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/Interleukins, Lymphokines and Related Peptides (7)
/Ac-Phe-Glu-Trp-Thr-Pro-Gly-Trp-Tyr-Gln-L-azetidine-2-carbonyl-Tyr-Ala-Leu-Pro-Leu-NH₂
Product details
Cat#：166P01
Three Letter Code: Ac-Phe-Glu-Trp-Thr-Pro-Gly-Trp-Tyr-Gln-L-azetidine-2-carbonyl-Tyr-Ala-Leu-Pro-Leu-NH₂
One Letter Code: Ac-FEWTPGWYQ-Aze-YALPL-NH₂
Synonyms: AF12198
Molecular Formula: C₉₆H₁₂₃N₁₉O₂₂
Relative Molecular Mass: 1895.15
CAS#: 185413-30-3
Source: Synthetic
Storage Conditions: -20 ± 5 °C
Areas of Interest: Cytokines/Chemokines & their Receptors
Details: AF12198 exhibited both in vitro and in vivo IL-1 antagonist activity. It selectively bound the human type I IL-1 receptor but not the human type II receptor or the murine type I receptor. In vitro, AF12198 inhibited IL-1-induced IL-8 production by human dermal fibroblasts with an IC₅₀ of 25 nM and IL-1-induced intercellular adhesion molecule-1 expression by endothelial cells with an IC₅₀ of 9 nM. In vivo it blocked ex-vivo IL-1 induction of IL-6 and down modulates in vivo induction of IL-6. This is the first small molecule which shows IL-1 receptor antagonist activity in vivo.
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