AF 12198
Biological Activity
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
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 1 mg/ml in 10% ethanol/PBS |
Preparing Stock Solutions
The following data is based on the product molecular weight 1895.14. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.53 mL | 2.64 mL | 5.28 mL |
| 5 mM | 0.11 mL | 0.53 mL | 1.06 mL |
| 10 mM | 0.05 mL | 0.26 mL | 0.53 mL |
| 50 mM | 0.01 mL | 0.05 mL | 0.11 mL |
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References
References are publications that support the products' biological activity.
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, supplier, Potent, selective, human, type, I, IL-1, receptors, antagonists, IL, Interleukins, Cytokines, AF12198, Cytokine, Receptors, Cytokine, Receptors, 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
Do you know of a great paper that uses AF 12198 from Tocris? If so please let us know.
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