Catalog No.
Product Name
Application
Product Information
Citations
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ETA Antagonist
ETA Antagonist 2 is a selective antagonist of the endothelin A (ETA) receptor, which plays a critical role in vascular biology and pathophysiology. This compound effectively inhibits ETA receptor-mediated signaling pathways, resulting in vasodilation and reduced cellular proliferation. ETA Antagonist 2 is primarily utilized in research focused on cardiovascular diseases, pulmonary hypertension, and renal dysfunction to explore therapeutic avenues for endothelin-related disorders. -
Endothelin Receptor Antagonist
SB-209670 is a highly potent non-peptide antagonist of the endothelin (ET) receptor, exhibiting subnanomolar affinity with Ki values of 0.2 nM for ETA and 18 nM for ETB. This compound effectively inhibits the binding of 125I-labeled ET-1 to both human ET receptor subtypes, making it a valuable tool in cardiovascular and neurological research. SB-209670 demonstrates significant biological activity by reducing blood pressure in hypertensive models, offering neuroprotective effects against ischemia-induced neuronal degeneration, and inhibiting neointima formation following carotid artery balloon angioplasty in rats. -
ET Receptor Antagonist
Aselacin A is an endothelin-1 receptor (ET-1 receptor) antagonist that effectively inhibits the binding of endothelin-1 to both ETA and ETB receptors. Demonstrating IC50 values of 22 μg/mL and 20 μg/mL, it inhibits ET-1 binding to bovine atrial and porcine cerebral membranes, respectively. This compound is valuable for research into cardiovascular diseases and exploring the pathological roles of endothelin signaling in various cardiovascular conditions. -
ET Receptor Antagonist
WS009A is a potent antagonist of endothelin receptors, exhibiting IC50 values of 5.8 µM and 6.9 µM for the ET-1 and ET-2 receptors, respectively. This compound is valuable for investigating the role of endothelin signaling in cardiovascular diseases and potential therapeutic applications. Its effective inhibition of endothelin receptors makes WS009A a useful tool for researchers studying vascular dysfunction and related pathophysiological conditions. -
FPR2 Agonist
BMS-986235 is a highly selective, orally active agonist of formyl peptide receptor 2 (FPR2), exhibiting EC50 values of 0.41 nM for human FPR2 and 3.4 nM for murine FPR2. This compound demonstrates key biological activity relevant to modulating inflammatory responses and has potential applications in the prevention of heart failure. Its specificity for FPR2 makes it a valuable tool in research focusing on cardiovascular and inflammatory pathways. -
FPR1 Antagonist
Boc-dPhe-Leu-dPhe-Leu-Phe is a selective antagonist of the N-formyl peptide receptor 1 (FPR1). It effectively inhibits fMIFL-induced NADPH oxidase activity, making it a valuable tool in the study of inflammatory processes. This compound is particularly useful for research aimed at understanding the mechanisms underlying inflammation and related signaling pathways. -
FPR Antagonist
BOC-FlFlF is a selective antagonist of the formyl peptide receptor 1 (FPR1). With an apparent dissociation constant (KD) of 230 nM, as determined by intracellular calcium mobilization assays, BOC-FlFlF demonstrates significant biological activity in inhibiting FPR1 signaling. This compound is valuable for research applications focused on inflammation and related signaling pathways. -
FPR1 Antagonist
FPR1 antagonist 1 is a selective antagonist of formyl peptide receptor 1 (FPR1) with an IC50 of 25 nM. This compound effectively inhibits cell growth by modulating both cell proliferation and apoptosis while simultaneously reducing cell migration. Additionally, FPR1 antagonist 1 has been shown to promote angiogenesis, making it a valuable tool for research applications related to cancer biology and inflammatory responses. -
FPR Antagonist
Boc-MLF is a selective antagonist of the formyl peptide receptor (FPR). This compound effectively inhibits superoxide production induced by fMLF, demonstrating an IC50 value of 0.63 μM. It is primarily utilized in research focused on inflammatory responses, immune modulation, and related signaling pathways. -
FPR Agonist
WKYMVM-NH2 TFA is a highly effective agonist of the N-formyl peptide receptors (FPR1) and FPRL1/2. This compound induces several key leukocyte effector functions, including chemotaxis, complement receptor-3 mobilization, and NADPH oxidase activation. It serves as a valuable tool for research focused on immune response mechanisms and the role of peptide receptors in leukocyte signaling. -
FPR1 Agonist
AG-09/1 is a specific agonist of the formyl peptide receptor 1 (FPR1), a crucial receptor involved in the immune response and host defense mechanisms. This compound activates FPR1, thereby influencing various biological activities such as chemotaxis and inflammation. AG-09/1 serves as a valuable tool for research into immune cell signaling, inflammatory pathways, and potential therapeutic interventions targeting FPR1-related conditions. -
FPR2/ALX Antagonist
Quin-C7 is an orally active antagonist of the FPR2/ALX pathways. This compound demonstrates significant anti-inflammatory activity and has been shown to ameliorate dextran sulfate sodium (DSS)-induced colitis in murine models. Quin-C7 is applicable in the research of inflammatory bowel disease and offers insights into therapeutic strategies targeting inflammatory processes. -
FPR2 Agonist
FPR2 Agonist 3 (compound CMC23) targets the formyl peptide receptor 2 (FPR2) to exhibit potent anti-inflammatory effects. This compound effectively limits lactate dehydrogenase release in LPS-stimulated cultures and reduces the secretion of pro-inflammatory cytokines IL-1β and IL-6. Additionally, FPR2 Agonist 3 downregulates phosphorylated STAT3 through the STAT3/SOCS3 signaling pathway, making it a valuable tool for research in inflammation and related signaling processes. -
FPR Agonist
Rezuforimod is a selective formyl peptide receptor (FPR) agonist that exhibits anti-inflammatory properties. This ophthalmic solution is designed for topical application and has been shown to significantly decrease corneal conjunctival staining and alleviate symptoms of ocular discomfort. With a favorable safety profile and no serious adverse events reported, Rezuforimod presents substantial potential as a novel therapeutic agent for the management of dry eye disease. -
FPR Agonist
N-Formyl-Nle-Leu-Phe-Nle-Tyr-Lys is a potent formyl peptide receptor (FPR) agonist, known for its ability to activate immune responses. This compound plays a significant role in studying inflammatory processes and immune cell signaling pathways. Its applications include research in chemotaxis, host defense mechanisms, and the modulation of immune responses, making it a valuable tool for scientists investigating FPR-related pathways. -
FPR Agonist
FPR-A14 is a potent agonist of the formyl peptide receptor (FPR), effectively activating neutrophil Ca2+ mobilization and chemotaxis with EC50 values of 630 nM and 42 nM, respectively. This compound also promotes cell differentiation, making it a useful tool for research into immune response mechanisms and inflammatory processes. FPR-A14 is suitable for studies involving neutrophil behavior and related signaling pathways. -
FPR2 Agonist
FPR2 Agonist 2 is a potent agonist targeting the formyl peptide receptor 2 (FPR2), demonstrating an EC50 of 0.13 μM for FPR2 and 1.1 μM for FPR1. This compound effectively inhibits the production of pro-inflammatory cytokines, restores mitochondrial function, and decreases caspase-3 activity. FPR2 Agonist 2 serves as a valuable tool for research in inflammation and neurobiology, facilitating studies related to immune responses and mitochondrial dynamics. -
FPR1 Antagonist
FPR1 Antagonist 3 is a potent and selective inhibitor of the formyl peptide receptor 1 (FPR1). It effectively inhibits superoxide anion generation and elastase release, with IC50 values of 0.33 μM and 0.84 μM, respectively. This compound is valuable for research applications aimed at investigating inflammatory responses and receptor signaling pathways related to FPR1 activity. -
FPR2/ALX Agonist
Quin C1 is a potent and selective agonist of the formyl peptide receptor 2 (FPR2/ALX). This compound effectively reduces neutrophil and lymphocyte counts in bronchoalveolar lavage fluid (BALF) and diminishes the expression of pro-inflammatory cytokines such as TNF-α, IL-1β, KC, and TGF-β1, while also decreasing collagen deposition in lung tissue. Quin C1 is valuable for investigating mechanisms underlying lung injury and inflammation. -
FPR Agonist
N-Formyl-Nle-Leu-Phe-Nle-Tyr-Lys TFA is a potent agonist of the formyl peptide receptor (FPR). This compound exhibits key biological activity by activating FPR, a receptor involved in immune response modulation and inflammation. Its applications in research include the investigation of immune cell signaling pathways and the study of inflammatory processes in various biological contexts. -
FPR2 Agonist
FPR2 agonist 4 is a potent selective agonist of the formyl peptide receptor 2 (FPR2), exhibiting an EC50 of 0.2 nM. This compound demonstrates significant biological activity in modulating immune responses, making it a valuable tool for research in inflammation and autoimmune disorders. Its high selectivity and efficacy position it for applications in the study of receptor signaling pathways and therapeutic interventions targeting FPR2. -
FPRL1/FPRL2 Recaptor Agonist
WKYMVM-NH2 is a hexapeptide that acts as an agonist for the FPRL1 and FPRL2 receptors, primarily activating neutrophils and myeloid cells. Its potent biological activity is characterized by EC50 values of 2 nM and 80 nM in HL-60 cells expressing FPRL1 and FPRL2, respectively. WKYMVM-NH2 induces chemotaxis in HL-60-FPRL2 cells, with optimal migration observed between 10 and 50 nM, and significantly stimulates superoxide production in neutrophils with an EC50 of 75 nM. This peptide serves as a valuable tool for studying inflammatory diseases and related mechanisms. -
FPRL1 Activator
SHAAGtide is an activator of the formyl peptide receptor-like 1 (FPRL1). This compound exhibits anti-inflammatory activity by modulating the immune response through FPR2, effectively reducing the expression of inflammatory cytokines in murine models. SHAAGtide is valuable for research investigating conditions such as lung inflammation and fibrosis, facilitating a deeper understanding of inflammatory pathways and potential therapeutic interventions. -
ALXR Agonist
ALXR-agonist-6 is a selective agonist of the ALX receptor, demonstrating an EC50 of >10 μM for calcium flux in CHO recombinant cells co-expressing the human formyl peptide receptor-like 1 (hFPRL1). This compound is valuable for investigating ALX receptor-mediated signaling pathways and inflammatory responses. Its applications extend to research on immune modulation and the pharmacological characterization of ALXR-targeted therapies. -
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. -
GPR120 Agonist
GPR120 Agonist 5 is a selective agonist for the GPR120 receptor, exhibiting an EC50 of 1.2 μM. This compound enhances the secretion of glucagon-like peptide-1 (GLP-1) through its interaction with GPR120, leading to increased insulin production and decreased blood glucose levels. Additionally, GPR120 Agonist 5 demonstrates anti-inflammatory properties, making it a valuable tool for studies focused on metabolic disorders, obesity, insulin resistance, and type 2 diabetes. This reagent is essential for investigating the biological functions and therapeutic potential of GPR120 in relevant disease models. -
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. -
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. -
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. -
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.
