Uses
Ac2-12, an annexin/lipocortin 1 (LC1)-mimetic peptide, inhibit neutrophil extravasation. Ac2-12 has antimigratory action and inhibits recruitment of neutrophils in experimental inflammation models[1][2].
Enzyme inhibitor
This annexin/lipocortin-1 peptidomimetic (FW = 1351.58 g/mol; Sequence: Acetyl-AMVSEFLKQAW; CAS 256447-08-2; Soluble to 1 mg/mL in 20% (vol/vol) acetonitrile-H2O) markedly reduces the degree of neutrophil adhesion and emigration across mouse mesenteric postcapillary venules, when administered at 13 mg/kg (s.c.), but does not modify cell rolling, when assessed directly by intravital microscopy. Ac2-12 also promotes neutrophil detachment from mesenteric endothelium after activation by intraperitoneal injection of 1 mg zymosan in mice (i.e., zymosan peritonitis). Ac2-12 phenocopies the effects observed in FormylatedPeptide Receptor (FPR) knock-out mice.
in vivo
Ac2-12 (i.v.; 6.7 mg/kg, ≈70 nmol per mouse), was found to mimic the actions of lipocortin 1 (LC1) and Ac2-26 in male Swiss Albino mice (10-15 g)[1].
Ac2-12 (100 μg) significantly reduces polymorphonuclear leukocyte (PMN) influx in wild-type C57BL/6 mice and is no longer active in FPR KO mice[2].
References
[1] L H Lim, et al. Promoting detachment of neutrophils adherent to murine postcapillary venules to control inflammation: effect of lipocortin 1. Proc Natl Acad Sci U S A. 1998 Nov 24;95(24):14535-9. DOI:
10.1073/pnas.95.24.14535[2] M Perretti, et al. Involvement of the receptor for formylated peptides in the in vivo anti-migratory actions of annexin 1 and its mimetics. Am J Pathol. 2001 Jun;158(6):1969-73. DOI:
10.1016/S0002-9440(10)64667-6
