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AF12198

Names

[ CAS No. ]:
185413-30-3

[ Name ]:
AF12198

[Synonym ]:
Ac-Phe-Glu-Trp-Thr-Pro-Gly-Trp-Tyr-Gln-L-azetidine-2-carbonyl-Tyr-Ala-Leu-Pro-Leu-NH2

Biological Activity

[Description]:

AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo[1].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Interleukin Related
Research Areas >> Inflammation/Immunology

[Target]

IC50: 8 nM (human IL1R1)[1]


[References]

[1]. F Aimbire, et al. Low level laser therapy (LLLT) decreases pulmonary microvascular leakage, neutrophil influx and IL-1beta levels in airway and lung from rat subjected to LPS-induced inflammation. Inflammation

[2]. A L Akeson, et al.AF12198, a novel low molecular weight antagonist, selectively binds the human type I interleukin (IL)-1 receptor and blocks in vivo responses to IL-1. J Biol Chem. 1996 Nov 29;271(48):30517-23.

Chemical & Physical Properties

[ Density]:
1.354 g/cm3

[ Molecular Formula ]:
C96H123N19O22

[ Molecular Weight ]:
1895.12000

[ Exact Mass ]:
1893.91000

[ PSA ]:
625.88000

[ LogP ]:
5.63910

MSDS