Formyl Peptide Receptor (FPR) Agonist

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.

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.

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.

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.

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.

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.

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.

MMK1 TFA 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 TFA is a potent chemotactic and calcium-mobilizing agonist. MMK1 TFA potently activates phagocytic leukocytes and enhances Pertussis Toxin-sensitive production by human monocytes of proinflammatory cytokines IL-1b and IL-6. MMK1 TFA exerts anxiolytic-like activity.

FPR2 agonist 4 (compound 20) is a selective agonist of FPR2 with an EC₅₀ of 0.2 nM.

FPR2 agonist 5 is a selective Formyl Peptide Receptor 2 (FPR2) agonist. FPR2 agonist 5 induces Ca²⁺ mobilization in FPR2-HL60 transfected cells with an EC₅₀ of 1.2 μM and causes FPR2 desensitization with an IC₅₀ of 0.32 μM. FPR2 agonist 5 exerts neuroprotective effects by mitigating LDH release, NO production, IL-1β, IL-6, IL-33, and IL-10 levels in LPS (HY-D1056)-induced mouse primary microglial cells. FPR2 agonist 5 can be used for the study of neuroinflammatory-related diseases.

FPR2/ALXR agonist-1 is a selective FPR2/ALXR agonist. FPR2/ALXR agonist-1 activates neutrophil superoxide production. FPR2/ALXR agonist-1 can be used for research on inflammatory diseases.

WKYMVM-NH2 is a hexapeptide that activates neutrophils and myeloid cells via the FPRL1 and FPRL2 receptors. It exhibits EC₅₀ values of 2 nM and 80 nM in HL-60-FPRL1 and HL-60-FPRL2 cells, respectively. In HL-60 cells stably expressing FPRL2, WKYMVM-NH₂ induces chemotaxis, with optimal migration observed at concentrations ranging from 10 to 50 nM. It also stimulates superoxide production in neutrophils, with an EC₅₀ of 75 nM. WKYMVM-NH₂ is a useful tool for research in the field of inflammatory diseases.

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.

ALXR-agonist-6 (compound 36) is an ALXR agonist with the EC₅₀ values of >10 μM for Ca²⁺ flux in CHO recombinant cells co-expressing hFPRL1.

FPR-A14 (Standard) is the analytical standard of FPR-A14 (HY-103472). This product is intended for research and analytical applications. 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.