Catalog No.
Product Name
Application
Product Information
Citations
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Free Fatty Acid Receptor Agonist
AS2034178 free base is a specific agonist of the Free Fatty Acid Receptor 1 (GPR40). This compound has been demonstrated to enhance glucose-dependent insulin secretion, making it a valuable tool for investigating mechanisms underlying type 2 diabetes mellitus. Its oral bioactivity suggests potential applicability in therapeutic research aimed at metabolic disorders. -
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. -
FFA1 Agonist
FFA1 agonist-1 is a potent agonist of fatty acid receptor 1 (FFA1), exhibiting an EC50 of 0.75 μM. This compound is designed for research applications related to type 2 diabetes mellitus, where modulation of FFA1 can influence metabolic pathways and insulin sensitivity. FFA1 agonist-1 provides a valuable tool for investigating the therapeutic potential of targeting this receptor in metabolic disorders. -
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. -
FFA4 Agonist
Metabolex-36 is a potent agonist of the free fatty acid receptor 4 (FFA4), demonstrating a pEC50 value of 5.9. In contrast, it exhibits a significantly lower activity for FFA1, with a pEC50 value of less than 4.0. This compound is crucial for studies focused on metabolic regulation and the modulation of inflammatory pathways, making it a valuable tool in research related to obesity, diabetes, and cardiovascular diseases. -
Free Fatty Acid Receptor Agonist
LY2922083 is a potent agonist of the free fatty acid receptor GPR40. This compound activates GPR40 in response to increased blood glucose levels, demonstrating potential as a glucose-lowering agent. Its biological activity makes it a valuable tool for research in metabolic diseases and insulin signaling pathways. -
Free Fatty Acid Receptor Agonist
GPR40 Agonist 2 is an agonist of the free fatty acid receptor GPR40, playing a crucial role in glucose metabolism and insulin secretion. This compound is primarily utilized in diabetes research, providing insights into the regulatory mechanisms of energy homeostasis and metabolic disorders. Its activation of GPR40 has potential therapeutic implications for the management of type 2 diabetes and related metabolic diseases. -
Anti-diabete Agent
Hyocholic acid is a bile acid primarily found in porcine sources, demonstrating significant anti-diabetic properties. Its mechanism involves promoting GLP-1 secretion through activation of TGR5 and inhibition of FXR in enteroendocrine cells. This compound has potential applications in research aimed at understanding and treating type 2 diabetes and related metabolic disorders. -
GPCR19 Agonist /FXR Antagonist
Ursodeoxycholic acid sodium is a potent agonist of the G-protein coupled receptor 19 (GPCR19) and antagonist of the farnesoid X receptor (FXR). This secondary bile acid plays a crucial role in maintaining intestinal barrier integrity and regulating lipid metabolism. Its ability to modulate bile acid-activated receptors makes it valuable for investigating various hepatic and gastrointestinal diseases. Ursodeoxycholic acid sodium is also orally active, making it suitable for diverse in vitro and in vivo research applications. -
TGR5 Agonist
Cholic acid 7-sulfate is a selective agonist for the TGR5 receptor with an EC50 of 0.17 μM. This compound enhances GLP-1 secretion in enteroendocrine L cells, leading to improved glucose tolerance through TGR5 activation. Additionally, as an endogenous ligand for MHC class I-related protein (MR1), it supports the survival of mucosal-associated invariant T (MAIT) cells and influences their development and function by modulating homeostatic gene expression. Cholic acid 7-sulfate is valuable in studies related to diabetes and MAIT cell-mediated immune regulation. -
TGR5 Agonist
TC-G 1005 is a selective agonist of the Takeda G protein-coupled receptor 5 (TGR5), demonstrating potent activity with EC50 values of 0.72 nM for human TGR5 and 6.2 nM for mouse TGR5. This compound has been shown to effectively reduce glucose levels in vivo, making it a valuable tool for researching metabolic disorders and the role of TGR5 in glucose homeostasis. Its oral bioactivity supports its application in various pharmacological studies related to energy metabolism and diabetic therapies. -
TGR5 Agonist
TGR5 Receptor Agonist 4 is a potent agonist of the bile acid receptor TGR5, exhibiting an EC50 of 2 nM for human TGR5 and 3 nM for mouse TGR5. This compound is instrumental in studies focusing on glucose metabolism and weight management. Its activation of TGR5 contributes to hypoglycemic effects and enhances energy expenditure, making it valuable for research in metabolic disorders. -
R enantiomer of TGR5 Receptor Agonist 4
(4′R)-TGR5 Receptor Agonist 4 is an R enantiomer that selectively targets the TGR5 receptor, a bile acid receptor essential in metabolic regulation. It exhibits high potency with EC50 values of 2 nM for human TGR5 and 3 nM for mouse TGR5. This compound is important for studies related to hypoglycemia and weight management, facilitating research into therapeutic strategies for metabolic disorders. -
TGR5 Agonist
TGR5 Receptor Agonist 3 (Compound 19) is a selective agonist for the G-protein-coupled bile acid receptor 1 (TGR5), demonstrating enhanced safety by minimizing gallbladder-filling effects. It exhibits effective activation of human TGR5 with an EC50 of 16.4 nM and mouse TGR5 with an EC50 of 209 nM. This compound is valuable in research applications focusing on metabolic regulation, energy expenditure, and bile acid signaling pathways. -
TGR5 Activator
WB403 is a potent TGR5 activator with an EC50 of 5.5 μM for human TGR5. It enhances downstream signaling pathways associated with glucose metabolism, notably promoting GLP-1 secretion, improving glucose tolerance, and lowering fasting and postprandial blood glucose levels as well as HbA1c in murine models of type 2 diabetes. Additionally, WB403 contributes to increased pancreatic β-cell mass and the restoration of the islet cell distribution. This compound is valuable for studying mechanisms and therapeutic strategies in type 2 diabetes research. -
GPBAR1 Agonist
FXR/TGR5 agonist 1 is a potent agonist of the G protein-coupled receptor TGR5 (GPBAR1) and also activates farnesoid X receptor (FXR). This compound demonstrates key biological activity in regulating metabolic pathways associated with lipid metabolism and inflammation. It is primarily utilized in research applications focusing on fatty liver disease and related metabolic disorders. -
TGR5 Agonist
INT-777 (R-enantiomer) is a selective agonist of the TGR5 receptor, exhibiting an EC50 value of 4.79 μM. This compound plays a significant role in studying metabolic disorders and gastrointestinal physiology due to its activation of TGR5. Research applications include investigations into energy homeostasis, insulin sensitivity, and the modulation of bile acid signaling pathways. -
GPBAR1 Agonist/CysLT1R Antagonist
GPBAR1-IN-3 is a selective agonist for the G protein-coupled receptor GPBAR1, exhibiting an EC50 of 0.17 μM. Additionally, it functions as an antagonist of the CysLT1 receptor. This compound is valuable for research into inflammatory processes and potential therapeutic strategies involving GPBAR1 activation and CysLT1R inhibition in various biological contexts. -
GPBAR1 Agonist
GPBAR-A is a selective agonist of the G protein-coupled bile acid receptor GPBAR1. This compound demonstrates significant biological activity in modulating metabolic pathways, making it valuable for research related to diabetes mellitus. GPBAR-A enables the investigation of bile acid signaling and its potential therapeutic effects on metabolic disorders. -
G protein-coupled Bile Acid Receptor 1 Antagonist
5-HT7R antagonist 1 (free base) is a selective antagonist of the serotonin 5-HT7 receptor, exhibiting a Ki value of 6.5 nM. This compound functions as a G protein-biased antagonist, modulating signaling pathways mediated by this receptor. It is primarily utilized in research applications focused on neuropharmacology and exploring the role of 5-HT7R in various physiological and pathological processes. -
TGR5 Agonist
RG-239 is a selective TGR5 agonist with an EC50 of 120 nM, exhibiting superior potency compared to Betulinic acid (EC50 = 1.04 μM). It enhances mitochondrial activity in adipocytes and promotes neurite outgrowth at elevated concentrations. Additionally, RG-239 effectively inhibits LPS-induced iNOS expression and nitrite production in Raw264.7 macrophages and microglial cells. This compound is valuable for studies related to type 2 diabetes and neurodegenerative disorders. -
GPBAR1 Agonist
Hyodeoxycholic acid sodium is a potent agonist of the G protein-coupled bile acid receptor 1 (GPBAR1, also known as TGR5). It is a secondary bile acid produced in the small intestine by gut microbiota, demonstrating biological activity with an EC50 of 31.6 µM in Chinese Hamster Ovary (CHO) cells. This compound is valuable for research applications focused on metabolic regulation and signaling pathways associated with bile acids. -
TGR5 Agonist
LT-188A is a potent agonist of TGR5, exhibiting an EC50 value of 23 μM. This compound has been shown to reduce the levels of inflammatory mediators in macrophages, suggesting its potential utility in inflammation-related research. Its role in modulating immune responses makes LT-188A valuable for investigating TGR5-related pathways and therapeutic applications in inflammatory diseases. -
TGR5 Agonist
RO5527239 is an orally active agonist of the TGR5 receptor, which stimulates enteroendocrine L cells to increase the secretion of the endogenous hormone GLP-2. This compound demonstrates potential in modulating gastrointestinal functions and may aid in research surrounding metabolic disorders. Its activation of TGR5 highlights its significance in studies focused on energy homeostasis and gut hormone dynamics. -
TGR5 Activator
5β-Cholestane-3α,7α,12α,25-tetrol is a potent TGR5 activator, exhibiting an EC50 of 1.36 μM. This bile acid alcohol plays a significant role in regulating metabolic processes and has shown promising biological activity relevant to energy expenditure and glucose metabolism. Additionally, it serves as a crucial disease marker in Cerebrotendinous xanthomatosis (CTX), making it valuable for research into bile acid signaling and related metabolic disorders. -
G protein-coupled Bile Acid Receptor 1 Antagonist
5-HT7R Antagonist 1 is a G protein-coupled receptor antagonist that selectively inhibits the 5-HT7 receptor, with a Ki value of 6.5 nM. This compound is primarily utilized in research exploring serotonergic signaling pathways and their implications in neuropsychiatric disorders. Its inhibition of 5-HT7R can aid in understanding the receptor's role in various physiological and pathological processes. -
Bile Acid Receptor Activator
Deoxycholic acid sodium hydrate is a bile acid that functions as an activator of the G protein-coupled bile acid receptor TGR5. It plays a significant role in lipid metabolism and has been implicated in various physiological processes, including glucose homeostasis and energy expenditure. This compound is commonly used in research applications focused on metabolic disorders, liver function, and signaling pathways influenced by bile acids. -
TGR5 Agonist
TGR5 Agonist 3 is a cholic acid derivative that selectively activates the TGR5 receptor, exhibiting an EC50 of 5 μM. This compound is utilized in research to explore the role of TGR5 in various metabolic processes, including glucose and lipid metabolism. Its specific action makes it a valuable tool for studying the therapeutic potential of TGR5 modulation in diseases such as obesity and diabetes. -
TGR5 Receptor Activator
6ECA is a selective activator of the TGR5 receptor, exhibiting an EC50 of 3.44 μM. This compound demonstrates no significant activity at the FXR, making it a useful tool for investigating the role of TGR5 in metabolic conditions. 6ECA is particularly applicable for research focused on diabesity and related disorders. -
Cholane Scaffolds
(3α,5β,6β,7α)-BAR501 is a cholane scaffold compound designed to target farnesoid X receptor (FXR) and Takeda G protein-coupled receptor 5 (TGR5/GPBAR1) pathways. This compound demonstrates significant potential in research related to FXR and TGR5-mediated physiological processes and disease states. Its applicability spans investigations into metabolic disorders and associated therapeutic targets. -
Stable Isotope
Cholic acid 7-sulfate-d4 is a deuterium-labeled derivative of cholic acid 7-sulfate, a selective agonist for the TGR5 receptor with an EC50 of 0.17 μM. This compound plays a crucial role in stimulating GLP-1 secretion and enhancing glucose tolerance through its action on enteroendocrine L cells. Additionally, cholic acid 7-sulfate-d4 serves as an endogenous ligand for MHC class I-related protein (MR1), influencing the development and function of mucosal-associated invariant T cells (MAIT). It is primarily utilized in research focused on diabetes and immune regulation related to MAIT cells. -
TGR5 Agonist
TGR5 agonist 10 is a selective, allosteric agonist of the Takeda G protein-coupled receptor 5 (TGR5), exhibiting EC50 values of 0.8 μM for human TGR5 and 0.6 μM for mouse TGR5. This compound uniquely activates both human and mouse TGR5, leading to increased cAMP accumulation, while exhibiting higher selectivity for cAMP formation over β-arrestin2 recruitment. TGR5 agonist 10 modulates the functional activity of lithocholic acid and has demonstrated glucose-lowering effects in oral glucose tolerance tests in Mus musculus. It is an important tool for research into diabetes and metabolic disorders. -
G protein-coupled Bile Acid Receptor 1 Agonist
TGR5 agonist 6 is a selective G protein-coupled bile acid receptor 1 agonist. This compound demonstrates notable and prolonged blood glucose-lowering effects, while maintaining an acceptable safety profile. Its design as a non-systemic, gut-targeted agent makes it valuable for research applications focused on metabolic disorders and glucose homeostasis. -
TGR5 Allosteric Agonist
TGR5 agonist 9 is a selective allosteric agonist targeting the TGR5 receptor, exhibiting EC₅₀ values of 0.48 μM for human and murine TGR5. This compound effectively recruits β-arrestin 1 and β-arrestin 2, with EC₅₀ values of 78.8 μM and 12.3 μM, respectively, and demonstrates notable efficacy in cAMP accumulation. In the ICR mouse model, TGR5 agonist 9 shows significant hypoglycemic effects, making it a valuable tool for research related to diabetes. -
GRK2 Degrader
GRK2 degrader-1 is a potent and orally active degrader of G protein-coupled receptor kinase 2 (GRK2) that mediates its degradation through the ubiquitin-proteasome pathway. This compound effectively inhibits right ventricular remodeling and reduces pulmonary artery pressure in mouse models of pulmonary artery hypertension (PAH). GRK2 degrader-1 serves as a valuable tool for investigating the role of GRK2 in PAH and related cardiovascular research. -
G protein-coupled receptor kinase Inhibitor
CCG 224061 is a selective inhibitor of G protein-coupled receptor kinase 2 (GRK2) with an IC50 of 0.066 μM. It effectively inhibits GRK activity in cardiomyocytes, making it a valuable tool for studying cardiac signaling pathways. This compound is particularly relevant for research focused on heart disease, heart failure, myocardial hypertrophy, and hypertension. -
GRK5 Inhibitor
CCG273441 is a selective covalent inhibitor of G protein-coupled receptor kinase 5 (GRK5), exhibiting an IC50 value of 3.8 nM. This compound demonstrates a high degree of selectivity over GRK2, with an IC50 of 4.8 μM, by targeting and covalently binding to the Cys474 residue, which is unique to the GRK5 subfamily. CCG273441 serves as a valuable tool for research into GRK5-related signaling pathways and potential therapeutic applications in various disease models. -
GRK2 Inhibitor
CCG258747 is a potent and selective inhibitor of GRK2, demonstrating an IC50 value of 18 nM and high selectivity against GRK1, GRK5, PKA, and ROCK1. This compound effectively prevents the internalization of the µ-opioid receptor (MOR) and inhibits the IgE-mediated anaphylaxis via the GRK2 and FcεRI signaling pathway, while also activating mast cells through MRGPRX2 and MRGPRB2. CCG258747 serves as a valuable tool for investigating disease mechanisms associated with GRK2 overexpression, including heart failure and opioid tolerance. -
Pathogenic G-protein-coupled receptor autoantibodies Neutralizer
Rovunaptabin (ARC 183) is an aptamer consisting of a single-stranded DNA molecule made up of 15 deoxynucleotides, specifically designed to neutralize pathogenic G-protein-coupled receptor autoantibodies. It exhibits broad-spectrum activity, making it a valuable tool for studying diseases such as cardiomyopathy and pulmonary hypertension. Researchers can utilize Rovunaptabin to investigate the underlying mechanisms and potential therapeutic approaches related to these conditions. -
GRK Inhibitor
GRK-IN-1 is a selective inhibitor of G protein-coupled receptor kinases (GRKs), which play a crucial role in the regulation of receptor desensitization and downregulation. This compound exhibits potential biological activity in modulating signaling pathways mediated by GPCRs, making it valuable for research focused on cardiovascular diseases, neurological disorders, and cancer. GRK-IN-1 can be utilized to investigate the impact of GRK inhibition on cellular signaling and to explore therapeutic strategies targeting GRK-related pathways. -
GRK6 Inhibitor
GRK6-IN-3 is a selective inhibitor of G protein-coupled receptor kinase 6 (GRK6), exhibiting an IC50 value of 1.03 μM. This compound modulates GRK6 activity, which is crucial for various cellular signaling pathways. GRK6-IN-3 is suitable for research applications aimed at exploring GRK6's role in receptor desensitization and its implications in various physiological and pathological processes. -
GRK5 Inhibitor
CCG-271423 is a selective inhibitor of G protein-coupled receptor kinase 5 (GRK5), demonstrating an IC50 of 2.1 nM for GRK5 and 44 μM for GRK2. This compound effectively reduces cardiomyocyte contractility and lowers calcium transient levels, making it valuable for cardiac research. Additionally, CCG-271423 features an alkyne group, enabling its use in copper-catalyzed azide-alkyne cycloaddition (CuAAc) for bioconjugation applications. -
GRK5 Inhibitor
GRK5-IN-4 is a selective covalent inhibitor of G protein-coupled receptor kinase 5 (GRK5), exhibiting an IC50 of 1.1 μM and demonstrating 90-fold selectivity over GRK2. This compound serves as a valuable tool for heart failure research by modulating GRK5 activity. Additionally, GRK5-IN-4 features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it useful for various chemical biology applications. -
GRK6 Inhibitor
GRK6-IN-4 is a selective inhibitor of G protein-coupled receptor kinase 6 (GRK6), exhibiting an IC50 of 1.56 μM. This compound plays a crucial role in the modulation of G protein-coupled receptor signaling pathways and is relevant for research investigating hematological malignancies, inflammatory diseases, and autoimmune disorders. By inhibiting GRK6, GRK6-IN-4 provides valuable insights into the underlying mechanisms of these conditions and potential therapeutic strategies. -
GRK Inhibitor
CCG 258001 is a selective inhibitor of G protein-coupled receptor kinases (GRK), demonstrating IC50 values of 0.29 µM for GRK2, 51.8 µM for GRK1, and 33 µM for GRK5. It effectively inhibits GRK activity in cardiomyocytes and other muscle cell types, making it a valuable tool for investigating the role of GRKs in cardiac function. This compound is relevant for research into various cardiovascular conditions, including heart failure, myocardial hypertrophy, and hypertension. -
GRK Inhibitor
GRL093-22 is a potent and selective inhibitor of G protein-coupled receptor kinases (GRKs), displaying IC50 values of 60 nM for GRK5 and 40 nM for GRK6. This compound is valuable for research on mechanisms underlying heart failure and multiple myeloma, facilitating investigations into the modulation of GRK activity in these conditions. -
Gβγ Antagonist
GRK2i is a selective Gβγ antagonist that inhibits Gβγ-mediated signaling pathways. This peptide corresponds to the Gβγ-binding domain of G-protein-coupled receptor kinase 2 (GRK2), making it a valuable tool for studying G-protein signaling mechanisms. Its application includes investigating the role of Gβγ subunits in various cellular processes and identifying potential therapeutic targets related to G-protein-coupled receptor signaling. -
GRK5 Inhibitor
CCG-273463 is a selective covalent inhibitor of G protein-coupled receptor kinase 5 (GRK5), demonstrating an IC50 of 8.6 nM. This compound is instrumental in research related to heart failure, hypertrophic cardiomyopathy, and various cancer pathways. Its specificity for GRK5 makes it a valuable tool for elucidating the role of this kinase in disease mechanisms and therapeutic development. -
GRK2 Inhibitor
CCG-224406 is a selective inhibitor of G protein-coupled receptor kinase 2 (GRK2), exhibiting an IC50 of 13 nM and demonstrating over 700-fold selectivity against other GRK subfamilies, with no inhibition of ROCK1. This small molecule is suitable for research into GRK2's role in heart failure and offers a valuable tool for exploring GRK-related signaling pathways in cardiovascular biology. -
GRK5 Inhibitor
GRK5-IN-3 is a covalent inhibitor targeting G Protein-Coupled Receptor Kinase 5 (GRK5). This compound demonstrates potent inhibitory activity against GRK5 and GRK6, with IC50 values of 0.22 μM and 0.41 μM, respectively. GRK5-IN-3 is suitable for research applications focused on understanding the role of GRK5 in cellular signaling and its implications in various pathological conditions.
