Catalog No.
Product Name
Application
Product Information
Citations
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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. -
GRK6 Inhibitor
GRK6-IN-5 is a selective inhibitor of G protein-coupled receptor kinase 6 (GRK6), exhibiting an IC50 of 4.48 μM. This compound is instrumental for investigating its role in hematological malignancies, inflammation-related conditions, and autoimmune disorders. Researchers can utilize GRK6-IN-5 to elucidate the biochemical pathways influenced by GRK6, potentially leading to therapeutic advancements in these diseases. -
GRK5 Inhibitor
GRK5-IN-5 is a selective inhibitor of G protein-coupled receptor kinase 5 (GRK5), demonstrating an IC50 of 0.03 μM. This compound also exhibits activity against GRK2 and GRK6, with IC50 values of 2.2 μM and 0.036 μM, respectively. GRK5-IN-5 is known for its potent activity in inhibiting myocardial hypertrophy and reducing non-myocardial cell proliferation. It effectively suppresses the upregulation of hypertrophy markers Nppa and Nppb, thereby preventing pathological remodeling of cardiac tissue. This reagent is valuable for investigating mechanisms underlying cardiac hypertrophy. -
G Protein-coupled Receptor 40 Agonist
DS-1558 is an orally bioavailable small molecule that acts as an agonist for G Protein-coupled Receptor 40 (GPR40). It enhances glucose-stimulated insulin secretion mediated by glucagon-like peptide-1 (GLP-1) and amplifies the insulinogenic response to intravenous glucose in normal Sprague Dawley rats. This compound is a valuable tool for researching mechanisms underlying type 2 diabetes and developing potential therapeutic strategies. -
GLP-1R/GCGR Agonist
Mazdutide is a long-acting synthetic analog of oxyntomodulin that functions as a dual agonist of the glucagon-like peptide-1 receptor (GLP-1R) and the glucagon receptor (GCGR). By binding to these targets with high affinity (Ki values of 17.7 nM for GCGR and 28.6 nM for GLP-1R in humans), Mazdutide promotes insulin secretion from mouse islets (EC50: 5.2 nM). This compound is primarily utilized in research addressing obesity and type 2 diabetes (T2D) to explore its therapeutic potential and metabolic effects. -
GLP-1R Agonist
GLP-1R Agonist 2 is a potent agonist of the glucagon-like peptide-1 receptor (GLP-1R), functioning through the formation of hydrogen bonds with key residues Tyr42, Cys71, and Ser84. This compound demonstrates significant biological activity in stimulating insulin secretion and inhibiting glucagon release, making it a valuable tool for research into metabolic disorders such as type 2 diabetes and obesity. Its mechanism of action positions it as an important candidate for the development of therapeutics targeting these conditions. -
GCGR/GLP-1R Agonist
Survodutide is a potent dual agonist of the glucagon receptor (GCGR) and GLP-1 receptor (GLP-1R), exhibiting EC50 values of 0.52 nM and 0.33 nM, respectively, in CHO-K1 cells. This 29-amino-acid acylated peptide, featuring a C18 fatty acid, demonstrates significant anti-obesity effects through mechanisms that enhance energy expenditure and reduce food intake. Survodutide is valuable for research into metabolic disorders and obesity management. -
GLP-1 Receptor Antagonist
GLP-1(9-36)amide is a potent antagonist of the glucagon-like peptide-1 (GLP-1) receptor, generated from the enzymatic action of dipeptidyl peptidase-4 (DPP-4) on GLP-1(7-36)amide. This peptide plays a crucial role in glucose metabolism and insulin signaling and is utilized in research aimed at understanding metabolic disorders and the role of GLP-1 in obesity and diabetic conditions. The study of GLP-1(9-36)amide can provide insights into receptor regulation and potential therapeutic strategies for GLP-1 related pathologies. -
GLP-1R/GLP-2R Agonist
Dapiglutide is a dual agonist targeting the glucagon-like peptide-1 receptor (GLP-1R) and glucagon-like peptide-2 receptor (GLP-2R). This long-acting compound has been shown to mitigate intestinal dysfunction in mouse models of short bowel syndrome and exhibits significant anti-obesity properties. Dapiglutide is valuable for research into metabolic disorders and the therapeutic potential of GLP-1/GLP-2 receptor modulation. -
GCGR Modulator
LSN3318839 is an orally active positive modulator of the glucagon receptor (GCGR). This compound enhances insulin secretion and exhibits hypoglycemic effects, making it valuable in the study of glucose metabolism and diabetes management. It is suitable for research applications focused on metabolic disorders and endocrine signaling pathways. -
GLP-1 Receptor Agonist
TT-OAD2 is a non-peptide agonist of the glucagon-like peptide-1 (GLP-1) receptor, exhibiting a potent EC50 of 5 nM. This compound plays a significant role in enhancing glucose-dependent insulin secretion and may be utilized in the treatment of diabetes. Its selective activity makes it a valuable tool for studying GLP-1 receptor signaling pathways and their implications in metabolic disorders. -
GLP-1R Agonist
Orforglipron hemicalcium hydrate is a calcium salt hydrate derivative of Orforglipron, functioning as a GLP-1 receptor (GLP-1R) agonist. This compound demonstrates significant biological activity in enhancing insulin secretion and lowering blood glucose levels, making it a pivotal candidate for research in type 2 diabetes treatment. Its oral bioavailability and receptor selectivity support various studies aimed at understanding the therapeutic potential of GLP-1R modulation in metabolic disorders. -
GLP-1/GCGR Agonist
Cotadutide is a potent dual agonist of glucagon-like peptide-1 (GLP-1) and glucagon receptor (GCGR), demonstrating EC50 values of 6.9 pM and 10.2 pM, respectively. This compound effectively promotes weight loss, enhances glycemic control, and alleviates fibrosis. Cotadutide is suitable for research applications focused on obesity and type 2 diabetes (T2D). -
GCGR Agonist
Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist that primarily targets the glucagon receptor (GCGR). It exhibits potent biological activity with an EC50 value of 0.06 nM. This compound is primarily investigated for its therapeutic potential in managing type 2 diabetes, promoting insulin secretion, and regulating glucose metabolism. Research applications include studying metabolic disorders and developing treatments for diabetes-related complications. -
GLP-2 Receptor Partial Agonist
GLP-2(3-33) is a partial agonist of the GLP-2 receptor, generated through the enzymatic action of dipeptidylpeptidase IV (DPPIV). It exhibits biological activity with an EC50 of 5.8 nM, making it a valuable tool for research into gastrointestinal physiology and potential therapeutic applications in metabolic disorders. Its role in modulating the GLP-2 receptor provides insight into gut hormone signaling and its effects on intestinal growth and function. -
Antioxidant
GLP-1(28-36)amide is a C-terminal nonapeptide derived from the cleavage of GLP-1 by neutral endopeptidase. This compound functions primarily as an antioxidant, targeting mitochondria and inhibiting mitochondrial permeability transition (MPT). GLP-1(28-36)amide exhibits significant anti-diabetic properties and offers cardioprotective effects, making it valuable in research focused on metabolic and cardiovascular diseases. -
Fragment Of Dulaglutide
GLP-1 moiety from Dulaglutide is a 31-amino acid fragment that acts as a glucagon-like peptide 1 (GLP-1) receptor agonist. This compound plays a crucial role in regulating glucose metabolism and insulin secretion, making it pertinent for research applications related to diabetes and myocardial injury. Its therapeutic potential is significant in studying metabolic disorders and cardiovascular health.
