AF12198 

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].

AF12198 competes for binding of ¹²⁵I-IL-1α with an IC₅₀ of 8.0 nM, nearly equal to that of IL-1ra, IC₅₀ of 4.0 nM for the type I receptor^[1].
AF12198 (0-5 ng; 8 hours) inhibits IL-6 induction with an IC₅₀ of 15 μM whereas IL-1ra inhibits with an IC₅₀ of 2 nM in heparinized human primate blood. Meanwhile, With blood from cynomolgus monkeys, the IC₅₀ values are 17 μM for AF12198 and 30 nM for IL-1ra. Additionally, AF12198 or IL-1RA alone does not induce IL-6 in blood from either humans or cynomolgus monkeys^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

AF12198 (intravenous infusion; 16 mg/kg; 30 min before LPS intravenous injection) significantly attenuates the increase in lung MPO activity induced by LPS in acute lung inflammation and it reduces the lung microvascular leakage from rats inflamed with LPS at the 4 h (32.6%), 12 h (50.1%) and 24 h (65.3%) after LPS^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1895.12

Solid

C₉₆H₁₂₃N₁₉O₂₂

185413-30-3

Ac-Phe-Glu-Trp-Thr-Pro-Gly-Trp-Tyr-Gln-{Aze}-Tyr-Ala-Leu-Pro-Leu-NH2

Ac-FEWTPGWYQ-{Aze}-YALPL-NH2

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light, under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

• [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  [Content Brief]

  [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.  [Content Brief]