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Description: Potent, selective human type I IL-1 receptor antagonist
Biological Activity for AF 12198
AF 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.
Technical Data for AF 12198
| M. Wt | 1895.14 |
| Formula | C96H123N19O22 |
| Sequence |
FEWTPGWYQXYALPL (Modifications: Phe-1 = N-terminal Ac, X - Aze, Leu-15 = C-terminal amide) |
| Storage | Desiccate at -20°C |
| CAS Number | 185413-30-3 |
| PubChem ID | 90488713 |
| InChI Key | VASLMBMCJADVGR-BRPRRQPRSA-N |
| Smiles | CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)C1CCN1C(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CC1=CNC2=C1C=CC=C2)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](CC1=CNC2=C1C=CC=C2)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC1=CC=CC=C1)NC(C)=O)[C@@H](C)O)C(N)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AF 12198
| Solubility | Soluble to 1 mg/ml in 10% ethanol/PBS |
Product Datasheets for AF 12198
References for AF 12198
References are publications that support the biological activity of the product.
Aimbire et al (2008) 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. Inflammation 31 189 PMID: 18421573
Akeson et al (1996) 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. 271 30517 PMID: 8940020
If you know of a relevant reference for AF 12198, please let us know.
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Keywords: AF 12198, AF 12198 supplier, Potent, selective, human, type, I, IL-1, receptors, antagonists, IL, Interleukins, Cytokines, AF12198, Cytokine, Receptors, 1793, Tocris Bioscience
1 Citation for AF 12198
Citations are publications that use Tocris products. Selected citations for AF 12198 include:
Lin et al (2010) Interleukin-1β expression is required for lysophosphatidic Acid-induced lymphangiogenesis in human umbilical vein endothelial cells. J Psychopharmacol 2011 351010 PMID: 21151531
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