AF 12198 - CAS 185413-30-3
Not Intended for Therapeutic Use. For research use only.
Category:
Inhibitor
Product Name:
AF 12198
Catalog Number:
185413-30-3
Synonyms:
Ac-Phe-Glu-Trp-Thr-Pro-Gly-Trp-Tyr-Gln-Aze-Tyr-Ala-Leu-Pro-Leu-NH2; AF-12198; AF12198
CAS Number:
185413-30-3
Description:
Potent, selective human type I IL-1 receptor antagonist
Molecular Weight:
1895.14
Molecular Formula:
C96H123N19O22
Quantity:
Milligrams-Grams
Quality Standard:
In-house
COA:
Inquire
MSDS:
Inquire
Canonical SMILES:
CC(C)CC(C(=O)N)NC(=O)C1CCCN1C(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CC2=CC=C(C=C2)O)NC(=O)C3CCN3C(=O)C(CCC(=O)N)NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(CC5=CNC6=CC=CC=C65)NC(=O)CNC(=O)C7CCCN7C(=O)C(C(C)O)NC(=O)C(CC8=CNC9=CC=CC=C98)NC(=O)C(CCC(=O)O)NC(=O)C(CC1=CC=CC=C1)NC
InChI:
1S/C96H123N19O22/c1-51(2)41-69(83(98)124)107-92(133)77-24-16-38-113(77)95(136)75(42-52(3)4)111-84(125)53(5)102-86(127)71(44-57-25-29-61(118)30-26-57)110-93(134)78-37-40-115(78)94(135)68(33-35-79(97)120)106-88(129)72(45-58-27-31-62(119)32-28-58)108-89(130)
InChIKey:
VASLMBMCJADVGR-XQDBXYBUSA-N
Targets:
Cytokine Receptor
Chemical Structure
CAS 185413-30-3 AF 12198

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Reference Reading


1.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.
Akeson AL1, Woods CW, Hsieh LC, Bohnke RA, Ackermann BL, Chan KY, Robinson JL, Yanofsky SD, Jacobs JW, Barrett RW, Bowlin TL. J Biol Chem. 1996 Nov 29;271(48):30517-23.
Interleukin-1 (IL-1) -alpha and -beta are potent regulators of inflammatory responses. The naturally occurring interleukin-1 receptor antagonist (IL-1ra) is effective in vitro and in vivo in modulating biological responses to IL-1. We have previously reported the discovery of IL-1 antagonist peptides from the search of phage display libraries. Further characterization of this group of peptides has led to a 15-mer, AF12198, Ac-FEWTPGWYQJYALPL-NH2 (J represents the unnatural amino acid, 2-azetidine-1-carboxylic acid), with both in vitro and in vivo IL-1 antagonist activity. AF12198 selectively binds the human type I IL-1 receptor but not the human type II receptor or the murine type I receptor. In vitro, AF12198 inhibits IL-1-induced IL-8 production by human dermal fibroblasts with a half-maximal inhibition concentration or IC50 of 25 nM and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression by endothelial cells with an IC50 of 9 nM.