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].

Product Specifications

CAS Number

[185413-30-3]

UNSPSC

12352209

Target

Interleukin Related

Type

Peptides

Related Pathways

Immunology/Inflammation

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/af12198.html

Purity

99.90

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(N1[C@@H](CCC1)C(NCC(N[C@H](C(N[C@H](C(N[C@@H](CCC(N)=O)C(N2[C@@H](CC2)C(N[C@H](C(N[C@@H](C)C(N[C@@H](CC(C)C)C(N3[C@@H](CCC3)C(N[C@H](C(N)=O)CC(C)C)=O)=O)=O)=O)CC4=CC=C(C=C4)O)=O)=O)=O)CC5=CC=C(C=C5)O)=O)CC6=CNC7=CC=CC=C67)=O)=O)[C@H]([C@H](O)C)NC([C@@H](NC([C@H](CCC(O)=O)NC([C@@H](NC(C)=O)CC8=CC=CC=C8)=O)=O)CC9=CNC%10=CC=CC=C9%10)=O

Molecular Formula

C96H123N19O22

Molecular Weight

1895.12

References & Citations

[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|[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.