Biological ActivityAF 12198 is a potent and selective antagonist for the human type I interleukin-1 (IL-1) receptor (IC50 values are 8 nM, > 6.7 mM and > 200 mM for human type I, human type II and murine type I IL-1 receptors respectively). Blocks IL-1-induced expression of ICAM-1 and E-selectin in HUVECs and IL-1β induction of IL-8 in human dermal fibroblasts. Reduces IL-1β-induced IL-6 production and exhibits anti-inflammatory activity in vivo.
(Modifications: Phe-1 = N-terminal Ac, X - Aze, Leu-15 = C-terminal amide)
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Low level laser therapy (LLLT) decreases pulmonary microvascular leakage, neutrophil influx and IL-1β levels in airway and lung from rat subjected to LPS-induced inflammation.
Aimbire 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.
Akeson et al.
Citation for AF 12198
The citations listed below are publications that use Tocris products. Selected citations for AF 12198 include:
1 Citation: Showing 1 - 1
Interleukin-1β expression is required for lysophosphatidic Acid-induced lymphangiogenesis in human umbilical vein endothelial cells.
Authors: Lin Et al.
J Psychopharmacol 2010;2011:351010
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