pathways.
  6. GLP-1 Agonist

    GLP-1 receptor agonist 7 is a highly effective agonist targeting the glucagon-like peptide-1 (GLP-1) receptor. This compound stimulates cAMP production via GLP-1R activation with an EC50 of ≤ 0.2 nM. GLP-1 receptor agonist 7 is valuable for research applications related to metabolic disorders, particularly type 2 diabetes, facilitating the investigation of GLP-1-mediated pathways and potential therapeutic interventions.
  7. GLP-1 Receptor Agonist

    GLP-1 receptor agonist 11 is a selective agonist of the glucagon-like peptide-1 (GLP-1) receptor. This compound demonstrates significant biological activity in stimulating insulin secretion and inhibiting glucagon release, making it a valuable tool in diabetes research. Additionally, GLP-1 receptor agonist 11 may be applied in studies related to non-alcoholic fatty liver disease, offering insights into metabolic regulation and potential therapeutic strategies.
  8. GLP-1 Antagonist

    Exendin(9-39) amide acetate is a potent glucagon-like peptide-1 (GLP-1) antagonist that selectively competes with endogenous GLP-1 for the GLP-1 receptor (GLP-1R). By inhibiting GLP-1 signaling, it counteracts the physiological effects associated with elevated GLP-1 levels. This reagent is particularly valuable for research into postbariatric hypoglycemia (PBH) and other metabolic disorders where GLP-1 modulation is critical.
  9. GLP-1 Activator

    3-Deoxyglucosone is a GLP-1 activator that plays a critical role in the Maillard reaction and the polyol pathway. This reactive intermediate interacts with protein amino groups to produce advanced glycation end products (AGEs), particularly imidazolone, the most specific AGE for 3-Deoxyglucosone. Additionally, it enhances GLP-1 secretion in the presence of low glucose levels, positioning it as a valuable biomarker for diabetes research.
  10. GLP Receptor Agonist

    GLP-1 receptor agonist 14 is a potent agonist of the glucagon-like peptide-1 (GLP-1) receptor. This compound demonstrates significant biological activity in promoting insulin secretion and enhancing glucose-dependent insulin release, making it a valuable tool for research in diabetes and metabolic disorders. Its unique properties facilitate investigations into GLP-1 signaling pathways and therapeutic strategies for metabolic diseases.
  11. GLP-1R PAM

    V-0219 hydrochloride is a positive allosteric modulator (PAM) of the glucagon-like peptide-1 receptor (GLP-1R). This compound has demonstrated oral bioactivity and is pertinent in the study of obesity-associated diabetes. Its ability to enhance GLP-1R signaling makes it a valuable tool for research into metabolic disorders and therapeutic interventions targeting glucose homeostasis.
  12. GLP1R Agonist

    DD202-114 is a selective agonist of the glucagon-like peptide-1 receptor (GLP1R), demonstrating significant potential for therapeutic applications in type 2 diabetes mellitus and obesity. This compound promotes cAMP accumulation, which is crucial for insulin secretion and glucose homeostasis. DD202-114 also exhibits inhibition of the hERG channel with an IC50 of 15.9 μM and demonstrates strong CYP2C8 inhibition with an IC50 of 0.22 μM. Additionally, it effectively reduces blood glucose levels and food intake, making it a valuable tool for research in metabolic disorders.
  13. GLP-1 Receptor Agonist

    GLP-1 Receptor Agonist 10 is a potent agonist of the glucagon-like peptide-1 (GLP-1) receptor. It has demonstrated the ability to inhibit food intake and reduce glucose excursions in mice, making it a valuable tool for investigating metabolic disorders. This compound is particularly relevant for research applications focused on type 2 diabetes (T2DM) and obesity, providing insights into potential therapeutic strategies for these conditions.
  14. GLP-1R Agonist Isomer

    (1R)-GLP-1 receptor agonist 12 is an isomer targeting the GLP-1 receptor (GLP-1R). It exhibits significant agonistic activity, which can stimulate insulin secretion and enhance β-cell function. This compound is particularly relevant in diabetes research and the study of metabolic disorders, making it a valuable tool for exploring therapeutic strategies in glucose homeostasis and appetite regulation.
  15. GLP-1R Agonist

    GLP-1R agonist 12 is a selective agonist for glucagon-like peptide-1 receptors (GLP-1R), which are integral to glucose metabolism and insulin secretion. This compound promotes insulin release and inhibits glucagon secretion, making it a valuable tool in diabetes research. Its activity may aid in the exploration of therapeutic strategies for metabolic disorders and related conditions.
  16. GLP Receptor Agonist

    Bofanglutide is an analog of glucagon-like peptide-1 (GLP-1) that acts as a GLP-1 receptor agonist, exhibiting an EC50 of 0.677 nM. This compound demonstrates significant efficacy in ameliorating type 2 diabetes by enhancing insulin secretion, suppressing glucagon release, and promoting β-cell proliferation. Bofanglutide is a valuable tool for diabetes research and therapeutic development targeting metabolic disorders.
  17. GLP-1 Receptor Agonist

    GLP-1 receptor agonist 12 is a potent agonist targeting the glucagon-like peptide-1 (GLP-1) receptor. This compound enhances insulin secretion and exhibits glucose-dependent effects, making it instrumental in diabetes research. Its mechanism of action provides valuable insights into the regulation of glucose homeostasis and potential therapeutic strategies for metabolic disorders.
  18. Liraglutide Side Chain

    Pal-Glu(OSu)-OH is a side chain of Liraglutide, which functions as a glucagon-like peptide-1 (GLP-1) receptor agonist. This compound is pivotal in research relating to type 2 diabetes mellitus, facilitating the study of metabolic regulation and therapeutic strategies targeting GLP-1 pathways. Its utilization aids in advancing knowledge in diabetes treatment and obesity research.
  19. GLP-1R Inhibitor

    GLP-1 receptor agonist 13 is a selective agonist targeting the glucagon-like peptide-1 receptor (GLP-1R), exhibiting an EC50 of 76 nM. This compound plays a significant role in enhancing glucose-dependent insulin secretion, thereby influencing metabolic processes. It is particularly useful in research applications focused on diabetes, obesity, and related metabolic disorders.
  20. GLP Inhibitor

    MS012 is a selective glucagon-like peptide (GLP) inhibitor with an IC50 value of 7 nM. This compound serves as a valuable tool in the investigation of GLP dysregulation associated with various conditions, including cancer, inflammatory diseases, and neuroregenerative disorders. Its application in research may facilitate the understanding of GLP's role in these pathophysiological processes.
  21. GLP-1 Antagonist

    Imapextide is a glucagon-like peptide-1 (GLP-1) receptor antagonist that plays a critical role in the study of hypoglycemia. By inhibiting GLP-1 activity, Imapextide provides insights into glucose homeostasis and insulin secretion regulation. It is a valuable tool for researchers investigating metabolic disorders and the physiological effects of GLP-1 signaling.
  22. GLP-2R Agonist

    Sonefpeglutide is a potent glucagon-like peptide-2 (GLP-2) receptor agonist, exhibiting an EC50 value of 0.327 nM for human GLP-2R. This long-acting analog is designed without a PEG linker and is fused to a human IgG Fc fragment, resulting in an extended half-life in vivo. Sonefpeglutide is particularly relevant for research into short bowel syndrome and related gastrointestinal disorders.
  23. GLP-1 Analog

    HAEGTFTSDVSSYLE is a GLP-1 analog designed to interact with GLP-1 receptors, mimicking the activity of endogenous glucagon-like peptide-1. This polypeptide exhibits key biological activities including the stimulation of insulin secretion and the inhibition of glucagon release, thereby regulating glucose homeostasis. HAEGTFTSDVSSYLE is utilized in research applications related to diabetes treatment, metabolic disorders, and obesity studies.
  24. Anti-GLP-1 receptor Antibody

    Efmedaglutide alfa is an anti-GLP-1 receptor antibody designed to interact specifically with the glucagon-like peptide-1 receptor. This fusion protein exhibits potent biological activity, promoting insulin secretion and inhibiting glucagon release, making it a useful tool in studies related to diabetes and metabolic disorders. Its application in research can aid in understanding the role of GLP-1 signaling in glucose homeostasis and potential therapeutic interventions for related diseases.
  25. Anti-GLP-1 receptor Antibody

    Efsubaglutide alfa is an anti-GLP-1 receptor antibody designed to target and inhibit the GLP-1 receptor, a key regulator of glucose metabolism and insulin secretion. This fusion protein exhibits potent biological activity in modulating glucose homeostasis and is primarily utilized in diabetes research. Its application extends to studies focused on the therapeutic potential for metabolic disorders and obesity management.
  26. GIPR/GLP-1R Agonist

    Zantrutide is an agonist of the glucagon, gastric inhibitory polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). It exhibits significant biological activity in the modulation of glucose metabolism and insulin secretion. This compound is valuable for research applications targeting metabolic diseases, particularly in the exploration of obesity and type 2 diabetes treatment strategies.
  27. GLP-1R PAM

    (S)-V-0219 is a selective positive allosteric modulator (PAM) of the glucagon-like peptide-1 receptor (GLP-1R). It induces calcium flux in HEK293 cells expressing human GLP-1R, enhancing receptor activity. In vivo studies demonstrate that (S)-V-0219 is orally bioavailable, effectively reducing hyperglycemia in murine models while also suppressing feeding behavior in fasting conditions. This compound presents valuable applications in diabetes research and appetite regulation studies.
  28. GLP-1R Agonist

    GLP-1R Agonist 18 is a potent agonist for the glucagon-like peptide-1 receptor (GLP-1R), exhibiting an EC50 of 0.044 nM. This compound enhances insulin secretion in response to glucose, making it a valuable tool for research in diabetes and metabolic disorders. Its high affinity for GLP-1R positions it as a significant candidate for investigating therapeutic strategies targeting glucose homeostasis and appetite regulation.
  29. GLP-1 Analogue

    Vurolenatide is a long-acting GLP-1 analogue that targets the glucagon-like peptide-1 receptor. It exhibits significant biological activity by enhancing insulin secretion, promoting satiety, and reducing gastric emptying, making it relevant for metabolic studies. Vurolenatide is particularly useful in research applications focusing on short bowel syndrome and disorders related to glucose metabolism.
  30. GLP-1R Agonist

    GLP-1R agonist 15 is a potent agonist of the glucagon-like peptide-1 receptor (GLP-1R). This compound plays a significant role in enhancing insulin secretion, inhibiting glucagon release, and promoting glucose-dependent insulin action. It is primarily utilized in research focused on metabolic disorders, including diabetes and obesity, and may aid in the development of novel therapeutic strategies targeting GLP-1R pathways.
  31. GLP Receptor Agonist

    GLP-1R agonist 21 is a selective agonist for the glucagon-like peptide-1 receptor (GLP-1R), exhibiting a potent binding affinity with an EC50 of 0.0104 nM. This compound enhances insulin secretion, promotes glucose-dependent insulin release, and plays a critical role in glucose homeostasis. It is primarily utilized in research related to metabolic disorders, diabetes, and obesity, providing valuable insights into therapeutic strategies targeting GLP-1R pathways.
  32. GLP-1R Agonist

    Linvixdutide is a potent GLP-1 receptor (GLP-1R) agonist known for its anti-obesity effects. By stimulating the GLP-1 pathway, it promotes insulin secretion, reduces glucagon release, and enhances satiety, making it a valuable tool in obesity research. This compound may also have applications in the study of metabolic disorders and diabetes management.
  33. GLP Receptor Agonist

    GLP-1 receptor agonist 15 selectively targets the GLP-1 receptor with an EC50 of 0.74 nM, demonstrating potent activity. This compound has an IC50 value of 10.1 μM for the hERG potassium ion channel, indicating a suitable safety profile. GLP-1 receptor agonist 15 is primarily utilized in diabetes research, providing valuable insights into glucose metabolism and insulin signaling pathways.
  34. GLP-1R Agonist

    GLP-1R agonist 19 is a potent and selective agonist of the glucagon-like peptide-1 receptor (GLP-1R). This compound demonstrates excellent plasma stability and liver microsomal stability, making it suitable for in vitro and in vivo studies. Additionally, it exhibits low hERG toxicity, ensuring a reduced risk of off-target effects. Research applications include investigations into glucose homeostasis, metabolic disorders, and potential therapeutics for type 2 diabetes.
  35. GLP Receptor Agonist

    GLP-1R agonist 20 (Compound I-132) is a selective agonist for the glucagon-like peptide-1 receptor (GLP-1R), exhibiting an EC50 value of 0.0162 nM. This compound plays a crucial role in enhancing insulin secretion and promoting glucose homeostasis. It is valuable for research applications focused on metabolic disorders such as type 2 diabetes and obesity.
  36. GIPR Antagonist

    GIPR Antagonist 2 is a potent antagonist of the GIP receptor, which plays a crucial role in glucose metabolism and energy homeostasis. This compound demonstrates significant potential for research applications related to obesity and type 2 diabetes. Its ability to inhibit GIPR signaling provides a valuable tool for investigating the underlying mechanisms of metabolic disorders and evaluating therapeutic strategies.
  37. GLP-1R Agonist

    GLP-1R agonist 27 is a potent agonist of the glucagon-like peptide-1 receptor (GLP-1R), demonstrating significant oral bioactivity. It enhances cyclic adenosine monophosphate (cAMP) accumulation, which is associated with reduced blood glucose levels and decreased food intake. This compound is instrumental in research related to obesity and type 2 diabetes mellitus (T2DM), offering potential insights into therapeutic approaches for metabolic disorders.
  38. GLP-1R PAM

    (R)-V-0219 is a positive allosteric modulator of the GLP-1 receptor (GLP-1R), functioning through enhanced receptor activation. It promotes calcium flux in human embryonic kidney (HEK) cells expressing hGLP-1R, indicating its role in metabolic regulation. This compound is particularly relevant for research focused on type 2 diabetes and obesity, allowing scientists to explore the therapeutic potentials of GLP-1R modulation.
  39. GLP-1R Agonist

    Zabopegdutide is a selective agonist of the glucagon-like peptide 1 receptor (GLP-1R). It exhibits significant biological activity in the modulation of glucose homeostasis and appetite regulation, making it a valuable tool for obesity research. This compound can facilitate studies aimed at understanding GLP-1R signaling pathways and their implications in metabolic disorders.
  40. GLP-1R Agonist

    GLP-1R agonist 16 is a selective agonist for the glucagon-like peptide-1 receptor (GLP-1R), exhibiting an EC50 of 0.15 nM. This compound is known to enhance insulin secretion and promote glucose-dependent insulin release, making it a valuable tool for diabetes research. GLP-1R agonist 16 is utilized in studies focused on metabolic pathways, therapeutic development for Type 2 diabetes, and potential cardiovascular effects related to GLP-1 signaling.
  41. GLP-1 Receptor Agonist

    GLP-1R Agonist 14 is a selective agonist for the glucagon-like peptide-1 receptor (GLP-1R), exhibiting an EC50 of 0-20 nM for human GLP-1 receptors. This compound stimulates insulin secretion and inhibits glucagon release, making it a valuable tool for studying glucose metabolism and diabetes-related research. Its strong activity at the GLP-1R positions it as an essential reagent for investigating potential therapeutic strategies in metabolic disorders.
  42. GIPR Antagonist

    GIPR Antagonist 1 is a potent inhibitor of the glucose-dependent insulinotropic polypeptide receptor (GIPR) with an IC50 of 4.8 nM. By effectively blocking GIPR signaling, this compound serves as a valuable tool in the study of type 2 diabetes and obesity. Its ability to modulate GIPR activity makes it significant for research focused on glucose metabolism and insulin regulation.
  43. GLP Receptor Agonist

    GLP-1R agonist 41 is a potent agonist for the glucagon-like peptide-1 receptor (GLP-1R), exhibiting an EC50 of 0.0187 nM. This compound actively stimulates GLP-1 signaling pathways, playing a significant role in glucose homeostasis and insulin secretion. It is primarily used in research focused on metabolic disorders such as diabetes and obesity, as well as in the investigation of potential therapeutic interventions targeting GLP-1R.
  44. GLP Receptor Agonist

    GLP-1R agonist 22 is a potent agonist of the glucagon-like peptide-1 receptor (GLP-1R), exhibiting an EC50 value of 0.0165 nM. This compound stimulates insulin secretion and enhances glucose homeostasis, making it a valuable tool for research in diabetes and metabolic disorders. Its specific action on GLP-1R allows for exploration of therapeutic applications in obesity and related conditions.
  45. GLP-1 Secretagogue

    JWU-A021 is a GLP-1 secretagogue that functions by activating the TRPA1 cation channel, resulting in a calcium ion influx and increased intracellular calcium levels in enteroendocrine cells and TRPA1-transfected cells. This activation subsequently stimulates the secretion of glucagon-like peptide-1 (GLP-1) from intestinal enteroendocrine and L cells. JWU-A021 is valuable for research in the context of type 2 diabetes, offering insights into GLP-1 modulation and its potential therapeutic implications.
  46. GLP-1 Agonist

    GLP-1R agonist 33 is a selective agonist for the glucagon-like peptide-1 receptor (GLP-1R). It exhibits significant bioactivity in stimulating insulin secretion and suppressing glucagon release, making it a valuable tool for investigating metabolic disorders. This compound is particularly applicable in research focused on diabetes, obesity, and non-alcoholic fatty liver disease (NAFLD).
  47. GIP/GLP-1 Receptor Agonist

    Acmopatide is a dual-acting agonist of the GIP and GLP-1 receptors. This compound exhibits significant biological activity in enhancing insulin secretion and regulating glucose homeostasis, making it a valuable tool in anti-diabetic research. Its unique mechanism of action supports investigations into novel therapeutic approaches for diabetes management.
  48. GLP-1R Agonist

    GLP-1R Agonist 34 is a small molecule that functions as an agonist of the glucagon-like peptide-1 receptor (GLP-1R). This compound enhances insulin secretion, suppresses glucagon release, and slows gastric emptying, leading to effective reductions in blood glucose levels. GLP-1R Agonist 34 is a valuable tool for research into metabolic disorders such as type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH).
  49. GLP-1R Agonist

    GLP-1R agonist 35 selectively targets the glucagon-like peptide-1 receptor (GLP-1R) with an EC50 of 0-10 nM, demonstrating potent agonistic activity. This compound is valuable for research applications focused on diabetes and obesity, facilitating the exploration of GLP-1R modulation in metabolic disorders and potential therapeutic interventions.
  50. GLP-1R/GIPR Agonist

    GLP-1R/GIPR agonist-2 is a selective agonist targeting the glucose-dependent insulinotropic polypeptide receptor (GIPR). It effectively enhances GIP(1-42)-induced intracellular cAMP production in human GIPR-expressing cells. This compound is valuable for research into type II diabetes mellitus, contributing to the understanding of insulin secretion and glucose homeostasis.

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