Catalog No.
Product Name
Application
Product Information
Citations
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GPR68 Positive Allosteric Modulator
MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). This compound exhibits high selectivity for GPR68, minimizing off-target effects on related proton GPCRs, neurotransmitter transporters, and hERG ion channels. Additionally, MS48107 demonstrates the ability to effectively cross the blood-brain barrier in murine models, making it a valuable tool for neurobiological research and studies involving GPR68-related pathways. -
GPR84 Antagonist
GLPG1205 is a potent and selective antagonist of GPR84, a G-protein-coupled receptor implicated in various inflammatory processes. This compound demonstrates anti-inflammatory activity and is being investigated for its potential in treating pulmonary fibrosis. Additionally, GLPG1205 features an alkyne group, enabling its use as a click chemistry reagent for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing compounds. -
GPR84 Agonist
LY237 is an efficacious agonist of the G protein-coupled receptor GPR84, exhibiting a high potency with a pEC50 of 10.15. This compound is important for investigating the roles of GPR84 in various biological processes, particularly in the context of inflammation and fibrosis. Its activation of GPR84 may provide valuable insights into therapeutic strategies for related diseases. -
GPR84 Antagonist
GPR84 Antagonist 10 is a potent and orally bioavailable inhibitor of GPR84, a receptor implicated in various inflammatory pathways. This compound is useful for investigating GPR84-related diseases, particularly those driven by inflammation, such as inflammatory pain conditions. Its selective antagonism facilitates research in understanding the role of GPR84 in disease mechanisms and therapeutic potential. -
GPR84 Agonist
PSB-17365 is a potent agonist of the GPR84 receptor, demonstrating EC50 values of 2.5 nM in cAMP accumulation assays and 100 nM in β-arrestin 2 recruitment assays. This compound effectively stimulates GPR84 activity, making it a valuable tool for investigating the role of this receptor in inflammatory responses and immune modulation. Research applications include studies in metabolic disorders and the examination of GPR84's involvement in various physiological processes. -
GPR84 Antagonist
GPR84 Antagonist 3 is a selective antagonist of the G-protein-coupled receptor 84 (GPR84). This compound effectively inhibits GTPγS binding with a pIC50 value of 8.28, demonstrating its potency in modulating GPR84 activity. GPR84 Antagonist 3 is suited for research applications focused on exploring the role of GPR84 in inflammatory processes and metabolic regulation. Its favorable pharmacokinetic profile enhances its utility in pharmacological studies. -
GPR84 Agonist
ZQ-16 is a potent and selective agonist for the GPR84 receptor, exhibiting an EC50 value of 0.213 μM. This compound demonstrates specificity by showing no activity on other free fatty acid receptors (FFARs), including GPR40, GPR41, GPR119, and GPR120. ZQ-16 is useful in studies related to inflammation and immune responses, providing valuable insights into GPR84-mediated signaling pathways. -
GPR84 Agonist
OX04528 is a potent agonist of the GPR84 receptor, exhibiting G-protein biased activity. This compound demonstrates a remarkable ability to inhibit cAMP production, with an EC50 value of 0.00598 nM, and shows no signs of cytotoxicity. It is suitable for research applications focused on studying GPR84-related biological pathways and therapeutic targets. -
GPR84 Agonist
TUG-2208 is a potent agonist of GPR84, exhibiting a pEC50 of 8.98. This compound is characterized by its low lipophilicity, good solubility, and favorable in vitro permeability and microsomal stability. TUG-2208 is suitable for research applications investigating the role of GPR84 in various biological processes and potential therapeutic targets. -
GPR84 Antagonist
GPR84 antagonist 2 is a selective oral antagonist of the GPR84 receptor, exhibiting an IC50 of 8.95 nM. It demonstrates enhanced potency in calcium mobilization assays and effectively inhibits the chemotaxis of neutrophils and macrophages activated by GPR84. This compound is valuable for research into conditions such as ulcerative colitis, providing insights into immune regulation and inflammation. -
GPR84 Agonist
DL-175 is a selective GPR84 agonist known for its biased agonistic activity. This compound selectively activates functional responses in immune cells, promoting enhanced chemotaxis and phagocytosis in human bone marrow cells. As a potential chemical probe, DL-175 is valuable for research focused on immune response modulation and associated pathways. -
GPR84 Antagonist
GPR84 Antagonist 1 is a potent and selective competitive antagonist of human GPR84. It demonstrates high affinity for the receptor, making it an essential tool for investigating the role of GPR84 in inflammatory processes and immune responses. This compound is valuable in research applications focused on understanding GPR84-mediated signaling pathways and potential therapeutic interventions in related diseases. -
GPR84 Antagonist
GPR84 antagonist 9 is a selective antagonist of the G protein-coupled receptor GPR84, demonstrating an IC50 value of 0.012 μM. This compound is primarily utilized in research focusing on inflammatory-driven pain diseases, facilitating the investigation of its role in pain modulation and potential therapeutic applications. Its oral bioactivity supports in vivo studies aimed at understanding GPR84's contribution to inflammatory processes. -
GPR84 Agonist
GPR84 agonist-1 is a selective agonist of the GPR84 receptor, exhibiting an EC50 value of 2.479 μM. This compound is crucial for studying the physiological and pathological roles of GPR84 in immune responses, particularly in the context of septicemia. Researchers may utilize GPR84 agonist-1 to explore its potential therapeutic applications in inflammatory diseases and immune modulation. -
GPR84 Agonist
PSB-16434 is a selective agonist of G protein-coupled receptor 84 (GPR84). This compound demonstrates potential in the study of inflammatory diseases, metabolic disorders, and immune regulation by activating GPR84 signaling pathways. Its role in modulating immune responses makes it a valuable tool for researchers investigating novel therapeutic approaches in these areas. -
GPR88 Inhibitor
GPR88-IN-1 is a selective inhibitor of GPR88, a G protein-coupled receptor involved in modulating dopaminergic signaling. This compound demonstrates potential for investigating the role of GPR88 in various central nervous system disorders, including schizophrenia and drug addiction. It serves as a valuable tool for researchers exploring therapeutic pathways related to neuropsychiatric conditions. -
GPR88 Agonist
GPR88 agonist 2 is a potent agonist for the GPR88 receptor, exhibiting an EC50 of 14 µM in cAMP functional assays. This compound is notable for its ability to penetrate the blood-brain barrier, making it a valuable tool for neurological research. Its specific action on GPR88 provides insights into its role in neuropharmacology and related biological pathways. This compound is suitable for studies investigating the modulation of GPR88 in various physiological and pathological contexts. -
GPR88 Agonist
RTI-122 is a potent agonist of the GPR88 receptor, demonstrating effective brain penetration and a half-life of 5.8 hours in murine models. This compound exhibits a cAMP EC50 value of 11 nM, making it a valuable tool for investigating mechanisms associated with excessive drinking behaviors. Its metabolic stability and selective activity position RTI-122 as a significant reagent for research in addiction neuroscience and related fields. -
GPR88 Agonist
GPR88 Agonist 3 is a selective agonist of the G protein-coupled receptor GPR88, exhibiting an EC50 value of 204 nM. This compound is valuable for research into psychiatric and neurodegenerative disorders, providing insights into the modulation of signaling pathways involved in these conditions. Its GPR88 activation can contribute to understanding GPR88's role in brain function and potential therapeutic interventions. -
GPR81 Agonist
3-Chloro-5-hydroxybenzoic acid is a selective agonist of the lactate receptor GPR81, with an EC50 of 16 μM for human GPR81. This compound demonstrates significant biological activity, promoting lipolysis in a murine obesity model. It serves as a valuable tool for research focused on metabolic regulation and obesity-related pathways. -
GPR81 Agonist
GPR81 agonist 1 is a selective agonist targeting the GPR81 receptor, demonstrating EC50 values of 58 nM for human GPR81 and 50 nM for mouse GPR81. This compound effectively inhibits lipolysis in differentiated 3T3-L1 adipocytes and demonstrates an ability to suppress lipolysis in vivo in mouse models without causing cutaneous flushing. GPR81 agonist 1 exhibits significant selectivity for GPR81 over GPR109a, making it a valuable tool for research into metabolic regulation and adipocyte biology. -
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.
