FPR2 agonist 2

• CAT Number: I043884
• CAS Number: 2829263-20-7
• Molecular Formula: C25H20F2N4O2
• Molecular Weight: 446.45
• Purity: ≥95%
• Synonyms: 1-[(2S)-3-(4-cyanophenyl)-1-(5-fluoro-2,3-dihydroindol-1-yl)-1-oxopropan-2-yl]-3-(4-fluorophenyl)urea
• InChI: InChI=1S/C25H20F2N4O2/c26-19-5-8-21(9-6-19)29-25(33)30-22(13-16-1-3-17(15-28)4-2-16)24(32)31-12-11-18-14-20(27)7-10-23(18)31/h1-10,14,22H,11-13H2,(H2,29,30,33)/t22-/m0/s1
• InChIKey: KCNMTQVKKFREAN-QFIPXVFZSA-N
• SMILES: C1CN(C2=C1C=C(C=C2)F)C(=O)C(CC3=CC=C(C=C3)C#N)NC(=O)NC4=CC=C(C=C4)F

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].
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].

Reference

[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.
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