Catalog No.
Product Name
Application
Product Information
Citations
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GPR agonist
TAK-875 is a potent, selective, and orally bioavailable GPR40 agonist.- Ying Liu, .et al. , Nucleic Acids Res, 2018, Oct 12; 46(18): 9864-9874 PMID: 30219861
- Deborah A. Goldspink, .et al. , Mol Metab, 2018, Jan; 7: 90-101 PMID: 29167062
- Hodaka Yamada, .et al. , Sci Rep, 2016, 6: 25912 PMID: 27180622
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GPR40 Inhibitor
GW 9508 is a cell-permeable aminophenylpropanoate that acts as a potent and selective agonist for the G-protein coupled receptor (GPCR) GRP40/FFA1 receptor (EC50 ?50 nM) with reduced activity towards family members GRP120 (EC50 ?3.5 μM), GRP41/GRP43 (EC50 >50 μM), as well as a panel of eight other free fatty acid (FFA) and prostaglandin receptors. -
GPR40/FFA1 agonist
AMG-837 calcium hydrate is a potent, orally bioavailable GPR40 agonist. -
FFA4/GPR120 agonist
GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively. - GPR120 modulator 1 is useful for modulating G protein-coupled receptor 120 (GPR120).
- GPR120 modulator 2 is useful for modulating G protein-coupled receptor 120 (GPR120).
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GPR40 full agonist
GPR40 agonist 1 is a potent and novel GPR40 full agonist with an EC50 of 2 nM and 17 nM for hGPR40 and rGPR40, respectively. -
GPR120 agonist
GPR120 Agonist 2 is a GPR120 agonist extracted from patent US 20110313003 A1, example 209. - Grifolic acid is a selective partial agonist of GPR120 that induces ERK activation and intracellular calcium responses in mouse enteroendocrine STC-1 cells.
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GPR120 agonist
GPR120 Agonist 1 is a potent and selective GPR120 agonist, and possesses promising antidiabetic effect and good safety profile to be a development candidate. -
GPR40/FFAR1 agonist
GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1). -
Gpr120 agonist
GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of ?7.62. -
GPR40 agonist
Setogepram sodium salt (PBI-4050 sodium salt) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. -
FFAR1/GPR40 activator
GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes. -
GPR40 activator
GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1. -
GPR40 agonist
AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. -
FFAR3 agonist
AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, also known as GPR41), with an IC₅₀ of 117 nM. It demonstrates anti-inflammatory, antitumor, and antidiabetic activities. AR420626 improves neurogenic diarrhea by modulating neural pathways mediated by nicotinic acetylcholine receptors (nAChRs). In cancer models, it suppresses the growth of HepG2 xenografts and inhibits hepatoma cell proliferation through apoptosis induction. Additionally, AR420626 mitigates allergic asthma and eczema and enhances glucose uptake by activating FFAR3-mediated Ca²⁺ signaling, offering potential therapeutic benefits in metabolic disorders such as diabetes. -
FFA4 Antagonist
AH-7614 is a selective antagonist of FFA4 (GPR120), exhibiting potent inhibition with pIC50 values of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. This compound demonstrates high specificity for FFA4 over FFA1, with a pIC50 value lower than 4.6. AH-7614 effectively blocks the biological effects induced by both linoleic acid, a polyunsaturated ω-6 fatty acid, and synthetic FFA4 agonists, making it a valuable tool for research on metabolic processes and signaling pathways associated with fat metabolism. -
FFAR1 Agonist
Tricosanoic acid is a natural agonist of the free fatty acid receptor FFAR1, primarily involved in stimulating hair growth. This long-chain saturated fatty acid also plays a significant role in enhancing cognitive function by modulating neuronal membrane fluidity, reducing neuroinflammation, and supporting myelination and energy metabolism in neurons. Notably, diminished levels of tricosanoic acid are observed in the prefrontal cortex of Alzheimer's disease models, with improved cognitive performance linked to elevated serum concentrations. Thus, tricosanoic acid has potential as a biomarker for conditions associated with cognitive decline. -
FFA2 Agonist
4-CMTB is a selective agonist for the free fatty acid receptor 2 (FFA2/GPR43), functioning as a positive allosteric modulator with a pEC50 of 6.38. This compound enhances receptor activity, making it valuable for studying metabolic processes and the regulation of inflammation. Its unique mechanism helps elucidate the role of FFA2 in various biological systems and potential therapeutic applications in metabolic diseases. -
FFA2 Allosteric Agonist
AMG7703 is a selective allosteric agonist of FFA2 (GPR43), a receptor that responds to short-chain fatty acids (SCFAs) such as acetate and propionate. This compound modulates FFA2 activity, making it a valuable tool for investigating its role in inflammatory and metabolic processes. Research applications include studying the physiological effects of SCFAs and their potential therapeutic implications in metabolic disorders. -
FFA2R Antagonist
CATPB is a selective antagonist of the free fatty acid receptor 2 (FFA2R/GPR43). It exhibits potent inhibitory activity, making it a valuable tool for studying the role of FFA2R in various biological processes. Research applications include investigating metabolic disorders and inflammatory responses, as well as exploring the receptor's potential as a therapeutic target. -
FFA1 Agonist
TUG-469 is a selective agonist of the free fatty acid receptor 1 (FFA1/GPR40) with an EC50 value of 19 nM, demonstrating over 200-fold selectivity for FFA1 compared to FFA4. This compound has been shown to significantly enhance glucose tolerance in pre-diabetic mouse models. TUG-469 serves as a valuable tool for research into diabetes and metabolic disorders, advancing the understanding of FFA1 signaling in glucose homeostasis. -
FFAR Agonist
CFMB is a full agonist of FFAR2 and FFAR3, exhibiting EC50 values of 0.8 μM for human FFAR2 and 0.2 μM for rat FFAR2. This compound plays a significant role in mediating free fatty acid signaling, contributing to metabolic regulation and potential therapeutic strategies. CFMB is valuable in research applications aimed at exploring the physiological effects and signaling pathways associated with FFAR modulation. -
FFAR1 Agonist
TUG-499 is a selective agonist of the free fatty acid receptor 1 (FFAR1 or GPR40), showcasing a pEC50 of 7.39. This compound demonstrates over 100-fold selectivity against related receptors, including FFA2, FFA3, and PPARγ, as well as other receptors, ion channels, and transporters. TUG-499 serves as a valuable tool in the investigation of type 2 diabetes and features an alkyne group, enabling its use in click chemistry applications through copper-catalyzed azide-alkyne cycloaddition (CuAAc). -
AH-7614 Analog
TUG-1387 is a structural analog of the FFA4 antagonist AH-7614 and serves as a negative control compound in research involving FFA4 functional assessments. It does not exhibit inhibitory activity against the FFA4 receptor, making it an ideal reference compound for evaluating the efficacy of FFA4 antagonists. TUG-1387 is valuable in studies aimed at understanding the role of FFA4 in various biological processes. -
Isomer
(S)-GLPG0974 is the isomer of GLPG0974 and serves as an experimental control in research settings. It acts as a potent antagonist of the free fatty acid receptor-2 (FFA2/GPR43) with an IC50 of 9 nM, making it valuable for studies investigating FFA2-mediated biological processes. This compound can be employed in various applications, including metabolic research and inflammation-related studies. -
Free Fatty Acid Receptor Agonist
TUG-424 is a selective agonist for the free fatty acid receptor 1 (FFA1/GPR40) with an EC50 of 32 nM. It significantly enhances glucose-stimulated insulin secretion at concentrations of 100 nM, making it a valuable tool for investigating the role of FFA1 in metabolic disorders such as diabetes and obesity. Additionally, TUG-424 contains an alkyne group and can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating its use in click chemistry applications. -
FFA2 Agonist
MOMBA is a selective agonist of the Free Fatty Acid Receptor 2 (FFA2), acting at the orthosteric site to activate receptor signaling pathways with high specificity. This reagent is valuable for investigating metabolic and inflammatory diseases, providing insights into receptor-mediated physiological responses and potential therapeutic targets. -
FFA3 Agonist
FFA3 Agonist 1 is a selective agonist of the free fatty acid receptor 3 (FFA3). By activating FFA3, this compound plays a crucial role in modulating the health effects of the intestinal microbiota, which is essential for maintaining gut homeostasis. FFA3 Agonist 1 is valuable for research applications exploring metabolic regulation and the interplay between diet, gut microbiota, and overall health. -
R-enantiomer of CFMB
(R)-CFMB is the R-enantiomer of CFMB, functioning as a selective agonist for the free fatty acid receptors FFAR2 and FFAR3. This compound exhibits remarkable biological activity, with EC50 values of 0.8 μM for human FFAR2 and 0.2 μM for rat FFAR2. It is valuable in research applications focusing on metabolic disorders and inflammation, providing insights into receptor signaling pathways and therapeutic targets. -
FFA2 Activator
AZ1729 is a potent allosteric agonist and positive modulator of the free fatty acid 2 receptor (FFA2). It enhances the activity of the endogenous short-chain fatty acid propionate in Gi-mediated signaling pathways, while exhibiting no effect on Gq/G11 transduction. In addition, AZ1729 has been shown to inhibit isoproterenol-induced lipolysis in mouse adipocytes and promote the migration of human neutrophils. This compound is valuable for studying the physiological roles and signaling pathways associated with FFA2. -
Isomer
(R)-Fasiglifam is the isomer of Fasiglifam, serving as an important experimental control in research. Fasiglifam is a selective and potent agonist of the G protein-coupled receptor GPR40, exhibiting an EC50 of 72 nM. This compound is primarily utilized in studies related to glucose metabolism and insulin secretion, highlighting its relevance in investigating metabolic disorders such as type 2 diabetes. -
Free Fatty Acid Receptor
3-Chloropropane-1,2-diol dipalmitate acts as a ligand for free fatty acid receptors, influencing various biological signaling pathways. This compound is primarily composed of diesters, making it relevant in studies focused on lipid metabolism and receptor activation. Research applications include investigations into metabolic disorders and the modulation of inflammatory responses through fatty acid signaling. -
FFAR1 Agonist
TP-051 is a potent agonist of FFAR1, exhibiting a Ki value of 16 nM for human FFAR1. This compound effectively stimulates insulin secretion in rat insulinoma cells, making it a valuable tool for studies related to type 2 diabetes. TP-051 can be utilized in research aimed at understanding the role of FFAR1 in metabolic disorders and the development of therapeutic strategies for diabetes management. -
FFA2 Agonist
FFA2 Agonist-1 is a selective agonist for the Free Fatty Acid Receptor 2 (FFA2/GPR43), exhibiting an EC50 of 81 nM. This compound effectively engages β-arrestin-2 in recruitment assays and demonstrates cAMP inhibition with EC50 values of 1.2 μM and 0.53 μM, respectively. FFA2 Agonist-1 has been shown to influence appetite regulation through peptide YY (PYY) mucosal responses, limiting fat accumulation and impacting intestinal functions and food intake. It is a valuable tool for obesity research and related metabolic studies. -
Antidiabetic Agent
GPR40 agonist 5 is a potent agonist of G protein-coupled receptor 40 (GPR40), exhibiting an EC50 of 47 nM. This compound demonstrates significant antidiabetic activity by reducing blood glucose levels and enhancing glucose tolerance, making it relevant for research in type 2 diabetes models. Additionally, GPR40 agonist 5 functions as a click chemistry reagent, featuring an alkyne group that allows for copper-catalyzed azide-alkyne cycloaddition with azide-containing molecules. -
FFAR1/FFAR4 Agonist
FFAR1/FFAR4 agonist-1 is a potent agonist of both FFAR1 and FFAR4, exhibiting an EC50 of 1 nM for FFAR1 and 4 nM for FFAR4. This compound demonstrates significant biological activity in modulating glucose metabolism and has potential applications in research focused on glycemic control and metabolic disorders. Its specificity and efficacy make it a valuable tool for exploring the roles of FFAR1 and FFAR4 in metabolic pathways. -
Neuroprotective Agent
Termitomycamide B, a neuroprotective agent isolated from Termitomyces titanicus, primarily functions by inhibiting endoplasmic reticulum stress-dependent cell death. This compound demonstrates significant potential in the research of neurodegenerative diseases, providing valuable insights into mechanisms of neuroprotection and potential therapeutic strategies. Researchers may utilize Termitomycamide B to explore its effects on cell survival and stress responses in neuronal models.
