1. Immunology/Inflammation
  2. Interleukin Related
  3. AF12198

AF12198 

Cat. No.: HY-P1110
Handling Instructions

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.

For research use only. We do not sell to patients.

AF12198 Chemical Structure

AF12198 Chemical Structure

CAS No. : 185413-30-3

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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].

IC50 & Target[1]

IL1R1

8 mM (IC50)

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].

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

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].

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

Animal Model: Male Wistar rats[2]
Dosage: 16 mg/kg
Administration: Intravenous infusion; 30 min before LPS intravenous injection
Result: Decreased pulmonary microvascular leakage in rats.
Molecular Weight

1895.12

Formula

C₉₆H₁₂₃N₁₉O₂₂

CAS No.

185413-30-3

Sequence

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

Sequence Shortening

Ac-FEWTPGWYQ-{Aze}-YALPL-NH2

SMILES

[Ac-FEWTPGWYQ-{Aze}-YALPL-NH2]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

AF12198AF 12198AF-12198Interleukin RelatedILco-adjuvant therapytracheainflammationlung permeabilitybronchoalveolar lavageinterleukin-1βInhibitorinhibitorinhibit

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