Catalog No.
Product Name
Application
Product Information
Citations
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GPR81 Agonist
3,5-Dihydroxybenzoic acid is an agonist of the hydroxycarboxylic acid receptor 1 (HCA1, also referred to as GPR81), known for its role in inhibiting lipolysis in adipocytes. This compound serves as a potential biomarker for the consumption of various food products, including beer, nuts, peanuts, and pulses. Additionally, 3,5-Dihydroxybenzoic acid acts as a competitive inhibitor for tyrosine phenol-lyase (TPL), with an affinity constant of Ki = 25.7 μM. Its oral bioactivity makes it suitable for various research applications in metabolic studies. -
GPR81 Agonist
GPR81 Agonist 2 specifically targets the GPR81 receptor, exhibiting potent agonistic activity with EC50 values of 0.023 µM for human GPR81 and 0.123 µM for human GPR109A. This compound is valuable for research in metabolic regulation, insulin sensitivity, and tumor metabolism. Its ability to selectively activate GPR81 makes it a useful tool for probing signaling pathways related to energy homeostasis and lipid metabolism. -
GPR54 Ligand
Kisspeptin-10, human is a potent ligand for the GPR54 receptor, playing a significant role in multiple biological processes. It functions as an inhibitor of angiogenesis and a tumor metastasis suppressor. The Kisspeptin-10/GPR54 signaling pathway is also crucial in embryonic kidney development and promotes osteoblast differentiation through NFATc4-mediated BMP2 expression. This makes Kisspeptin-10 a valuable reagent for research in developmental biology and cancer metastasis. -
KISS1/GPR54 Antagonist
Kisspeptin 234 TFA is a 10 amino acid peptide that acts as an antagonist of the kisspeptin receptor, specifically KISS1/GPR54. This reagent serves as a valuable tool in research applications related to reproductive physiology, neuroendocrine function, and the regulation of puberty. Its ability to modulate the kisspeptin signaling pathway makes it important for investigating the roles of kisspeptins in various biological processes. -
GPR54 Activator
Kisspeptin-14 human is a peptide hormone that serves as an endogenous ligand for the G protein-coupled receptor, GPR54. It plays a crucial role in reproductive function and has been shown to activate various intracellular signaling pathways upon binding to KISS1R. This compound is instrumental in research focused on reproductive development and the mechanisms underlying tumor metastasis. Kisspeptin-14 human exhibits receptor binding efficiency and potency comparable to full-length kisspeptin, making it a valuable tool in beta-cell and endocrine research. -
GPR54 Ligand
Kisspeptin-10 (mouse, rat) is a specific ligand for the GPR54 receptor, primarily influencing reproductive functions. This peptide demonstrates significant vasoconstrictive properties and acts as an inhibitor of angiogenesis. Additionally, Kisspeptin-10 has been shown to mitigate Methotrexate-induced reproductive toxicity, suggesting its potential role as an antioxidant in various research applications. -
Metastin/GPR54 Agonist
TAK-683 is a potent full agonist of the KISS1 receptor (KISS1R), exhibiting an IC50 value of 170 pM and a remarkable metabolic stability. As a nonapeptide analog of metastin, TAK-683 demonstrates significant agonistic activity with EC50 values of 0.96 nM and 1.6 nM for human and rat KISS1R, respectively. This compound effectively depletes GnRH in the hypothalamus and subsequently lowers plasma levels of FSH, LH, and testosterone. TAK-683 is valuable for investigating hormone-dependent prostate cancer and related endocrine research applications. -
KISS1/GPR54 Antagonist
Kisspeptin 234 is a 10-amino acid peptide that acts as an antagonist of the kisspeptin receptor (KISS1, GPR54). This compound is a structural analog of Kisspeptin 10 and is utilized in research to investigate the role of kisspeptin signaling in reproductive biology and neuroendocrine regulation. Its ability to inhibit KISS1/GPR54 interactions makes it a valuable tool for studying the modulation of hormonal pathways and physiological responses associated with reproductive health. -
LPA5/GPR92 Antagonist
TC LPA5 4 is a selective antagonist of LPA5 (GPR92) with a non-lipid structure. It effectively inhibits LPA-induced aggregation of isolated human platelets, demonstrating an IC50 value of 800 nM. Additionally, TC LPA5 4 shows potent inhibition of cell proliferation and migration in thyroid cancer cells, making it a valuable tool for research in cancer biology and cell signaling pathways associated with LPA5. -
GPR92 Receptor Activator
1-Octadecyl lysophosphatidic acid is a GPR92 receptor (LPA5) activator implicated in various biological processes. This compound exhibits potential flavoring effects and is useful in research applications focused on cellular signaling pathways involving lysophosphatidic acid. Its role in modulating receptor activity makes it a valuable tool for investigating the physiological effects mediated by GPR92. -
GPR183 Agonist
7α,25-Dihydroxycholesterol is a potent agonist of the orphan G protein-coupled receptor GPR183 (EBI2). This compound exhibits high efficacy in activating EBI2, with an EC50 of 140 pM and a Kd of 450 pM. It plays a critical role in chemokine signaling, directing the migration of immune cells such as B cells, T cells, and dendritic cells, making it valuable for research in immunology and cell signaling pathways. -
GPR183 Antagonist
SAE-14 is a selective antagonist of GPR183, exhibiting an IC50 value of 28.5 nM. It effectively inhibits 7α, 25-OHC–induced calcium mobilization in HL-60 cells with an IC50 under 50 nM. SAE-14 has demonstrated potential in reversing allodynia in murine models, making it a valuable tool for research into pain mechanisms and immune regulation. -
GPR40 Partial Agonist
MK-8666 is a potent and selective partial agonist of GPR40, with an EC50 of 0.54 nM for human GPR40. This compound exhibits significant selectivity over other G-protein-coupled receptors, including GPR119, GPR43, GPR41, and GPR120. MK-8666 has demonstrated the ability to lower glucose levels in rodent models, making it a valuable tool in type 2 diabetes research and related metabolic studies. -
GPR40/GPR84 Modulator
Fezagepras is a selective modulator of GPR40 and GPR84, functioning as an oral agonist for GPR40 while acting as an antagonist or inverse agonist for GPR84. This compound has demonstrated significant anti-fibrotic, anti-inflammatory, and anti-proliferative activities, effectively reducing renal, liver, and pancreatic fibrosis. Fezagepras holds promise for research related to metabolic disorders and fibrotic diseases, facilitating insights into the roles of GPR40 and GPR84 in various pathological conditions. -
GPR40 Agonist
SCO-267 is an allosteric full agonist of the GPR40 receptor, primarily involved in enhancing insulin secretion. This compound exhibits significant potential in the study of chronic metabolic disorders, particularly diabetes mellitus. Its distinct mechanism of action enhances glucose-dependent insulin release, making it a valuable tool for investigating therapeutic strategies in diabetes management and related metabolic diseases. -
FFAR4/GPR120 Agonist
13Z,16Z-Docosadienoic acid is an agonist of the free fatty acid receptor 4 (FFAR4 or GPR120), which is a receptor for long-chain fatty acids. This ω-6 polyunsaturated fatty acid exhibits anti-borreliae activity, making it relevant in the study of bacterial infections. Its role in modulating receptor activity positions it as a valuable tool for research on metabolic pathways and inflammatory responses associated with FFAR4 signaling. -
GPR40 Agonist
GPR40 Agonist 6 is a potent and selective agonist of the G protein-coupled receptor FFAR1 (GPR40), exhibiting an EC50 of 0.058 μM. This compound is valuable for investigating glucose homeostasis and insulin secretion pathways. It has potential applications in research related to metabolic disorders and therapeutic strategies for type 2 diabetes. -
GPR41 Agonist
GPR41 agonist-1 is a potent agonist of the G-protein coupled receptor 41 (GPR41). This compound plays a significant role in modulating metabolic processes and is particularly useful in the study of insulin-related disorders. Its ability to activate GPR41 makes it a valuable tool for researchers investigating the mechanisms underlying metabolic regulation and related diseases. -
GPR43 Inhibitor
BTI-A-404 is a selective and competitive inverse agonist of the human G protein-coupled receptor GPR43. This compound exhibits potent inhibitory activity, making it valuable for studying mechanisms related to inflammation, obesity, and type 2 diabetes. BTI-A-404 aids in elucidating the role of GPR43 in metabolic disorders and inflammatory responses, providing essential insights for therapeutic development. -
GPR120 Ligand
(±)-Pinocembrin, a GPR120 ligand, is a natural flavonoid known for its significant biological activity in promoting wound healing. It has demonstrated efficacy in modulating cellular responses in the HaCaT cell line, making it a valuable reagent for research in regenerative medicine and skin biology. Investigating its effects can provide insights into therapeutic strategies for enhancing tissue repair and inflammation resolution. -
GPR40/FFA1 Agonist
CPL207280 is an orally active agonist of GPR40/FFA1, known for its antidiabetic properties. This compound enhances glucose-stimulated insulin secretion and improves glucose tolerance in both MIN6 pancreatic β-cells and various rat models, including healthy and diabetic strains. CPL207280 serves as a valuable tool for research into type 2 diabetes mechanisms and potential therapies. -
GPR40 Agonist
LY3104607 is a selective agonist of the G protein-coupled receptor 40 (GPR40). This compound enhances the signaling pathways associated with GPR40, playing a significant role in insulin secretion and glucose metabolism. It is primarily utilized in research focused on diabetes and metabolic disorders, providing insight into potential therapeutic strategies. -
GPR40 (FFAR1) Agonist
BI-2081 is a GPR40 (FFAR1) partial agonist with an EC50 of 4 nM. This compound stimulates glucose-dependent insulin secretion and effectively lowers plasma glucose levels. BI-2081 is valuable for research applications focused on metabolic diseases, particularly type 2 diabetes. -
GPR40/FFA1 Inhibitor
AMG 837 hemicalcium is a potent partial agonist targeting the GPR40/FFA1 receptor, demonstrating high oral bioavailability. This compound inhibits [3H]AMG 837 binding at the human FFA1 receptor with a pIC50 value of 8.13. Research indicates that AMG 837 hemicalcium may enhance insulin secretion and help regulate glucose levels in rodent models, making it valuable for studies in metabolic disorders and diabetes research. -
GPR40 Full Agonist
AM-5262 is a full agonist of the GPR40 receptor, exhibiting an EC50 value of 0.081 μM. This compound is primarily utilized in research focused on type II diabetes and its associated metabolic pathways, providing valuable insights into glucose regulation and insulin secretion mechanisms. -
GPR40 Agonist
TUG-905 is a potent agonist of the GPR40 receptor, exhibiting an pEC50 value of 7.03. It demonstrates significant biological activity by promoting cell proliferation and survival in hypothalamic cells. Additionally, TUG-905 has been shown to reduce body mass while enhancing the expression of pro-opiomelanocortin (POMC) mRNA, making it a valuable tool for research into metabolic regulation and obesity-related studies. -
GPR120 Agonist
GPR120 Agonist 5 is a selective agonist for the GPR120 receptor, exhibiting an EC50 of 1.2 μM. This compound enhances the secretion of glucagon-like peptide-1 (GLP-1) through its interaction with GPR120, leading to increased insulin production and decreased blood glucose levels. Additionally, GPR120 Agonist 5 demonstrates anti-inflammatory properties, making it a valuable tool for studies focused on metabolic disorders, obesity, insulin resistance, and type 2 diabetes. This reagent is essential for investigating the biological functions and therapeutic potential of GPR120 in relevant disease models. -
GPR120 Agonist
GPR120 Agonist 4 is a potent agonist of the GPR120 receptor, demonstrating EC50 values of 1 μM and 0.35 μM for β-arrestin A and Calcium A signaling pathways, respectively. This compound is valuable in the study of type II diabetes mellitus, providing insights into the receptor's role in metabolic regulation and inflammation. Its ability to activate GPR120 makes it a significant tool for investigating therapeutic strategies in related metabolic disorders. -
GPR40 Agonist
(R)-AM-1638 is a R-isomer of AM-1638 and acts as a full agonist of the GPR40 receptor, exhibiting an EC50 of 0.16 μM. This compound plays a significant role in mediating glucose-dependent insulin secretion and is of particular interest in diabetes research. Its selectivity for GPR40 positions it as a valuable tool for studying metabolic disorders and potential therapeutic interventions. -
GPR40 Activator
GPR40 Activator 3 is a selective activator of the GPR40 receptor, known for its role in regulating lipid metabolism and inflammation. This compound demonstrates significant biological activity by mitigating pulmonary fibrosis through the inhibition of M2 macrophage polarization via the GPR40/PKD1/CD36 signaling pathway. It is valuable for research focused on metabolic disorders, immune response modulation, and fibrotic diseases. -
GPR40 Agonist
AS2575959 sodium is a potent agonist of the GPR40 receptor, which plays a crucial role in modulating glucose metabolism. This compound has demonstrated the ability to enhance insulin and incretin secretion, particularly in synergy with Sitagliptin. AS2575959 sodium is valuable for research focusing on type 2 diabetes and associated metabolic disorders. -
GPR40 Full Agonist
AM-6226 is a potent full agonist of the G protein-coupled receptor 40 (GPR40), exhibiting an EC50 of 0.12 μM. This compound effectively activates GPR40 receptors on pancreatic β cells and enteroendocrine L cells, promoting insulin secretion in a glucose-dependent manner while enhancing the release of incretin hormones like GLP-1 and GIP. AM-6226 is valuable for research into metabolic diseases, particularly diabetes, due to its potential to mitigate hypoglycemia risks. -
GPR40 Agonist
GPR40 Agonist 7 is a potent and orally active agonist of the G protein-coupled receptor GPR40. This compound enhances insulin and GLP-1 secretion, demonstrating notable hypoglycemic effects in vivo, with an effective dose (ED50) of 0.58 mg/kg. It serves as a valuable research tool for studying glucose metabolism and related metabolic disorders. -
GPR40 Agonist
Xelaglifam is a potent GPR40 agonist known for its antihyperglycemic activity. In addition to its biological properties, Xelaglifam serves as a click chemistry reagent due to the presence of an alkyne group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. This dual functionality makes Xelaglifam valuable for both therapeutic research and synthetic applications in chemical biology. -
GPR40 Agonist
MK-8666 tromethamine is a potent agonist of the GPR40 receptor, which is involved in glucose metabolism and insulin secretion. This compound is primarily utilized in the study of type II diabetes, aiding in the exploration of new therapeutic targets related to insulin sensitivity and metabolic regulation. MK-8666 tromethamine's ability to stimulate GPR40 may provide insights into novel treatments for glycemic control. -
GPR40 Agonist
GPR40 agonist 9 is a potent agonist of the G protein-coupled receptor 40 (GPR40), exhibiting an EC50 value of 0.21 nM. This compound is relevant for research focused on metabolic disorders such as type 2 diabetes and obesity, making it a valuable tool for understanding the mechanisms of these diseases and developing therapeutic strategies. -
GPR40 Agonist
BMS-986118 is a selective agonist of GPR40, exhibiting potent biological activity with an EC50 of 0.07 µM. This compound enhances insulin secretion and stimulates GLP-1 release, leading to significant reductions in plasma glucose levels in acute animal models. BMS-986118 is valuable for research in diabetes and metabolic disorders, providing insights into the regulation of glucose homeostasis. -
GPR40 Receptor Agonist
AP5 sodium is a selective GPR40 receptor agonist that functions as a positive allosteric modulator of endogenous ligands (AgoPAM). It exhibits potent biological activity, with EC50 values of 0.49 nM in rat models and 0.8 nM in human assays for inositol monophosphate (IP1) signaling. This compound holds potential for applications in type II diabetes research, contributing to the understanding of glucose metabolism and insulin secretion mechanisms. -
GPR120 Agonist
LXT34 is a potent agonist of the GPR120 receptor, demonstrating significant anti-inflammatory activity. This compound enhances GLP-1 production in the gastrointestinal tract and ameliorates insulin resistance in both macrophages and pancreatic cells. LXT34 is applicable in studies related to inflammatory diseases, including type 2 diabetes, obesity, and non-alcoholic fatty liver disease. -
GPR40 Agonist
GPR40 Agonist 8 is a potent GPR40 agonist, exhibiting an EC50 of 5 nM for human GPR40-mediated calcium signaling. This compound plays a crucial role in the activation of GPR40, making it a valuable tool for research focused on metabolic disorders, including Type II diabetes and obesity. Its high specificity and efficacy enable investigations into therapeutic strategies targeting GPR40 pathways. -
GPR40 Agonist
LY2881835 is a selective agonist of the G protein-coupled receptor 40 (GPR40), demonstrating potent activity in promoting the secretion of insulin and GLP-1, while effectively lowering glucose levels in a dose-dependent manner. This compound shows promise for research applications related to type 2 diabetes mellitus. Additionally, LY2881835 features an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) for click chemistry experiments. -
GPR40 Agonist
AM-3189 is a selective agonist of GPR40, with EC50 values of 33 nM in buffer and 10 μM in 100% human serum. This compound enhances glucose-stimulated insulin secretion from pancreatic β cells, offering potential therapeutic applications in type 2 diabetes research. Importantly, AM-3189 shows minimal activity on GPR41, GPR43, and PPAR subtypes, and exhibits low central nervous system penetration. Its efficacy in reducing blood glucose levels has been demonstrated in humanized GPR40 mouse models, making it a valuable tool for metabolic studies. -
GPR41 Modulator
GPR41 modulator 1 is a potent agonist of the GPR41 receptor, exhibiting an EC50 value of 0.679 µM. This compound is valuable for research exploring the role of GPR41 in metabolic regulation and gut-brain signaling. Its modulatory activity makes it a useful tool for studying the physiological effects mediated by this receptor and its potential implications in metabolic disorders. -
GPR40 Agonist
Fasiglifam hemihydrate is a potent and selective agonist of the GPR40 receptor, exhibiting an EC50 value of 72 nM. This compound enhances glucose-dependent insulin secretion and has demonstrated efficacy in reducing hyperglycemia in type 2 diabetic rat models. It is important to note that Fasiglifam may also induce liver injury, warranting careful consideration in research applications. -
GPR83 Ligand
PEN (human) is an endogenous ligand of the GPR83 receptor, primarily found in the hypothalamus. This neuropeptide is derived from the proprotein ProSAAS and plays a crucial role in various biological processes, including neuroendocrine regulation and stress responses. Research applications include the investigation of GPR83 signaling pathways and the exploration of its potential roles in metabolic disorders and neuropsychiatric conditions. -
GPR83 Ligand
PEN (rat) is a potent endogenous ligand for the GPR83 receptor, primarily identified in the hypothalamic region. This neuropeptide, derived from the proprotein ProSAAS, plays a critical role in neuroendocrine regulation and appetite control. It is valuable for research focusing on metabolic disorders and neuropeptide signaling pathways. -
GPR132 Antagonist
GPR132 antagonist 1 is a selective antagonist of the GPR132 receptor, exhibiting an EC50 value of 0.075 μM. It promotes insulin secretion with an EC50 value of 0.7 μM, making it a valuable tool for research in diabetes and metabolic regulation. Its ability to modulate insulin release can be utilized in studies exploring therapeutic strategies for metabolic disorders. -
G2A/GPR132 Agonist
T-10418 is a potent and selective agonist of the G2A/GPR132 receptor, exhibiting an EC50 of 0.82 μM for human G2A activation. This compound demonstrates favorable water solubility, metabolic stability, and pharmacokinetic properties, making it suitable for in vitro and in vivo studies. T-10418 is valuable for research into various medical conditions, including neuropathic pain, acute myeloid leukemia, and inflammation. -
GPCR G2A/GPR132 Agonist
Commendamide is a potent agonist of the GPCR G2A/GPR132, exhibiting an EC50 of 11.8 μM. It plays a significant role in modulating immune responses and is valuable for research focused on autoimmunity and atherosclerosis. Its unique mechanism highlights its potential in elucidating GPCR-mediated pathways in these conditions. -
GPR39 Activator
Obestatin (rat) TFA is an endogenous peptide encoded by the Ghrelin gene, consisting of 23 amino acids, that primarily targets the G-protein coupled receptor 39 (GPR39). This compound is known to suppress food intake, inhibit jejunal contractions, and reduce body weight gain. Additionally, Obestatin (rat) TFA exhibits notable anti-inflammatory, cardioprotective, and antioxidant properties, making it valuable for research applications focused on metabolic regulation and cardiovascular health.
