Date published: 2025-9-5

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FPR Activators

Formyl Peptide Receptors (FPRs) are integral components of the innate immune system, functioning as G-protein-coupled receptors (GPCRs) that detect formyl peptides found in both bacterial sources and host mitochondria. These receptors are primarily expressed on the surface of phagocytic leukocytes, including neutrophils, monocytes, and dendritic cells, where they play a critical role in guiding these cells to sites of infection or tissue damage. Activation of FPRs triggers a series of intracellular signaling pathways that lead to chemotaxis, the directed movement of immune cells towards the source of formyl peptides, as well as the activation of cellular functions necessary for pathogen clearance, including phagocytosis, the release of proteolytic enzymes, and the production of reactive oxygen species. This receptor-ligand interaction is fundamental to the host's ability to rapidly respond to microbial invasion, facilitating early immune responses and initiating the recruitment of other immune cells to amplify and sustain the inflammatory response. The specificity and sensitivity of FPRs to their ligands enable the immune system to quickly detect and respond to pathogens, highlighting the importance of these receptors in maintaining host defense and homeostasis.The activation mechanism of FPRs involves the binding of formyl peptides to the extracellular domain of the receptor, initiating a conformational change that activates the associated G-proteins. This activation leads to the dissociation of Gα and Gβγ subunits, which then interact with downstream effectors to generate second messengers, such as inositol trisphosphate (IP3) and diacylglycerol (DAG), and to increase intracellular calcium levels. These signaling molecules collectively contribute to the activation of various intracellular pathways, including the MAPK/ERK pathway, PI3K/Akt pathway, and the PLCβ pathway, each playing a role in mediating cellular responses such as chemotaxis, degranulation, and the oxidative burst. The precise regulation of FPR activation is critical, as it ensures an effective immune response against pathogens while inhibiting excessive inflammation that could lead to tissue damage. Through the nuanced control of these signaling cascades, FPRs orchestrate a finely balanced immune response, demonstrating their vital role in the rapid detection of microbial threats and the coordination of the body's defense mechanisms.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

N-Formyl-Met-Leu-Phe

59880-97-6sc-358988
sc-358988A
5 mg
10 mg
$44.00
$59.00
(1)

N-Formyl-Met-Leu-Phe acts as a potent FPR, showcasing remarkable selectivity in receptor binding due to its unique peptide structure. The compound's conformation allows for specific interactions with G-protein coupled receptors, triggering distinct intracellular signaling cascades. Its stability in physiological conditions enhances its kinetic profile, promoting rapid receptor activation. Additionally, the compound's hydrophobic regions facilitate membrane penetration, influencing its bioactivity and interaction dynamics.

FPR A14

329691-12-5sc-294992
sc-294992A
2 mg
10 mg
$160.00
$660.00
(0)

FPR A14 exhibits unique characteristics as a formyl peptide receptor (FPR) ligand, distinguished by its ability to engage in specific hydrogen bonding and hydrophobic interactions with receptor sites. This compound demonstrates a high affinity for G-protein coupled receptors, initiating targeted signaling pathways that modulate cellular responses. Its structural rigidity contributes to enhanced binding kinetics, while its amphipathic nature aids in effective membrane integration, influencing its overall biological activity.

15-keto Fluprostenol isopropyl ester

404830-45-1sc-220621
sc-220621A
1 mg
5 mg
$84.00
$380.00
(0)

15-keto Fluprostenol isopropyl ester functions as a potent FPR ligand, characterized by its selective binding to formyl peptide receptors. Its unique stereochemistry facilitates specific electrostatic interactions, enhancing receptor affinity. The compound's lipophilic properties promote efficient membrane penetration, while its conformational flexibility allows for dynamic receptor engagement. This results in distinct signaling cascades, influencing cellular behavior through modulation of intracellular pathways.

15(S)-Fluprostenol isopropyl ester

157283-68-6sc-220634
sc-220634A
1 mg
5 mg
$136.00
$615.00
(0)

15(S)-Fluprostenol isopropyl ester acts as a selective ligand for formyl peptide receptors, exhibiting unique molecular interactions due to its stereochemical configuration. The compound's hydrophobic characteristics enable effective integration into lipid bilayers, enhancing its bioavailability. Its ability to adopt multiple conformations allows for versatile binding dynamics, leading to varied downstream signaling effects. This adaptability in receptor engagement contributes to its distinct biological activity.

Lipoxin A4

89663-86-5sc-201060
sc-201060A
sc-201060B
sc-201060C
25 µg
50 µg
100 µg
250 µg
$342.00
$485.00
$923.00
$2025.00
2
(1)

Lipoxin A4 functions as an FPR activator by binding to the receptor and triggering a cascade of events. It enhances chemotaxis and reactive oxygen species production, contributing to FPR activation.

5(S),6(R)-7-trihydroxymethyl Heptanoate

78606-80-1sc-221076
sc-221076A
1 mg
5 mg
$64.00
$188.00
(0)

Also called BML-111, this compound serves as an FPR activator by directly binding to the receptor. It induces FPR-mediated calcium mobilization and downstream signaling, modulating cellular responses associated with FPR activation.