Cat#：166P01
序列（三字母）：Ac-Phe-Glu-Trp-Thr-Pro-Gly-Trp-Tyr-Gln-L-azetidine-2-carbonyl-Tyr-Ala-Leu-Pro-Leu-NH₂
序列（单字母）：Ac-FEWTPGWYQ-Aze-YALPL-NH₂
类似名：AF12198
分子式：C₉₆H₁₂₃N₁₉O₂₂
分子量：1895.15
CAS#：185413-30-3
合成方法：Synthetic
存储条件：-20 ± 5 °C
应用：Cytokines/Chemokines & their Receptors
描述：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.