Catalog No.
Product Name
Application
Product Information
Citations
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Endogenous Ligand for GPR54
Kisspeptin-54 (human) is an endogenous ligand for the GPR54 receptor, also known as KISS1. It exhibits high binding affinity, with Ki values of 1.81 nM for rat GPR54 and 1.45 nM for human GPR54. This peptide plays a crucial role in inhibiting tumor metastasis and promoting the secretion of gonadotropins, such as luteinizing hormone (LH), as well as testosterone. It is valuable in research applications related to reproductive biology and cancer metastasis. -
GPR10 Ligand
Prolactin Releasing Peptide (1-31), human is a potent ligand for the GPR10 receptor, facilitating the release of prolactin. This peptide exhibits high affinity binding, with Ki values of 1.03 nM for human GPR10 and 0.33 nM for rat GPR10. It is a valuable tool for investigating the hypothalamo-pituitary axis and studying prolactin-related physiological processes. -
GPR54/GnRH Receptor Activator
Kisspeptin 13 functions as an activator of the G protein-coupled receptor GPR54 and the gonadotropin-releasing hormone (GnRH) receptor. This peptide is known to inhibit glucose-induced insulin secretion with an IC50 of 1.2 nM and plays a role in activating the hypothalamic-pituitary-adrenal (HPA) axis, which can induce hyperthermia and influence motor behavior and anxiety in animal models. Additionally, Kisspeptin 13 has been implicated in enhancing memory, suggesting potential applications in Alzheimer's disease research. Its interactions with α2-adrenergic and 5-HT2 serotonin receptors further indicate its antidepressant-like properties. -
GPR109A Agonist
GSK256073 is a potent and selective agonist of the GPR109A receptor, also known as hydroxy-carboxylic acid receptor 2 (HCA2). With a pEC50 of 7.5 in human HCA2, this orally active compound acts as a full agonist without causing flushing. GSK256073 has demonstrated the ability to acutely enhance glucose homeostasis by inhibiting lipolysis, making it a valuable tool for research into type 2 diabetes mellitus (T2DM) and dyslipidemia. -
GPR109A Agonist
MK-1903 is a selective agonist of the hydroxycarboxylic acid receptor 2 (HCA2, GPR109A). This compound demonstrates strong activation of GPR109A, a receptor involved in regulating various metabolic processes. It is primarily used in research applications related to metabolic diseases and inflammation, providing insights into therapeutic pathways for conditions associated with dysregulated lipid metabolism. -
GPR109b Agonist
GPR109 receptor agonist-1 is a selective agonist for the human G-protein-coupled receptor GPR109b, exhibiting a pEC50 of 6.4. This compound plays a critical role in the modulation of metabolic processes and holds potential for research applications related to cardio-metabolic diseases. Its specificity and activity make it a valuable tool for elucidating the biological functions of GPR109b in various metabolic pathways. -
GPR109b Agonist
GPCR Agonist-2 is a selective agonist of the GPR109b receptor (HM74), exhibiting a pEC50 value of 6.51. This compound demonstrates potential for modulating lipid metabolism and is valuable in research focused on lipid disorders and related metabolic conditions. Its specificity for GPR109b makes it an important tool for investigating the receptor's role in various biological pathways. -
GPR109A Agonist
GPR109 receptor agonist-2 is a selective agonist of the GPR109A receptor, demonstrating a pEC50 of 5.53. This compound modulates the activity of GPR109A, which plays a crucial role in metabolic regulation and inflammation. It is suitable for use in research related to metabolic disorders and the therapeutic potential of GPR109A in various biological systems. -
GPR109A/GPR109B Agonist
Acifran is a potent agonist of GPR109A and GPR109B, which are receptors associated with the pharmacological effects of niacin. This compound has demonstrated efficacy as an antihyperlipidemic agent, making it valuable for studies focused on lipid metabolism and cardiovascular disease. Acifran is utilized in research applications related to the modulation of inflammatory responses and the regulation of energy homeostasis. -
GPR109 Receptor Agonist
GPR109 receptor agonist-3 is an orally active compound that selectively targets and activates the GPR109 receptor, exhibiting an IC50 of 310 nM. This agonist demonstrates significant antioxidative and cytoprotective properties similar to Lipoic acid. In preclinical studies, GPR109 receptor agonist-3 effectively reduces total cholesterol, triglycerides, and low-density lipoprotein cholesterol, while increasing high-density lipoprotein cholesterol in high-fat diet-fed rats. It serves as a valuable tool for investigating the mechanisms underlying atherosclerosis and lipid metabolism. -
GPR109A Agonist
GSK256073 tris is a selective and orally bioavailable agonist of GPR109A (HCA2), exhibiting a high potency with a pEC50 of 7.5 in human models. This compound acutely enhances glucose homeostasis through the inhibition of lipolysis, making it a valuable tool for research related to type 2 diabetes mellitus (T2DM) and dyslipidemia. Its long-lasting effect and non-flushing profile provide significant utility in metabolic disorder investigations. -
GPR119 Activator
YH18968 is an orally active GPR119 agonist, exhibiting an EC50 of 2.8 nM for cAMP accumulation. This compound enhances intracellular cyclic adenosine monophosphate levels, promotes glucagon-like peptide-1 secretion from intestinal L cells, and stimulates glucose-dependent insulin secretion from pancreatic β cells. YH18968 has been shown to improve glucose tolerance in both normal and diet-induced obese mouse models, making it a valuable reagent for research aimed at understanding and managing type 2 diabetes. -
GPR119 Agonist
MKP10241 is an orally active agonist of GPR119, a G protein-coupled receptor involved in the regulation of glucose metabolism. This compound significantly elevates cAMP levels in GPR119-expressing cell lines, demonstrating an EC50 of 3.7 nM. MKP10241 effectively lowers blood glucose levels and HbA1c in both acute and chronic diabetic mouse models, and exhibits promising preclinical efficacy in addressing obesity and metabolic associated steatotic hepatitis (MASH) in rodent studies. -
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. -
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. -
GPR119 Agonist
DA-1241 is a selective agonist of the GPR119 receptor. It effectively inhibits macrophage differentiation by downregulating NFκB signaling pathways through GPR119 activation. Additionally, DA-1241 demonstrates potential in conjunction with DPP4 inhibitors to alleviate liver inflammation and normalize inflammation-related gene expression in the liver. This compound is primarily utilized in research focused on metabolic dysfunction-associated steatohepatitis (MASH). -
GPR119 Agonist
PSN 375963 is a potent agonist of the GPR119 receptor, demonstrating EC50 values of 8.4 μM for human and 7.9 μM for mouse GPR119. This compound exhibits comparable potency to the endogenous agonist oleoylethanolamide (OEA). PSN 375963 may serve as a valuable tool for research into metabolic disorders and obesity by elucidating the role of GPR119 in glucose homeostasis and insulin secretion. -
GPR119 Agonist
GPR119 agonist 3 is a potent agonist of GPR119, exhibiting an EC50 value of 3.8 nM for human GPR119. This compound demonstrates significant hypoglycemic effects, making it a valuable tool for the investigation of type 2 diabetes and obesity in research settings. Its oral bioactivity facilitates ease of use in various experimental designs aimed at elucidating the role of GPR119 in metabolic regulation. -
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. -
GPR119 Agonist
BMS-986034 is a selective agonist of the GPR119 receptor, which plays a significant role in glucose homeostasis and insulin secretion. This compound demonstrates notable efficacy in enhancing glucose-dependent insulin release and may contribute to the regulation of appetite and energy balance. BMS-986034 is primarily utilized in research related to metabolic disorders, including type 2 diabetes and obesity, making it a valuable tool for investigating therapeutic strategies targeting the GPR119 pathway. -
GPR119 Agonist
AS1907417 is a selective agonist of GPR119, demonstrating oral bioactivity. This compound exhibits antihyperglycemic properties, making it a valuable tool in the study of type 2 diabetes and related metabolic disorders. Its unique chemical structure enhances its potential for research applications targeting glucose homeostasis and insulin sensitivity. -
GPR119 Agonist
GSK1104252A is a potent and selective agonist of the GPR119 receptor. This compound demonstrates significant insulinotropic activity, making it relevant for research applications focused on type 2 diabetes and metabolic disorders. Its ability to enhance glucose-dependent insulin secretion positions GSK1104252A as a valuable tool for exploring therapeutic strategies in glycemic control. -
GPR-119 Agonist
MK-8282 is a potent, orally active agonist of the GPR-119 receptor. This compound has demonstrated the ability to improve glucose tolerance, making it a valuable tool for investigating metabolic disorders. MK-8282 is primarily utilized in research focused on type 2 diabetes and its associated pathways. -
GPR119 Agonist
PSN 375963 hydrochloride is a potent agonist of GPR119, exhibiting EC50 values of 8.4 μM and 7.9 μM for human and mouse GPR119, respectively. This compound demonstrates comparable efficacy to the endogenous agonist oleoylethanolamide (OEA). PSN 375963 hydrochloride is valuable for research applications targeting metabolic disorders and the modulation of glucose homeostasis. -
GPR119 Agonist
BMS-903452 is a selective agonist of GPR119, a G protein-coupled receptor implicated in glucose metabolism and insulin secretion. This compound enhances the release of incretin hormones, which play a crucial role in regulating blood sugar levels. BMS-903452 is primarily utilized in diabetes research to explore potential therapeutic avenues for the management of type 2 diabetes and related metabolic disorders. -
GPR119 Agonist
GSK2041706A is a potent agonist of the G protein-coupled receptor 119 (GPR119). This compound has demonstrated significant biological activity in modulating glucose metabolism and insulin secretion, making it a valuable tool in the research of type 2 diabetes. Its ability to activate GPR119 positions it as a promising candidate for studies focusing on metabolic disorders and potential therapeutic interventions. -
GPR119 Agonist
GSK-1292263 hydrochloride is a potent orally active agonist of GPR119, demonstrating a pEC50 of approximately 6.9 nM for human GPR119 and 6.7 nM for rat GPR119. This compound is primarily utilized in research focused on type 2 diabetes and dyslipidemia, contributing to a better understanding of metabolic regulation and potential therapeutic interventions. Its ability to activate GPR119 makes it a valuable tool for exploring signaling pathways and metabolic processes influenced by this receptor. -
GPR119 Agonists
GPR119 Agonist 2 is an orally active compound targeting the GPR119 receptor, known for its role in glucose metabolism. This reagent demonstrates favorable pharmacokinetic properties in rodent models and effectively enhances glucose tolerance in both mice and rats. GPR119 Agonist 2 is valuable for research focused on type 2 diabetes and metabolic disorders. -
GPR119 Agonist
AS-1669058 free base is a potent agonist of the GPR119 receptor, making it a candidate for diabetes treatment. It stimulates insulin secretion in response to elevated glucose levels both in vitro and in vivo, enhancing insulin promoter activity. In preclinical studies, AS-1669058 demonstrated the ability to improve glucose tolerance and lower blood glucose levels in db/db mice, supporting its potential in metabolic research. -
GPR119 Agonist
AS-1669058 is a selective agonist of the GPR119 receptor, showing promise in the management of type 2 diabetes. This compound enhances insulin secretion in response to elevated blood glucose levels both in vitro and in vivo, while also stimulating insulin promoter activity. In studies using db/db mice, AS-1669058 demonstrated significant improvements in glucose tolerance and reductions in blood glucose levels, indicating its potential utility in diabetes research. -
GPR139 Agonist
Zelatriazin is a selective agonist of the GPR139 receptor, exhibiting a potency with an EC50 of 22 nM. This compound is of particular interest in the study of negative symptoms associated with schizophrenia. Its ability to selectively activate GPR139 makes it a valuable tool for exploring the underlying mechanisms of this psychiatric disorder. -
GPR139 Antagonist
LP-471756 is a potent antagonist of the GPR139 receptor, exhibiting an IC50 value of 640 nM. This compound effectively inhibits cAMP production stimulated by LP-360924, making it a valuable tool for researchers investigating GPR139 signaling pathways and related biological processes. Its application extends to studies in neurobiology and metabolic regulation, where GPR139 plays a crucial role. -
GPR139 Agonist
GPR139 agonist-2 is a selective agonist targeting the GPR139 receptor, demonstrating a potent EC50 of 24.7 nM. This compound has shown promising biological activity by rescuing social interaction deficits and ameliorating cognitive impairments in murine models of schizophrenia. GPR139 agonist-2 holds potential for use in antipsychotic drug research and the exploration of novel therapeutic strategies for schizophrenia. -
GPR171 Agonist
MS15203 is a potent and selective agonist of GPR171, a G protein-coupled receptor involved in neuropeptide signaling. This compound is known to enhance food intake and body weight, likely through the stimulation of neuronal activity. Additionally, MS15203 significantly increases the mRNA levels of proSAAS, neuropeptide Y (NPY), and agouti-related peptide (AgRP), making it a valuable tool for research in appetite regulation and metabolic disorders. -
GPR171 Agonist
BigLEN (mouse) is a highly potent and selective agonist of the orphan G protein-coupled receptor 171 (GPR171), demonstrating a Kd of approximately 0.5 nM. This compound is instrumental in modulating biological processes related to food intake and metabolism, making it valuable for research in appetite regulation and metabolic studies. -
GPR35 Antagonist
CID 2745687 is a selective, reversible antagonist of GPR35, exhibiting a binding affinity with a Ki value of 12.8 nM. This compound is valuable for studies investigating the role of GPR35 in various physiological processes and disease states, making it a useful tool in pharmacology and drug discovery research. Its specificity allows for the exploration of GPR35-related signaling pathways and potential therapeutic interventions. -
GPR35 Antagonist
CID1231538 is a potent antagonist of the GPR35 receptor, a member of the G protein-coupled receptors (GPCRs) family. This benzothiazole analog demonstrates selective inhibition, exhibiting no significant activity against rodent orthologs of GPR35. Its unique properties make it a valuable tool for exploring GPR35-related biological pathways and for investigating potential therapeutic applications in diseases where this receptor is implicated. -
GPR35 Agonist
GPR35 Agonist 4 is a selective activator of the GPR35 receptor, exhibiting a potency with an pEC50 value of 5.86. This compound demonstrates significant biological activity in both human and rat models, making it a valuable tool for studying GPR35 signaling pathways. Notably, mutation of the arginine at position 3.36 negates the agonistic effect of GPR35 Agonist 4, underscoring its mechanism of action. This reagent can be utilized in pharmacological research investigating the role of GPR35 in various physiological and pathological processes. -
GPR35 Agonist
YE120 is a potent agonist of the GPR35 receptor, exhibiting an EC50 of 32.5 nM. This compound activates GPR35, which is involved in various physiological processes, including inflammation and metabolic regulation. YE120 is utilized in research applications focused on understanding GPR35 signaling pathways and its potential roles in disease modulation. -
GPR35 Agonist
GPR35 agonist 5 (3,5-dinitro-bisphenol A; compound 6) functions as a weak agonist of the GPR35 receptor. This compound has been shown to induce cell cycle arrest in CHO-S cells at the G1/G0 phase, highlighting its potential role in cell proliferation studies. GPR35 agonist 5 may be useful for research applications focused on understanding GPR35 signaling pathways and their implications in various biological processes. -
Gpr35 Modulator
Gpr35 Modulator 1 is a potent GPR35 modulator, exhibiting an IC50 of ≤ 100 nM in HEK293 cells stably expressing human GPR35. This compound is valuable for investigating the physiological and pathological roles of GPR35 in various biological processes. Research applications include studies on inflammation, metabolic disorders, and gastrointestinal functions, facilitating the exploration of GPR35 as a therapeutic target. -
GPR35 Modulator
Gpr35 modulator 2 is a selective modulator of the GPR35 receptor, which plays a critical role in various physiological processes. This compound is valuable for investigating GPR35-related disorders and elucidating the receptor's role in cellular signaling pathways. It presents a useful tool for researchers studying the pathophysiology associated with GPR35 and exploring potential therapeutic avenues. -
GPR35 Activator
GPR35 activator-1 is a highly potent activator of the GPR35 receptor, exhibiting an inhibition constant (Ki) of 0.08 nM for human GPR35. This compound is valuable for research involving GPR35 signaling pathways, making it applicable in studies of immune response, gastrointestinal function, and neurobiology. Its high potency makes it a useful tool for elucidating the biological roles and therapeutic potential of GPR35 in various physiological and pathological contexts. -
GPR35 Agonist
GPR35 Agonist 3 is a synthetic compound that selectively activates the GPR35 receptor, exhibiting an EC50 value of 1.4 μM. This reagent is valuable for investigating a range of biological mechanisms and disease states, including gastric cancer, type 2 diabetes, cardiovascular disorders, and immune system functions. Researchers can utilize GPR35 Agonist 3 to explore its therapeutic potential and the role of GPR35 in various physiological processes. -
GPR Agonist
ML301 is a small molecule G-protein coupled receptor (GPCR) agonist that activates GPR signaling pathways. This compound exhibits potent biological activity, effectively competing for 125I-NT binding and demonstrating inhibition by SR142948A with an IC50 of approximately 63 nM. ML301 is useful for research applications exploring GPCR mechanisms, signal transduction, and receptor pharmacology. -
GPR35
Diethyl-Lodoxamide is a potent agonist of the GPR35 receptor, demonstrating significant potential for the treatment of inflammatory bowel disease. It activates GPR35 in human, mouse, and rat models, exhibiting similar EC50 values across these species. Notably, Diethyl-Lodoxamide has been shown to alleviate clinical symptoms in DSS-induced mouse models of inflammatory bowel disease, offering a more effective solution compared to traditional therapies such as 5-ASA. The compound's pharmaceutical properties have been carefully optimized to align with advanced drug design requirements. -
GPR39 Agonist
Lithocholic acid 3-sulfate (disodium) is a GPR39 agonist demonstrating robust activation with EC50 values of 0.88 μM in the presence of Zn2+ and 41 μM in its absence, in relevant cell lines. This compound initiates intracellular calcium signaling through GPR39, not relying on Zn2+-binding sites. Additionally, it functions as a ligand for RORγt, selectively inhibiting Th17 cell differentiation. Lithocholic acid 3-sulfate (disodium) is valuable for investigations into cholestatic liver diseases and related immunological studies. -
GPR39 Agonist
Taurolithocholic acid 3-sulfate disodium is an agonist of the GPR39 receptor, demonstrating EC50 values of 71.6 μM and 69.4 μM in the absence of Zn2+ and 9 μM and 9.6 μM in the presence of Zn2+, as observed in M39-20 and hGPR39-2 cell lines, respectively. This compound activates GPR39 to promote intracellular calcium signaling while functioning independently of Zn2+ binding sites H17 and H19. Taurolithocholic acid 3-sulfate disodium is suitable for investigations related to gallbladder disease and its underlying mechanisms. -
GPR52 Agonist
PW0787 is a potent and selective agonist of the GPR52 receptor, exhibiting an EC50 of 135 nM. This compound demonstrates significant brain penetration and has been shown to effectively suppress psychostimulant behavior. It is valuable for research applications in neuropharmacology and the study of GPR52's role in modulating psychiatric disorders. -
GPR52 Antagonist
GPR52 antagonist-1 is a selective antagonist of the GPR52 receptor, exhibiting an IC50 of 0.63 μM. This compound effectively reduces levels of the mutant huntingtin protein (mHTT) and supports the survival of mouse primary striatal neurons. GPR52 antagonist-1 is important for research applications investigating neurodegenerative disorders, particularly Huntington's disease, and offers insights into the role of GPR52 in neuronal health.
