GPCR/G Protein

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  1. Ghrelin Agonist

    CP-464709 is a potent agonist of the ghrelin receptor, capable of crossing the blood-brain barrier. This compound induces a biphasic blood pressure response when administered intravenously and elicits a pressor response following intrathecal administration by activating pre-sympathetic neurons in the spinal cord. CP-464709 is valuable for research on cardiovascular conditions and the mechanisms regulating blood pressure dynamics.
  2. GHSR1a Agonist

    PF-6870961 is a selective inverse agonist of the growth hormone secretagogue receptor 1a (GHSR1a). It demonstrates Ki values of 73.6 nM for human GHSR, 239 nM for rat GHSR, and 217 nM for canine GHSR. This compound effectively inhibits constitutive GHSR1a-induced inositol phosphate accumulation with an IC50 of 300 nM and also blocks β-arrestin mobilization with an IC50 of 1.10 nM. PF-6870961 serves as a valuable tool in research focused on GHSR signaling pathways and their physiological roles.
  3. GH Secretagogue

    L-163255 free base is an orally active spiropiperidine that functions as a growth hormone (GH) secretagogue. This compound has been shown to elevate plasma levels of insulin-like growth factor I (IGF-I), making it a valuable tool for research into GH regulation and its effects on various physiological processes. Its unique mechanism of action supports studies in endocrinology and metabolic research.
  4. GHSR

    GHRF, mouse is a peptide composed of 44 amino acids that acts as a growth hormone-releasing factor primarily targeting GHSR. This reagent stimulates the release and synthesis of growth hormone, playing a crucial role in growth regulation and metabolic functions. It is widely utilized in research applications focusing on endocrinology, growth disorders, and the mechanisms of hormone action.
  5. GHSR

    Obestatin (rat) is a 23-amino acid peptide encoded by the Ghrelin gene that primarily targets the G-protein coupled receptor 39 (GHSR). It plays a critical role in regulating food intake, inhibiting jejunal contractions, and promoting weight management. Additionally, obestatin exhibits anti-inflammatory, cardioprotective, and antioxidant properties, making it a valuable reagent for research in metabolic disorders and cardiovascular health.
  6. GHS-R1a Inverse Agonist

    AZ-GHS-22 is a potent inverse agonist targeting the growth hormone secretagogue receptor type 1a (GHS-R1a) with an IC50 of 0.77 nM. This compound exhibits significant inhibition of receptor activity, making it a valuable tool for research into metabolic regulation and appetite control. AZ-GHS-22 is particularly useful for studies focused on obesity and related disorders, enabling exploration of the physiological roles of GHS-R1a in non-central nervous system contexts.
  7. GH Release Inducer

    GHRF, porcine is a growth hormone releasing factor peptide that acts as a potent inducer of growth hormone (GH) release. By binding to the growth hormone secretagogue receptor (GHSR), it stimulates the secretion of GH from the anterior pituitary gland. This reagent is valuable in studies focused on growth hormone regulation, metabolic processes, and endocrine signaling pathways.
  8. GHSR Agonist

    BMS-604992 is a selective, orally active agonist of the growth hormone secretagogue receptor (GHSR). It exhibits high-affinity binding with a Ki of 2.3 nM and demonstrates potent functional activity with an EC50 of 0.4 nM. This compound has been shown to effectively stimulate food intake in rodent models, making it valuable for research in appetite regulation and metabolic studies.
  9. GHSR1a Agonist

    PF-6870961 hydrochloride is a potent inverse agonist of GHSR1a, exhibiting Ki values of 73.6 nM for human GHSR, 239 nM for rat GHSR, and 217 nM for dog GHSR. It effectively inhibits GHSR1a-induced inositol phosphate (IP) accumulation with an IC50 of 300 nM and demonstrates a strong inhibition of constitutive GHSR1a β-arrestin mobilization with an IC50 of 1.10 nM. This compound is relevant for research applications exploring the physiological roles of GHSR1a in metabolic and neuroendocrine processes.
  10. Growth Hormone-releasing Factor

    GHRF, bovine (bGRF(1-44)-NH2) is a peptide that functions as the Growth Hormone-releasing Factor, stimulating the secretion of bovine growth hormone (GH). This compound is essential for studying GH release mechanisms and is utilized in research involving growth regulation and metabolic processes. Furthermore, GHRF, bovine exhibits a synergistic effect when combined with Hydrocortisone, enhancing its biological activity.
  11. Ghrelin Receptor Agonist

    K-(D-1-Nal)-FwLL-NH2 is a potent inverse agonist of the ghrelin receptor, exhibiting a high affinity with an EC50 of 3.4 nM and a Ki of 4.9 nM. This compound is instrumental for studies related to obesity, providing valuable insights into the regulation of appetite and energy balance. Its specificity and efficacy make it a relevant tool for investigating the physiological and pathological roles of ghrelin signaling.
  12. GHSR Agonist

    Macimorelin is a potent GHSR agonist that serves as a growth hormone secretagogue. It effectively stimulates the release of growth hormone, making it a valuable tool in the investigation of adult growth hormone deficiency (AGHD) and cancer anorexia-cachexia syndrome (CACS). This compound is instrumental in research aimed at understanding the physiological roles of growth hormone and its potential therapeutic applications in these conditions.
  13. GHSR Agonist

    BMS-604992 dihydrochloride is a selective agonist of the growth hormone secretagogue receptor (GHSR), exhibiting high-affinity binding with a Ki of 2.3 nM and potent functional activity with an EC50 of 0.4 nM. This small-molecule compound has been shown to stimulate food intake in rodent models, making it a valuable tool for studies related to appetite regulation and metabolic disorders. Its distinctive mechanism and efficacy position BMS-604992 dihydrochloride as an important reagent for research in endocrinology and neurobiology.
  14. ASM Inhibitor

    KARI 201 is a selective, brain-penetrant competitive inhibitor of acid sphingomyelinase (ASM), exhibiting an IC50 of 338.3 nM. This compound acts as a ghrelin receptor agonist and demonstrates significant potential in ameliorating neuropathological features associated with Alzheimer's disease. KARI 201 is valuable for research investigating the modulation of ASM activity and its implications in neurodegenerative disorders.
  15. GHS-R Agonist

    BMS-317180 is a potent and orally active agonist of the growth hormone secretagogue receptor (GHS-R), with an EC50 of 7.9 nM. This compound effectively stimulates the endogenous release of growth hormone. BMS-317180 is suitable for research applications related to age-related frailty, osteoporosis, and cancer cachexia.
  16. Growth Hormone Receptor Antagonist

    Tezusomant is a growth hormone receptor antagonist that effectively inhibits the activity of growth hormone. This compound is instrumental in investigating conditions related to excessive growth hormone secretion, such as acromegaly and related endocrine disorders. Tezusomant facilitates research aimed at understanding the underlying mechanisms of these diseases and exploring potential therapeutic interventions.
  17. GHRH Antagonist

    JV-1-36 is a growth hormone-releasing hormone (GHRH) antagonist. This compound effectively inhibits the production of reactive oxygen species in A549 lung cancer cells, making it a valuable tool for investigating the biological effects of GHRH antagonists. Research applications include in vitro studies focused on cancer biology and role of GHRH in tumorigenesis.
  18. Growth Hormone-Releasing Factor

    GHRF, ovine is a growth hormone-releasing factor that specifically stimulates the secretion of pituitary growth hormone (GH). It plays a crucial role in the physiological response to hypoglycemia, enhancing GH release to regulate metabolic processes. This reagent is utilized in research focused on growth hormone regulation, metabolic disorders, and endocrine system studies.
  19. Growth Hormone Secretagogue Agonist

    L-692429 hydrochloride is a nonpeptidyl growth hormone secretagogue (GHS) agonist and a benzolactam derivative, primarily targeting the growth hormone secretagogue receptor. With a binding affinity characterized by a Ki of 63 nM, this compound effectively stimulates growth hormone release, making it valuable for studies in endocrine regulation and metabolic research. Its applications extend to investigating the physiological roles of growth hormone and exploring therapeutic avenues for growth-related disorders.
  20. Ghrelin Receptor Agonist

    GSK894281 is a highly potent ghrelin receptor agonist exhibiting a pEC50 of <4.9 at the human motilin receptor. This compound demonstrates the ability to penetrate the central nervous system effectively. GSK894281 is primarily utilized in research applications related to gastrointestinal function, particularly for investigating therapies for constipation and facilitating colonic emptying prior to procedures such as colonoscopy or colon surgery.
  21. GHSR

    JMV 3002 is a potent antagonist of the growth hormone secretagogue receptor (GHSR). It exhibits significant biological activity by inhibiting hexarelin-stimulated food intake in rat models, achieving up to 98% reduction at a dose of 80 μg/kg. JMV 3002 does not induce release of growth hormone on its own, nor does it inhibit hexarelin-stimulated growth hormone secretion in infant rats at a dose of 160 μg/kg. This compound is valuable for research focused on energy homeostasis and the regulation of appetite.
  22. GHSR-1a Agonist

    GHSR-1a agonist-1 is a potent agonist of the human growth hormone secretagogue receptor 1a (GHSR-1a), exhibiting an EC50 value of 0.49 nM. This compound effectively stimulates the release of endogenous growth hormone, making it valuable for investigating growth and developmental processes. In preclinical studies, oral administration at a dosage as low as 0.1 mg/kg led to significant increases in body weight and length in 4-week-old rats, supporting its potential applications in addressing growth and development retardation in pediatric research.
  23. GHS-R1a Antagonist

    JMV 3008 is a GHS-R1a antagonist with an IC50 of 5.6 nM, effectively inhibiting the growth hormone secretagogue receptor 1a. This compound demonstrates potential in the study of metabolic disorders, including diabetes and obesity, by modulating appetite and energy homeostasis. Research involving JMV 3008 can contribute valuable insights into therapeutic strategies targeting these diseases.
  24. GHSR Inverse Agonist

    KwFwLL-NH2 is a hexapeptide that functions as an inverse agonist at the growth hormone secretagogue receptor (GHSR). This compound demonstrates moderate potency with an EC50 of 45.6 nM, making it a valuable tool for investigating the role of ghrelin signaling in various biological processes. It is applicable in research focused on appetite regulation, metabolic disorders, and potential therapeutic interventions targeting the ghrelin pathway.
  25. GLP-1R Agonist

    Lotiglipron is an orally active GLP-1 receptor agonist that plays a crucial role in enhancing glucose-dependent insulin secretion and reducing appetite. This compound is primarily utilized in research related to Type 2 diabetes mellitus (T2DM) and metabolic disorders, demonstrating significant effects on glycemic control and weight management. Its unique mechanism makes Lotiglipron a valuable tool for studying potential therapeutic strategies in diabetes treatment.
  26. Semaglutide Intermediate

    tBuO-Ste-Glu(AEEA-AEEA-OH)-OtBu is a key intermediate in the synthesis of Semaglutide, a glucagon-like peptide 1 receptor (GLP-1R) agonist. This compound is essential for facilitating the development of therapeutics targeting GLP-1R, which plays a crucial role in glucose metabolism and appetite regulation. Research applications include the study of metabolic disorders and the development of obesity and diabetes treatments.
  27. GLP-1R Agonist

    Aleniglipron is a potent glucagon-like peptide-1 receptor (GLP-1R) agonist that exhibits an EC50 value of less than 0.1 nM in human-derived beta (HDB) cell lines through cAMP stimulation assays. This compound selectively activates the Gαs-cAMP signaling pathway of GLP-1R, avoiding β-arrestin recruitment. Aleniglipron is demonstrated to enhance insulin release, improve glucose clearance, reduce food intake, and promote weight loss. It serves as a valuable tool in research focused on type 2 diabetes and obesity.
  28. GLP-1 Analog

    GLP-1 (7-36), amide, biotin labeled is a biotinylated analog of human Glucagon-Like Peptide 1, specifically comprising the C-terminal region. This compound serves as a valuable tool for studying GLP-1 receptor interactions and signaling pathways. It is commonly utilized in research applications focused on metabolic disorders, diabetes, and obesity, providing insights into peptide hormone functions and their implications in therapeutic development.
  29. GPCR Agonist

    Tryptophan-cholic acid (Trp-CA) serves as an agonist for the orphan G protein-coupled receptor MRGPRE, exhibiting an EC50 of 9.6 μM. This compound facilitates the secretion of glucagon-like peptide GLP-1, improving glucose tolerance in diabetic mouse models. Although Trp-CA is orally effective, its poor absorption and inability to cross the blood-brain barrier limit its systemic application. Its primary research applications focus on understanding mechanisms in type 2 diabetes (T2D) and investigating treatments for insulin secretion and hepatic steatosis associated with high-fat diets.
  30. GLP-1R PAM

    V-0219 is an orally active positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R). This compound enhances GLP-1R signaling, making it a valuable tool for studying therapeutic strategies in obesity-associated diabetes and related metabolic disorders. Its mechanism of action offers potential insights into the modulation of glucose homeostasis and appetite regulation.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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