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MedChemExpress - Model AF12198 - ...

MedChemExpress - Model AF12198 - 185413-30-3

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

MCE China：AF12198

Brand：MedChemExpress (MCE)

Cat. No.HY-P1110

CAS：185413-30-3

Purity：99.75%

Storage：Sealed storage, away from moisture and light, under nitrogen Powder -80°C 2 years -20°C 1 year *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

Shipping：Room temperature in continental US; may vary elsewhere.

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.

In Vitro：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].

In Vivo：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].

IC50 & Target：IL-6 IL-8 IL1R1 8 nM (IC50)

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

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 [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]

Brand introduction:
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•   The biological activity of the products has been verified by the experiments of customers in various countries；
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