FPR2 agonist 2 is a potent and permeates the blood-brain barrier 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[1].
FPR2 agonist 2 (compound (S)-11l) (1-100 µM; 48 h) exhibits low cytotoxicity with an EC50 value of 20.8 µM in N9 cells[1].
FPR2 agonist 2 (FPR1/FPR2 HL60 cells) shows agonist activity with EC50s of 0.13 µM, 1.1 µM (IC50s of 0.085 µM, Not determined) for FPR2 and FPR1, respectively[1].
FPR2 agonist 2 (0.1 µM) effectively blocks LPS-induced cell death and NO production and effectively suppresses the effect of LPS stimulation[1].
FPR2 agonist 2 (0.1 µM) counterbalances the changes in mitochondrial function, and inhibits caspase-3 activity[1].
Cell Viability Assay[1]
| Cell Line: | N9 cells |
| Concentration: | 1-100 µM |
| Incubation Time: | 48 h |
| Result: | Exhibited low cytotoxicity with an EC50 value of 20.8 µM in N9 cells. |
FPR2 agonist 2 (1 mg/kg for i.v.; 10 mg/kg for i.p.) shows the ability to permeate the blood-brain barrier and to accumulate in the brain[1].
| Animal Model: | 25-30 g, male CD-1 mice[1] |
| Dosage: | |
| Administration: | 1 mg/kg for i.v.; 10 mg/kg for i.p. (dissolved in 5% DMSO, 10% solutol HS 15, and 85% sterile water) |
| Result: | Showed the ability to permeate the blood-brain barrier and to accumulate in the brain. |
[1]. Mastromarino M, et al. Design, Synthesis, Biological Evaluation, and Computational Studies of Novel Ureidopropanamides as Formyl Peptide Receptor 2 (FPR2) Agonists to Target the Resolution of Inflammation in Central Nervous System Disorders. J Med Chem. 2022; 65(6):5004-5028.