Catalog No.
Product Name
Application
Product Information
Citations
-
TGR5(GPCR19) agonist
TGR5 Receptor Agonist is a potent TGR5(GPCR19) agonist, showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5). - Sodium deoxycholate is a bile acid formed by bacterial action from cholate. It is usually conjugated with glycine or taurine. Deoxycholic acid acts as a detergent to solubilize fats for intestinal absorption, is reabsorbed itself, and is used as a choleretic and detergent.
-
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
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. -
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. -
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.
