GPCR/G Protein

Items 5151-5200 of 6977

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  1. GLP-1R Agonist

    (Asp28)-Exenatide is a potent GLP-1 receptor agonist known for its role in glucose homeostasis. This compound is a degradation product of exenatide and retains significant biological activity, making it valuable for research applications related to diabetes and metabolism. (Asp28)-Exenatide may provide insights into the pharmacological mechanisms of GLP-1R stimulation and its effects on insulin secretion and appetite regulation.
  2. GLP-1 Receptor Agonist

    Vensemaglutide is a GLP-1 receptor agonist that enhances insulin secretion and inhibits glucagon release in a glucose-dependent manner. This compound demonstrates significant biological activity in regulating blood glucose levels and promoting weight loss, making it useful for research in diabetes and other metabolic disorders. Its mechanism of action supports investigations into therapeutic strategies for managing conditions related to glucose homeostasis.
  3. GLP-1R Agonist

    Taspoglutide acetate is a selective agonist of the glucagon-like peptide-1 receptor (GLP-1R), exhibiting a Ki value of 1.1 nM. This compound effectively stimulates cAMP accumulation in CHO-K1 cells expressing human GLP-1R, with an EC50 of 0.06 nM. In vivo studies demonstrate that Taspoglutide acetate significantly reduces blood glucose levels and elevates insulin levels in Zucker diabetic obese rats. Additionally, it has been shown to lower gastric inhibitory polypeptide (GIP) levels, plasma triglycerides, and body weight in this model, highlighting its potential for metabolic research and diabetes treatment.
  4. GLP-1R/GIPR Agonist

    Poterepatide is a long-acting dual agonist of the GLP-1 receptor (GLP-1R) and glucose-dependent insulinotropic peptide receptor (GIPR). It demonstrates significant activity at both receptor sites, making it a valuable tool in the investigation of metabolic disorders. Poterepatide is primarily utilized in research focused on obesity and type 2 diabetes, offering insights into potential therapeutic strategies for these conditions.
  5. GLP-1 Receptor Agonist

    Zovaglutide is a long-acting GLP-1 receptor agonist that enhances albumin binding capacity through dual fatty acid chain modification. It mediates metabolic effects via central and peripheral GLP-1 pathways, promoting satiety, reducing caloric intake, and enhancing glucose-dependent insulin secretion, without affecting GIP or glucagon receptors. This compound is well-suited for research applications related to type 2 diabetes and obesity.
  6. GLP-1R Agonist

    Anvoglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist that plays a significant role in the regulation of glucose metabolism and appetite control. This compound exhibits potent antidiabetic and anti-obesity properties, making it a valuable tool for research in metabolic disorders. Its ability to enhance insulin secretion and reduce glucagon levels supports its application in studies focused on type 2 diabetes and weight management interventions.
  7. GLP-1R Agonist

    GLP-1R modulator-1 is a potent selective agonist of the glucagon-like peptide-1 receptor (GLP-1R), acting primarily through G-protein coupled signaling pathways. This compound elevates intracellular cAMP levels, facilitating insulin secretion, delaying gastric emptying, and suppressing appetite. GLP-1R modulator-1 is valuable for research in type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH).
  8. GLP-1 Agonist

    Liraglutide acetate is an acetate derivative of Liraglutide, a glucagon-like peptide-1 (GLP-1) receptor agonist. It is primarily utilized in the management of type 2 diabetes by enhancing insulin secretion, suppressing glucagon release, and promoting glucose-dependent regulation of blood sugar levels. Research applications include studies on metabolic disorders, appetite regulation, and cardiovascular effects related to GLP-1 signaling.
  9. GLP-1R Agonist

    GLP-1R-agonist-43 is a potent GLP-1 receptor agonist with an EC50 of 2.68 nM, demonstrating significant biological activity. This compound is primarily utilized in research focused on non-insulin-dependent diabetes mellitus (type 2 diabetes) and obesity. Its capacity to stimulate the GLP-1 receptor makes it a valuable tool for investigating metabolic disorders and potential therapeutic interventions.
  10. GLP-1R Agonist

    GLP-1R agonist 36 is a selective agonist for the glucagon-like peptide-1 receptor (GLP-1R), exhibiting activity through receptor activation. This compound plays a crucial role in regulating glucose homeostasis and appetite control, making it a valuable tool in diabetes and obesity research. Its multiple isomers allow for comprehensive studies on receptor interaction and therapeutic potential.
  11. GLP Receptor Agonist

    GLP-1R agonist 42 is a potent agonist of the glucagon-like peptide-1 receptor (GLP-1R), exhibiting an EC50 of 0.0122 nM. This compound effectively stimulates insulin secretion and modulates glucagon release, making it relevant for diabetes research. Its application in metabolic studies provides insights into glucose homeostasis and potential therapeutic targets for metabolic disorders.
  12. GLP-1 Receptor Agonist

    Berobenatide is a selective glucagon-like peptide-1 (GLP-1) receptor agonist, which stimulates insulin secretion and inhibits glucagon release in a glucose-dependent manner. This compound plays a crucial role in enhancing glucose homeostasis and promoting weight loss. Berobenatide is primarily utilized in research related to diabetes management and obesity treatment.
  13. GLP-1R Agonist

    GLP-1R agonist 23 is a potent agonist of the GLP-1 receptor, exhibiting an EC50 of 0.056 nM. This compound plays a critical role in enhancing insulin secretion and glucose homeostasis, making it valuable for diabetes research and therapeutic applications. Its high affinity and specificity for GLP-1R support studies aimed at understanding glucoregulatory mechanisms and developing potential treatments for metabolic disorders.
  14. GLP-1 Receptor Agonist

    GLP-1R Agonist 13 is a selective agonist of the GLP-1 receptor, which plays a crucial role in glucose metabolism and appetite regulation. This compound exhibits potent biological activity by enhancing insulin secretion and inhibiting glucagon release, making it a valuable tool for diabetes research. Its application extends to studying metabolic disorders and evaluating potential therapeutic strategies for conditions such as type 2 diabetes and obesity.
  15. Glucagon Peptide

    (Asp28)-Glucagon (1-29) is a modified form of the glucagon peptide, where aspartic acid (Asp) has been introduced at position 28 to enhance its aqueous solubility in physiological pH buffers. This structural optimization preserves the biological activity characteristic of glucagon. It serves as a valuable reagent for research applications that investigate glucagon's role in glucose metabolism, diabetes, and other metabolic disorders in human, rat, and porcine models.
  16. GLP-1 Agonist

    GLP-1 Receptor Agonist 16 is a potent agonist of the GLP-1 receptor, primarily involved in regulating glucose metabolism and appetite. This compound demonstrates significant biological activity in modulating insulin secretion and promoting weight loss. It is particularly valuable in research focused on diabetes, obesity, and nonalcoholic steatohepatitis-related conditions.
  17. GLP-1R Agonist

    GLP-1R agonist 30 is a highly selective and orally active agonist of the glucagon-like peptide-1 receptor (GLP-1R), demonstrating an EC50 of 0.048 nM. It displays significant selectivity with EC50 values greater than 20 μM for GLP-2 receptor, GIP receptor, and glucagon receptor. This compound enhances cAMP signaling while minimizing hERG inhibition, indicating favorable safety profiles. It effectively improves glucose tolerance and promotes insulin secretion in B-hGLP1R knock-in mouse models, making it a valuable tool for research applications in diabetes and metabolic disorders.
  18. GLP-1R/GIPR Agonist

    Brenipatide is a dual agonist of the glucagon-like peptide-1 (GLP-1) receptor and the gastric inhibitory polypeptide (GIP) receptor. It is primarily utilized in researching metabolic disorders, obesity, and diabetes, demonstrating significant potential in enhancing insulin secretion and promoting weight loss. This compound is essential for studies investigating the pathways and mechanisms involved in glucose homeostasis and energy balance.
  19. GLP-1 Receptor Agonit

    Utreglutide is a potent glucagon-like peptide-1 (GLP-1) receptor agonist that plays a significant role in the regulation of glucose metabolism. This compound not only aids in lowering blood pressure and blood lipid levels but also contributes to weight reduction and enhances cardiovascular health. Utreglutide is particularly valuable in research focusing on type 2 diabetes and obesity-related conditions, facilitating a deeper understanding of metabolic disorders.
  20. GLP-1R Agonist

    CHU-128 is a selective GLP-1 receptor (GLP-1R) agonist that effectively activates the Gs/cAMP signaling pathway. This compound is characterized by its strong signal specificity, as it does not engage the Gq/calcium signaling pathway, ERK phosphorylation, or recruit β-inhibitory proteins. CHU-128 is suitable for research applications focused on type 2 diabetes and related metabolic disorders.
  21. GLP-1 Receptor Positive Allosteric Modulator

    GLP-1R agonist 39 is a potent positive allosteric modulator of the GLP-1 receptor. This compound enhances the activity of the GLP-1 receptor, making it valuable for studies related to obesity and type 2 diabetes. Its application in research enables the exploration of therapeutic strategies aimed at metabolic disorders.
  22. GLP-1R Agonist

    GLP-1R agonist 38 is a selective agonist of the glucagon-like peptide-1 receptor (GLP-1R). This compound exhibits significant biological activity in enhancing insulin secretion, suppressing glucagon release, and promoting weight reduction, making it a valuable tool for studying metabolic disorders. It is applicable in research related to type II diabetes mellitus (T2DM), obesity, and non-alcoholic fatty liver disease (NASH).
  23. GLP-1 Receptor Agonist

    GLP-1 Receptor Agonist 18 is a potent GLP-1 receptor agonist with an EC50 of 0.22 nM. This compound demonstrates significant biological activity by lowering blood glucose levels and promoting weight loss, making it valuable for diabetes research. Its efficacy in modulating GLP-1 receptor signaling positions it as a useful tool for investigating therapeutic strategies in metabolic disorders.
  24. GLP-1R Agonist

    GLP-1R agonist 26 is a potent agonist of the glucagon-like peptide-1 receptor (GLP-1R), exhibiting an EC50 of less than 10 nM. This compound plays a crucial role in enhancing insulin secretion, promoting weight loss, and exhibiting cardioprotective effects. It is primarily utilized in research focused on metabolic disorders, diabetes, and obesity treatment.
  25. GLP-1R Agonist

    GLP-1R agonist 29 is a potent agonist of the GLP-1 receptor, effectively stimulating cAMP production with an EC50 value of 0.018 nM. This compound demonstrates favorable pharmacokinetic properties, evidenced by a robust body exposure reflected in an AUC0-∞,sc of 77688 ng·h/mL. It serves as a valuable tool for research applications related to metabolic disorders and diabetes, allowing for exploration of GLP-1R signaling pathways.
  26. GLP-1R Agonist

    GLP-1R Agonist 25 is a selective agonist for the glucagon-like peptide-1 receptor (GLP-1R), exhibiting an EC50 value of 0.167 nM. This compound plays a crucial role in stimulating insulin secretion and regulating glucose metabolism, making it a valuable tool for research focused on type II diabetes and related metabolic disorders. Its potent biological activity supports the exploration of therapeutic strategies aimed at improving glycemic control.
  27. GPR120 Agonist

    AZ13581837 is a potent GPR120 agonist, demonstrating human and mouse EC50 values of 5.2 nM and 4.3 nM, respectively. This compound activates Gαq, Gαs, and β-arrestin signaling pathways, effectively reducing cAMP levels, stimulating GLP-1 secretion, promoting glucose lowering, and enhancing insulin secretion. AZ13581837 is valuable for research related to type 2 diabetes, providing insights into potential therapeutic strategies targeting metabolic disorders.
  28. GPR119 Agonist

    AS1269574 is a potent agonist of GPR119, exhibiting an EC50 of 2.5 μM in HEK293 cells expressing the human receptor. This compound activates TRPA1 cation channels, thereby facilitating the secretion of glucagon-like peptide-1 (GLP-1). Notably, AS1269574 induces glucose-dependent insulin secretion from pancreatic β-cells exclusively under high-glucose conditions, making it a valuable tool for research into type 2 diabetes.
  29. GPR119 Agonist

    K-833 is a potent GPR119 agonist with EC50 values of 39.8 nM in humans, 100 nM in mice, 75.4 nM in rats, and 12.6 nM in dogs. This compound enhances GLP-1 secretion and exhibits a synergistic effect on GLP-1 levels when administered alongside AM-5262 in acute gut peptide secretion assays in mice. K-833 is suitable for research focusing on weight loss and metabolic regulation.
  30. H1R Antagonist

    Fexofenadine Impurity F is a derivative of Fexofenadine, primarily acting as a histamine H1 receptor (H1R) antagonist. This compound exhibits biological activity associated with anti-allergic properties, making it relevant in the study of allergic reactions and potential therapeutic interventions for conditions such as seasonal allergic rhinitis and chronic idiopathic urticaria. It serves as a useful reagent for research in drug development and impurity profiling.
  31. Active Metabolite of Cannabinol

    11-Hydroxy cannabinol is an active metabolite of Cannabinol, primarily targeting cannabinoid receptors in the endocannabinoid system. This compound exhibits biological activity that may influence numerous physiological processes, including pain modulation and anti-inflammatory effects. It is utilized in preclinical research to explore therapeutic applications related to cannabinoid signaling pathways and their potential impact on various health conditions.
  32. Xylazine Metabolite

    2,6-Dimethylphenylthiourea is a metabolite of xylazine, an established α2-adrenergic agonist. This compound serves as a valuable tool in pharmacological research, specifically in studies examining the metabolic pathways of xylazine and its effects on α2-adrenergic receptors. It provides insights into its pharmacokinetics and potential physiological implications.
  33. Adenosine A2A Receptor Inhibitor

    4-Desmethyl Istradefylline is a selective adenosine A2A receptor antagonist, serving as a significant metabolite of Istradefylline. With a Ki of 2.2 nM, it demonstrates potent inhibition of the A2A receptor, making it relevant for exploring therapeutic strategies in Parkinson's disease and related neurological disorders. Its oral bioactivity allows for convenience in in vivo research applications targeting adenosine signaling pathways.
  34. Stable Isotope

    Quetiapine Sulfoxide-d8 is a deuterated analog of Quetiapine sulfoxide, a primary metabolite of the second-generation antipsychotic Quetiapine. This compound acts as a 5-HT receptor agonist and dopamine receptor antagonist, playing a critical role in the pharmacokinetic studies of Quetiapine metabolism. Quetiapine Sulfoxide-d8 is commonly utilized in research applications involving drug metabolism, pharmacology, and analytical chemistry, particularly in the development and validation of quantitation methods in biological samples.
  35. Pergolide Metabolite

    Pergolide sulfone is a metabolite of Pergolide, primarily acting as a dopamine receptor agonist. This compound exhibits significant dopaminergic activity, making it relevant for research into Parkinson's disease and other neurological disorders. Pergolide sulfone can be utilized in studies investigating the pharmacological profiles of dopamine receptor interactions and their implications in neurodegenerative conditions.
  36. Drug Derivative

    (±)-p-Fluoro pseudoephedrine hydrochloride is a drug derivative associated with the pharmacological activity of pseudoephedrine. This compound exhibits decongestant properties, primarily functioning as a sympathomimetic agent that influences adrenergic receptors. Its biological activity is employed in studies related to respiratory distress, providing valuable insights into drug metabolism and therapeutic efficacy in treatments for nasal congestion.
  37. MMB-CHMICA Metabolite

    MMB-ICA is a metabolite of MMB-CHMICA, primarily targeting the cannabinoid receptor system. This compound demonstrates significant biological activity in modulating receptor signaling pathways, making it valuable for research in cannabinoid pharmacology. MMB-ICA is utilized in studies investigating the therapeutic potential of cannabinoids and their metabolic pathways.
  38. PB-22 Metabolite

    PB-22 N-(5-Hydroxypentyl)-3-carboxyindole metabolite is a primary metabolite of the cannabinoid PB-22. This compound exhibits biological activity through its interaction with the endocannabinoid system, influencing cannabinoid receptor signaling pathways. It is utilized in research to explore the metabolic pathways of synthetic cannabinoids and their pharmacological effects in various biological systems.
  39. Drug Metabolite

    Reduced Haloperidol, a primary metabolite of Haloperidol, functions as a dopamine receptor antagonist. It exhibits significant antipsychotic activity, primarily utilized in research related to schizophrenia and other psychotic disorders. This compound is instrumental in studies investigating the modulation of neurotransmitter systems, aiding in the reduction of hallucinations and delusions associated with these conditions.
  40. Clonidine Metabolite

    4-Hydroxyclonidine is a metabolite of Clonidine, primarily functioning as an alpha-2 adrenergic agonist. It exhibits comparable potency to Clonidine in displacing labeled Clonidine from specific antibodies. This compound is of significant interest in pharmacological research, particularly in studies examining adrenergic receptor interactions and the metabolic pathways of antihypertensive agents.
  41. Propranolol Active Metabolite

    Norpropranolol hydrochloride is the active metabolite of Propranolol, primarily targeting beta-adrenergic receptors. It exhibits significant cardiovascular effects, including the reduction of heart rate and blood pressure. This compound is used in research applications focused on studying cardiovascular pharmacology and the modulation of stress response pathways.
  42. Bufuralol Metabolite

    4-Hydroxybufuralol is a primary metabolite of Bufuralol, known for its significant role in pharmacokinetics. It exhibits interactions with beta-adrenergic receptors, contributing to cardiovascular research applications. This compound is essential for studies focused on drug metabolism and the pharmacological effects of beta-blockers.
  43. PB-22 Metabolite

    PB-22 N-(4-Hydroxypentyl)-3-carboxyindole metabolite is a significant metabolite of the synthetic cannabinoid PB-22. This compound interacts primarily with cannabinoid receptors, influencing cannabinoid signaling pathways. It is valuable for research applications focused on studying the metabolism and pharmacological effects of cannabinoids, as well as providing insights into potential therapeutic uses and regulatory impacts associated with cannabinoid exposure.
  44. Alprenolol Metabolite

    4-Hydroxyalprenolol is a metabolite of the β-receptor blocker Alprenolol, known for its role in modulating adrenergic signaling. This compound exhibits biological activity related to cardiovascular function and may be utilized in research focused on the pharmacokinetics and pharmacodynamics of β-blockers. Its analysis can provide insights into the metabolism of therapeutic agents and their effects on β-adrenergic receptors.
  45. MMB-CHMICA Metabolite

    AB-INACA is a metabolite of the synthetic cannabinoid AB-CHMINACA, acting primarily on the cannabinoid receptors. This compound has been utilized in research to investigate synthetic cannabinoid metabolism and receptor interaction dynamics. Its biological activity provides valuable insights into the pharmacological pathways of synthetic cannabinoids, making it a useful tool for toxicological studies and drug metabolism research.
  46. 5-HT Metabolite

    5-Hydroxy NMT oxalate is a metabolite of serotonin (5-HT) that functions as a neuromodulator. This compound has been implicated in various neurophysiological processes and is associated with cocaine addiction, as elevated plasma levels have been observed in affected individuals. Its utility in research extends to the study of serotonergic signaling pathways and addiction-related behaviors.
  47. Platelet Aggregation Inhibitor

    U-51605 is a platelet aggregation inhibitor that targets thromboxane synthesis. It also functions as a prostaglandin I2 synthase inhibitor and has been shown to block retinal vasodilation responses induced by nitric oxide donors like NOR3. This reagent is valuable for research applications focusing on cardiovascular health and vascular biology.
  48. S1P₁ Agonist

    PPI-4955 is a selective agonist of the sphingosine-1-phosphate receptor subtype 1 (S1P₁), displaying an EC50 of 1.62 nM. Its active phosphorylated form, PPI-4955-P, demonstrates exceptional receptor selectivity, with IC50 values of 0.23 nM for hS1P₁, 2000 nM for hS1P₃, 6.5 nM for hS1P₄, and 184 nM for hS1P₅. This compound significantly enhances in vivo phosphorylation efficiency, leading to lymphocyte reduction and a potential decrease in cardiovascular risk. PPI-4955 is applicable for research in immunomodulation and cardiovascular studies.
  49. TRPA1 Channel Antagonist

    ADM 12 is a selective antagonist of the transient receptor potential ankyrin 1 (TRPA1) channel. It effectively inhibits nitroglycerin-induced trigeminal hyperalgesia in animal models, leading to decreased expression of pain-related genes such as c-Fos and TRPA1, as well as neuropeptides including CGRP and substance P. This compound holds potential for research applications in the fields of migraine and neuropathic pain.
  50. TRP Channel Inhibitor

    Cannabidiorcol (CBDO) is an inhibitor of transient receptor potential (TRP) channels. This compound, structurally related to cannabidiol with a shortened pentyl side chain, exhibits anti-inflammatory properties while displaying low affinity for cannabinoid receptors. Research applications include investigations into its potential role in modulating inflammation and exploring its effects on tumorigenesis at elevated concentrations.

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