Formyl Peptide Receptor (FPR)

HCH6-1 is a competitive antagonist of Formyl peptide receptor 1 (FPR1), an emerging therapeutic target for the discovery of drugs to treat neutrophilic inflammatory diseases.

FPR Agonist 43 (compound 43) is a dual formyl peptide receptor 1 (FPR1) and formyl peptide receptor 2 (FPR2)/ALX agonist.

ACT-389949 is a first-in-class, potent and selective and agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC50 of 3 nM for FPR2/ALX internalization into monocytes.

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.

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.

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 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.

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.

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.

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.

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 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.

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.

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-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 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 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.

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.

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 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.

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.

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-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.