Formyl Peptide Receptor (FPR)

Formyl peptide receptors (FPRs) are a group of G protein-coupled chemoattractant receptors, including FPR1, FPR2 and FPR3. FPR1 and FPR2 are expressed in both monocytes and neutrophils, while FPR3 is found in monocytes but not neutrophils. Besides myeloid cells, FPR1 is expressed in astrocytes, microglial cells, hepatocytes and immature dendritic cells. FPR2 shows an even wider distribution pattern than FPR1 and is expressed in a variety of non-myeloid cells including astrocytoma cells, epithelial cells, hepatocytes, microvascular endothelial cells, neuroblastoma cells, in addition to phagocytic leukocytes. FPRs are classified as Pathogen Recognition Receptors (PRRs) located on immune cells that play a key role in innate immunity due to their ability to recognize both, pathogen associated and damage-associated molecular patterns (PAMPs and DAMPs). FPRs participate not only in host defense and regulation of inflammatory response but also in the migration, proliferation, superoxide production and in several physio-pathological processes due to their unique binding properties and interaction with structurally diverse ligands.

Formyl Peptide Receptor (FPR) Related Products (56):

By Effects:	Inhibitors (7) Agonists (15) Ligand (1) Antagonists (10) Activators (3)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-P1744

N-Formyl-Met-Leu-Phe-Lys		99.83%
N-Formyl-Met-Leu-Phe-Lys (fMLFK) is a peptide, acts as a potent and selective agonist of FPR1, with EC₅₀s of 3.5 nM, 6.7 μM and 0.88 μM for FPR1, FPR2 and FPR2-D281^7.32G, respectively.

HY-P1117

MMK1	Agonist	99.71%
MMK1 is a potent and selective human formyl peptide receptor like-1 (FPRL-1/FPR2) agonist with EC₅₀s of <2 nM and >10000 nM for FPRL-1 and FPR1, respectively. MMK1 is a potent chemotactic and calcium-mobilizing agonist. MMK1 potently activates phagocytic leukocytes and enhances Pertussis Toxin-sensitive production by human monocytes of proinflammatory cytokines IL-1b and IL-6. MMK1 exerts anxiolytic-like activity.

HY-W668775

Quin-C7	Antagonist	99.76%
Quin-C7 is an orally active FPR2/ALX antagonist. Quin-C7 has anti-inflammatory activity and can ameliorate DSS (HY-116282)-induced colitis in mice. Quin-C7 can be used in the research of inflammatory bowel disease.

HY-P10724

fMIFL	Agonist	99.79%
fMIFL is a formyl tetrapeptide derived from Staphylococcus aureus, and also an agonist of mouse formyl peptide receptor 1 (mFPR1). It exhibits nanomolar activity against mFPR1 and micromolar activity against mFPR2. fMIFL is applicable to studies related to bacterial infections.

HY-P4744

LL-37 amide	Inhibitor	99.77%
LL-37 amide is a selective agonist of formyl peptide receptor-like FPRL1, effectively inhibiting periodontal pathogens (ED₉₉=8.5-8.7 μg/mL). LL-37 amide exerts its bactericidal effect by activating FPRL1-mediated immune cell chemotaxis and disrupting bacterial cell membrane integrity. It can also regulate inflammatory responses (inhibiting the release of factors such as TNF-α) and promote angiogenesis. Amidation modification reduces its sensitivity to serum inhibition and improves its stability. LL-37 amide possesses key activities in bactericidal action, immunomodulation, and wound healing, and is mainly used in research on infection-related diseases such as periodontal disease and deep tissue injuries (pressure ulcers), and wound healing.

HY-155335

FPR2 agonist 3	Agonist	99.39%
FPR2 agonist 3 (compound CMC23) can limit the lactate dehydrogenase release in LPS (HY-D1056) -stimulated cultures and decrease the levels of pro-inflammatory IL-1β and IL-6. FPR2 agonist 3 decrease the level of phosphor-STAT3 via the STAT3/SOCS3 signaling pathway.

HY-172435

Rezuforimod	Agonist	98.63%
Rezuforimod (AGN-232411; AG-80308) is an ophthalmic solution targeting the formyl peptide receptor (FPR) pathway. Rezuforimod exerts anti-inflammatory effects by targeting the formyl peptide receptor pathway. Administered topically, Rezuforimod significantly reduces the corneal conjunctival staining score and improves ocular discomfort symptoms, with no serious adverse events reported and favorable overall safety profile. Rezuforimod shows remarkable potential to serve as a novel therapeutic option for dry eye disease.

HY-117971

BVT173187	Inhibitor	99.97%
BVT173187 is a selective inhibitor of the neutrophil formyl peptide receptor FPR1, with activity that inhibits FPR1 activation. BVT173187 inhibits FPR1 agonist-induced activation in neutrophils, reduces adhesion molecule mobilization and superoxide anion production, and has inhibitory activity on FPR1 similar to that of earlier described peptide antagonists, but also has effects on C5aR and CXCR signaling.

HY-P1591

N-Formyl-Nle-Leu-Phe-Nle-Tyr-Lys		98.86%
N-Formyl-Nle-Leu-Phe-Nle-Tyr-Lys TFA (For-Nle-Leu-Phe-Nle-Tyr-Lys-OH TFA) is a formyl peptide receptor (FPR) agonist.

HY-176403

FPR1 antagonist 3	Antagonist	98.07%
FPR1 antagonist 3 (compound 10) is a potent and selective FPR1 antagonist. FPR1 antagonist 3 inhibits superoxide anion generation and elastase release with IC₅₀s of 0.33 and 0.84 μM, respectively.

HY-P1118

Ac9-25		98.14%
Ac9-25, a N-terminal peptide of Annexin I, acts as a formyl peptide receptor (FPR) agonist and activates the neutrophil NADPH oxidase through FPR.

HY-103472

FPR-A14	Agonist	98.58%
FPR-A14 is a potent formyl peptide receptor (FPR) agonist. FPR-A14 is a potent activator of neutrophil Ca²⁺ mobilization and chemotaxis with EC₅₀s of 630 nM and 42 nM, respectively. FPR-A14 induces cell differentiation.

HY-144604

FPR2 agonist 2	Agonist	98.51%
FPR2 agonist 2 is a potent and CNS-penetrant FPR2 agonist with an EC₅₀ of 0.13 μM, 1.1 μM for FPR2 and FPR1, respectively. FPR2 agonist 2 inhibits the production of pro-inflammatory cytokines, counterbalances the changes in mitochondrial function, and inhibits caspase-3 activity.

HY-P991864

Annexuzlimab	Inhibitor
Annexuzlimab is a humanised IgG1 monoclonal antibody which specifically binds to ANXA1 disrupting its interaction with formyl peptide receptors 1 and 2 (FPR1/2). Annexuzlimab arrests cell cycle progression with cancer cells accumulating in the G1 phase. Annexuzlimab targets secreted ANXA1, preventing FPR1/2 activation and reducing cancer progression. Annexuzlimab can be used for the research of triple negative breast cancer, pancreatic cancer and osteosarcoma.

HY-P10738A

N-Formyl-MMYALF TFA	Inhibitor
N-Formyl-MMYALF TFA is a mitochondrial N-formyl peptide that has the activity of depleting calcium ions in the endoplasmic reticulum. N-Formyl-MMYALF TFA can inhibit the FPR-1-mediated chemotactic response of PMNs to bacterial peptides.

HY-P1756

N-Formyl-Met-Ala-Ser		98.08%
N-Formyl-Met-Ala-Ser is a peptide, binds to formyl peptide receptors on neutrophils.

HY-110246

Quin C1	Agonist	98.47%
Quin C1 is a highly specific and potent agonist for formyl peptide receptor 2 (FPR2/ALX). Quin-C1 significantly reduces the neutrophil and lymphocyte counts in BALF, diminishes expression of TNF-α, IL-1β, KC, and TGF-β1, and decreases collagen deposition in lung tissue. Quin C1 has the potential for the research of lung injury.

HY-P1120A

WKYMVm TFA
WKYMVm (TFA) is a selective formylpeptide receptor 2 (FPR2) agonist. WKYMVm has a powerful anti-inflammatory effect that can reduce lung injury and spinal cord injury. WKYMVm ameliorates obesity by regulating lipid metabolism and leptin signaling. WKYMVm is involved in the regulation of immune cells by activating FPRs, and WKYMVm can promote the chemotactic migration of immune cells and inhibit the apoptosis of phagocytes. In addition, WKYMVm may play a favorable or unfavorable role in tumors, depending on the type of tumor.

HY-P1119A

WRW4 TFA
WRW4 TFA, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC₅₀ of 0.23 μM. WRW4 TFA specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide.

HY-W745090

Isomaltulose monohydrate	Activator
Isomaltulose monohydrate is a fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Isomaltulose monohydrate can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC₅₀: 1.98 μM) , cathepsin G release (IC< sub>50: 2.76 μM) and chemotaxis. Isomaltulose monohydrate can improve excessive activation of neutrophils and reduce inflammation or tissue damage. A series of derivatives of Isomaltulose monohydrate are found to have inhibitory effects on FSGS-related TRPC6 functional mutants.

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