2. Signaling Pathways
  3. GPCR/G Protein
  4. Formyl Peptide Receptor (FPR)

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 (55):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P1119
    WRW4
    		99.80%
    WRW4, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC50 of 0.23 μM. WRW4 specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide.
    WRW4
  • HY-P1122
    Cyclosporin H
    		99.87%
    Cyclosporin H is a selective and potent inhibitor of FPR-1 (formyl peptide receptor 1). Cyclosporin H, a viral transduction enhancer, increases lentiviral transduction up to 10-fold in human cord blood-derived hematopoietic stem and progenitor cells (HSPCs). Cyclosporin H displays an additive effect when combined with Rapamycin (HY-10219) or Prostaglandin E2 (HY-101952). Cyclosporin H lacks immunosuppressant activity of Cyclosporin A.
    Cyclosporin H
  • HY-101283
    HCH6-1
    		99.16%
    HCH6-1 is a potent and competitive dipeptide antagonist of Formyl peptide receptor 1 (FPR1). HCH6-1 inhibits chemotaxis, superoxide anion generation, and elastase release in human neutrophils specifically activated by fMLF (an FPR1 agonist). HCH6-1 has protective effects against acute lung injury (ALI) in vivo and can be used for the research of FPR1-involved inflammatory lung diseases.
    HCH6-1
  • HY-131180
    BMS-986235
    		99.74%
    BMS-986235 (LAR-1219) is a selective, orally active formyl peptide receptor 2 (FPR2) agonist, with EC50s of 0.41 nM and 3.4 nM for hFPR2 and mFPR2, respectively. BMS-986235 has potential for the prevention of heart failure.
    BMS-986235
  • HY-P1120
    WKYMVm
    		99.74%
    WKYMVm 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. 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.
    WKYMVm
  • HY-P11704
    f-MKKFRW
    		Activator
    f-MKKFRW is a selective mouse formyl peptide receptor 3 (Fpr3) activator and bacterial MgrB-derived peptide motif. f-MKKFRW activates Fpr3 to trigger downstream signaling and calcium responses in Fpr3-expressing cells. f-MKKFRW stimulates a subset of mouse vomeronasal sensory neurons in the accessory olfactory system to evoke calcium responses. f-MKKFRW drives innate avoidance behavior in mice via nasal contact.
    f-MKKFRW
  • HY-P11718
    cFLFLF
    		Ligand
    cFLFLF is a FPR-specific peptide. cFLFLF is sequentially conjugated with a bifunctional polyethylene glycol moiety (PEG, 3.4 kD) and a DOTA through a lysine (K) spacer and finally labeled with 64Cu-CuCl2 to form cFLFLFKPEG-64Cu. cFLFLFKPEG-64Cu is a neutrophil-specific PET imaging agent.
    cFLFLF
  • HY-181822
    BMS-986331
    		Agonist
    BMS-986331 is an orally active selective N-Formyl Peptide Receptor 2 (FPR2) agonist with an EC50 of 0.5 nM in humans and 1 nM in rats. BMS-986331 activates Gαi2, GαoA, Gα12, Gα13 signaling pathways, recruits β-arrestin1 and β-arrestin2, and inhibits downstream cAMP. BMS-986331 induces the expression and release of the pro-resolution cytokine IL-10. BMS-986331 improves cardiac structure and function in a rat model of heart failure induced by permanent coronary artery occlusion. BMS-986331 can be used for the research of heart failure.
    BMS-986331
  • HY-173591
    T0080
    		Antagonist 99.94%
    T0080 is a central nervous system-penetrant FPR1 inhibitor. By functionally blocking the FPR1 signaling pathway, T0080 effectively reduces neutrophil infiltration into ischemic brain tissue and maintains the integrity of the blood-brain barrier. T0080 alleviates tPA-associated hemorrhagic transformation, inhibits demyelination responses and the expression of NOX2. T0080 also possesses anti-apoptotic (apoptosis) and anti-inflammatory properties, thereby protecting myelin and reducing neurological deficits. T0080 is widely used in studies related to ischemic stroke complicated by hemorrhagic transformation after tPA thrombolysis, as well as multiple sclerosis.
    T0080
  • HY-19574
    FPR Agonist 43
    		99.79%
    FPR Agonist 43 (compound 43) is a dual formyl peptide receptor 1 (FPR1) and formyl peptide receptor 2 (FPR2)/ALX agonist.
    FPR Agonist 43
  • HY-P1795
    Boc-dPhe-Leu-dPhe-Leu-Phe
    		Antagonist 98.09%
    Boc-dPhe-Leu-dPhe-Leu-Phe (Boc-fLfLF) is a selective N-formyl peptide receptor1 (FPR1) antagonist. Boc-dPhe-Leu-dPhe-Leu-Phe inhibits fMIFL(HY-P0224)-induced NADPH oxidase activity. Boc-dPhe-Leu-dPhe-Leu-Phe can be used for the study of inflammation.
    Boc-dPhe-Leu-dPhe-Leu-Phe
  • HY-P4744A
    LL-37 amide TFA
    		Inhibitor 99.97%
    LL-37 amide TFA is a selective agonist of formyl peptide receptor-like FPRL1, effectively inhibiting periodontal pathogens (ED99=8.5-8.7 μg/mL). LL-37 amide TFA 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 TFA 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.
    LL-37 amide TFA
  • HY-P2355
    BOC-FlFlF
    		Antagonist 98.31%
    BOC-FlFlF (Boc-Phe-dLeu-Phe-dLeu-Phe) is a selective FPR1 antagonist. Boc-FlFlF has an apparent dissociation constant (KD) of 230 nM as determined by the intracellular calcium mobilization assay. Boc-FlFlF can be used for the study of inflammation.
    BOC-FlFlF
  • HY-103473
    Boc-MLF
    		Antagonist 99.36%
    Boc-MLF is a formyl peptide receptor (FPR) antagonist, and reduces superoxide production induced by fMLF with an IC50 of 0.63 μM.
    Boc-MLF
  • HY-124071
    ACT-389949
    		99.96%
    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. ACT-389949 has potential for the treatment of inflammatory disorders.
    ACT-389949
  • HY-156293
    FPR1 antagonist 1
    		Antagonist
    FPR1 antagonist 1 (compound 24a) is a formyl peptide receptor 1 (FPR1) antagonist with an IC50 of 25 nM. FPR1 antagonist 1 inhibits cell growth through a combined effect on cell proliferation and apoptosis and reduces cell migration, while inducing an increase in angiogenesis.
    FPR1 antagonist 1
  • HY-103473A
    Boc-MLF TFA
    		99.69%
    Boc-MLF (TFA) is a peptide, used as a specific formyl peptide receptor (FPR) antagonist, also inhibits the signaling through formyl peptide receptor like 1 (FPRL1) at higher concentrations.
    Boc-MLF TFA
  • HY-P1121A
    WKYMVM-NH2 TFA
    		99.67%
    WKYMVM-NH2 TFA is a potent N-formyl peptide receptor (FPR1) and FPRL1/2 agonist, also activates several leukocyte effector functions such as chemotaxis, mobilization of complement receptor-3, and activation of the NADPH oxidase.
    WKYMVM-NH2 TFA
  • HY-P10738
    N-Formyl-MMYALF
    		Inhibitor 99.78%
    N-Formyl-MMYALF is a potent mitochondrial N-formyl peptide (mtFP) that has the activity of depleting calcium ions in the endoplasmic reticulum. N-Formyl-MMYALF can inhibit the FPR-1-mediated chemotactic response of polymorphonuclear leukocytes (PMNs) to bacterial peptides.
    N-Formyl-MMYALF
  • 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.
    MMK1