AF 12198 - CAS 185413-30-3
Catalog number: 185413-30-3
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Cytokine Receptor
Potent, selective human type I IL-1 receptor antagonist
Brife Description:
Potent, selective human type I IL-1 receptor antagonist
White lyophilised solid
Ac-Phe-Glu-Trp-Thr-Pro-Gly-Trp-Tyr-Gln-Aze-Tyr-Ala-Leu-Pro-Leu-NH2; AF-12198; AF12198
Soluble to 1 mg/ml in 10% ethanol/PBS
Desiccate at -20°C
Quality Standard:
Canonical SMILES:
1.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.
Akeson AL1, Woods CW, Hsieh LC, Bohnke RA, Ackermann BL, Chan KY, Robinson JL, Yanofsky SD, Jacobs JW, Barrett RW, Bowlin TL. J Biol Chem. 1996 Nov 29;271(48):30517-23.
Interleukin-1 (IL-1) -alpha and -beta are potent regulators of inflammatory responses. The naturally occurring interleukin-1 receptor antagonist (IL-1ra) is effective in vitro and in vivo in modulating biological responses to IL-1. We have previously reported the discovery of IL-1 antagonist peptides from the search of phage display libraries. Further characterization of this group of peptides has led to a 15-mer, AF12198, Ac-FEWTPGWYQJYALPL-NH2 (J represents the unnatural amino acid, 2-azetidine-1-carboxylic acid), with both in vitro and in vivo IL-1 antagonist activity. AF12198 selectively binds the human type I IL-1 receptor but not the human type II receptor or the murine type I receptor. In vitro, AF12198 inhibits IL-1-induced IL-8 production by human dermal fibroblasts with a half-maximal inhibition concentration or IC50 of 25 nM and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression by endothelial cells with an IC50 of 9 nM.
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CAS 185413-30-3 AF 12198

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