Catalog No.
Product Name
Application
Product Information
Citations
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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. -
GPBAR1 Agonist/RORγt Inhibitor
Allolithocholic acid functions as a dual agonist of GPBAR1 and an inverse agonist of RORγt, exhibiting an EC50 of 2.7 μM and an IC50 of 3.4 μM, respectively. This compound modulates immune and metabolic pathways by influencing immune cell polarization and preventing the differentiation of M1 macrophages and Th17 CD4 cells. Allolithocholic acid enhances insulin sensitivity and mitigates liver lipid accumulation, while also restoring bile acid homeostasis and modulating intestinal immunity. It is a valuable reagent for research in cancer, inflammation, immunology, and metabolic disorders. -
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. -
GnRH-R Antagonist
GnRH-R antagonist-3 is a potent gonadotropin-releasing hormone receptor (GnRH-R) antagonist with IC50 values of 94 nM for rat GnRH-R and 275 nM for human GnRH-R. This compound demonstrates significant potential in the study of hormone-dependent diseases, including endometriosis, breast cancer, and prostate cancer. It serves as a valuable tool for researchers investigating the therapeutic mechanisms and biological pathways associated with these conditions. -
LHRH Antagonist
Ramorelix is an LHRH antagonist that inhibits the action of luteinizing hormone, thereby interfering with hormone-driven tumor progression. This compound is primarily utilized in cancer research focused on hormone-sensitive tumors, offering insights into therapeutic strategies targeting the endocrine system. Ramorelix's biological activity makes it a valuable tool for exploring mechanisms of tumor inhibition and advancing anti-cancer therapies. -
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. -
GnRH Analogue
Lecirelin is a synthetic gonadotropin-releasing hormone (GnRH) analogue that functions as a GnRH agonist. It plays a crucial role in the regulation of reproductive hormones and is primarily utilized in the study of bovine ovarian follicular cysts. This compound is essential for investigating reproductive physiology and addressing disorders related to ovarian function in cattle. -
GnRHR Agonist
DCOIT is a potent agonist of the gonadotropin-releasing hormone receptor (GnRHR), promoting the synthesis of follicle-stimulating hormone and luteinizing hormone in the brain. This isothiazolinone compound engages G protein-coupled receptors, influencing MAPK and calcium signaling pathways. Its capacity to modulate hormone production makes DCOIT valuable for studies related to reproductive biology and endocrinology. -
GnRH Agonist
(Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH is a potent agonist of gonadotropin-releasing hormone (GnRH). This compound exhibits significant biological activity in the modulation of hormone secretion and can be utilized as an internal standard for LC-MS analysis of leuprorelin acetate. (Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH is relevant in biochemical research and has potential applications in the study of fertility and reproductive health. -
LHRH Antagonist
Antide (D-21074) is a potent LHRH antagonist that specifically inhibits luteinizing hormone-releasing hormone receptors. It displays significant biological activity in blocking the secretion of gonadotropins, making it instrumental in research related to hormone-dependent cancers, particularly prostatic cancer. This compound serves as a valuable tool for studying the effects of LHRH modulation in various therapeutic applications. -
GnRH-R Antagonist
BAY-784 is a gonadotropin-releasing hormone receptor (GnRH-R) antagonist that demonstrates inhibitory activity with IC50 values of 21 nM for human and 24 nM for rat GnRH-R. This compound is utilized in research to investigate the role of GnRH-R in reproductive biology and endocrine signaling. Its effectiveness makes it a valuable tool for studying hormonal regulation and potential therapeutic applications in reproductive disorders. -
GnRH Antagonist
Ganirelix is a competitive and selective gonadotropin-releasing hormone (GnRH) antagonist. It effectively inhibits the action of endogenous GnRH, thereby preventing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This compound is primarily utilized in reproductive research and in the management of controlled ovarian stimulation protocols in assisted reproductive technology. -
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. -
GnRH Antagonist
Linzagolix is a potent non-peptide gonadotropin-releasing hormone (GnRH) antagonist that is orally active. It has demonstrated significant biological activity in the modulation of hormone secretion and is utilized in research focused on uterine fibroids, endometriosis, and adenomyosis. This compound provides a valuable tool for investigating reproductive health and therapeutic interventions in related disorders. -
GnRH Receptor Antagonist
Lumigolix is a GnRH receptor antagonist that effectively inhibits gonadotropin-releasing hormone signaling. This compound demonstrates potential in the treatment and research of endometriosis by modulating hormone levels and preventing the effects of GnRH on pituitary hormone release. Its role in lowering estrogen production makes it a valuable reagent for studying reproductive health and related disorders. -
hGnRH-R Antagonist
BAY 1214784 is a potent and selective antagonist of the human gonadotropin-releasing hormone receptor (hGnRH-R), classified as a spiroindoline derivative. This compound effectively reduces plasma luteinizing hormone levels by up to 49%, demonstrating low pharmacokinetic variability and good tolerability in biological assays. BAY 1214784 holds promise for research applications related to uterine fibroids, providing a valuable tool for studies in reproductive health and hormone regulation. -
GnRH Agonist
LGnRH-III, derived from the sea lamprey, acts as a weak agonist of gonadotropin-releasing hormone (GnRH). This compound has been explored for its potential antitumor activities, making it a valuable tool in cancer research. Its mechanism involves the modulation of hormonal pathways, which may provide insights into therapeutic strategies targeting GnRH receptors in various malignancies. -
GnRH Antagonist
Abarelix Acetate is a potent gonadotropin-releasing hormone (GnRH) antagonist targeting GnRH receptors. It is primarily utilized in prostate cancer research, where it plays a crucial role in inhibiting the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This compound is instrumental in exploring therapeutic strategies for androgen-dependent tumors through its effects on hormone regulation. -
GnRH Analogue
sGnRH-A is a salmon gonadotropin-releasing hormone (GnRH) analogue that primarily targets the GnRH receptors. This compound effectively stimulates the secretion of growth hormone, making it valuable in studies related to hormonal regulation. Additionally, sGnRH-A serves as an inducer of ovulation and is commonly utilized in artificial insemination protocols for reproductive research and agricultural applications. -
GnRH Receptor Antagonist
AG-045572 is a potent antagonist of the gonadotropin-releasing hormone (GnRH) receptor, exhibiting Ki values of 6.0 nM for the human and 3.8 nM for the rat GnRH receptor. This compound is metabolized by CYP3A and effectively represses testosterone levels, making it valuable for research on reproductive hormone regulation and potential therapeutic applications in hormone-dependent conditions. Its specific activity highlights its relevance in pharmacological studies focusing on reproductive health and endocrine function. -
GnRH-R Antagonist
GnRH-R antagonist 1 is a potent GnRH receptor antagonist that exhibits high binding affinity with an IC50 of 0.57 nM and strong in vitro antagonistic activity at an IC50 of 2.18 nM. This compound is membrane-permeable and orally bioavailable, making it suitable for various research applications. It is particularly valuable in studies focused on advanced prostate cancer and in investigating the prevention of premature luteinizing hormone peaks. -
GnRH Antagonist
Merigolix is a potent gonadotropin-releasing hormone (GnRH) antagonist that effectively inhibits the release of gonadotropins such as luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This compound is primarily utilized in research related to reproductive biology and endocrinology, facilitating the study of hormonal regulation and the modulation of reproductive functions. Its application in animal models can aid in the exploration of fertility treatments and hormonal therapies. -
GnRH Antagonist
Linzagolix choline is a non-peptide gonadotropin-releasing hormone (GnRH) antagonist that acts by binding to GnRH receptors in the pituitary gland, thereby inhibiting the secretion of endogenous gonadotropins, including luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This mechanism leads to decreased levels of sex hormones such as estrogen and progesterone, making it valuable for investigating sex hormone-dependent conditions. Linzagolix choline is particularly relevant in the research of disorders such as endometriosis and uterine fibroids. -
LHRH Analogue
(D-Ser(tBu)6,D-Leu7,Azagly10)-LHRH is an analogue of luteinizing hormone-releasing hormone (LHRH) that primarily targets the LHRH receptor. This compound is designed to modulate reproductive hormone release by stimulating the secretion of pituitary luteinizing hormone (LH) and follicle-stimulating hormone (FSH). It serves as a valuable tool in reproductive biology and endocrinology research, particularly in studies related to fertility and hormonal regulation. -
GnRH Agonist
Avorelin is a gonadotropin-releasing hormone (GnRH) agonist that stimulates the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This compound is primarily utilized in research related to hormone regulation and reproductive biology. Avorelin is particularly relevant for studies investigating prostate cancer, as it can influence hormone-dependent tumor growth and serve as a potential therapeutic agent. -
LHRH Antagonist
Argtide is a luteinizing hormone-releasing hormone (LHRH) antagonist that effectively inhibits the release of gonadotropins. This compound is utilized in research related to endometriosis and hormone-sensitive cancers, providing valuable insights into therapeutic strategies and mechanisms of action. Its role in modulating LHRH signaling pathways makes it an important tool for studying reproductive and oncological health. -
GnRH analogue
Federelin is a gonadotropin-releasing hormone (GnRH) analog that acts by binding to GnRH receptors to stimulate the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This compound plays a significant role in reproductive biology and is used in research applications involving hormonal regulation, fertility studies, and endocrine system investigations. Its ability to modulate hormone levels makes it a valuable tool in studying reproductive health and related disorders. -
GnRH Receptor Antagonist
ORG 30276 is a potent GnRH receptor antagonist that effectively inhibits gonadotropin secretion by reducing serum LH and FSH levels. It decreases the expression of unoccupied pituitary GnRH receptors, resulting in significant downregulation of gonadotropin beta-subunit mRNA in the pituitary gland. The modulatory effects of ORG 30276 on gonadotropin dynamics can be selectively reversed by the administration of specific sex steroids, particularly androgens, which notably influence FSH beta-subunit mRNA levels. This compound is valuable for research in reproductive biology and endocrine regulation. -
GnRH Receptor Agonist
[Ala6]-LHRH is a synthetic analog of luteinizing hormone-releasing hormone (GnRH) that functions as a potent agonist for GnRH receptors. This compound effectively stimulates the secretion of luteinizing hormone from the pituitary gland, thereby enhancing reproductive hormone regulation. [Ala6]-LHRH is instrumental in fertility treatments and plays a significant role in managing conditions associated with hormone imbalances. -
GnRH Receptor Agonist
Histrelin is a GnRH receptor agonist that functions by stimulating the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to elevated testosterone levels. This compound serves as a valuable tool in research related to prostate cancer and endometriosis by modulating hormonal pathways. Histrelin's ability to influence reproductive hormone levels makes it instrumental in exploring treatments for hormone-dependent conditions. -
LHRH Analogue
(D-Ser4,D-Ser(tBu)6,Azagly10)-LHRH is an analogue of luteinizing hormone-releasing hormone (LHRH), targeting the LHRH receptor. This compound enhances the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), playing a crucial role in regulating reproductive functions. It is valuable for research applications focused on reproductive biology and hormone signaling pathways.
