耗材描述
AF12198
产品活性:AF12198 是针对人类I型白介素-1 受体 (IL1R1) (IC50=8 nM) 的有效,选择性和特异性肽拮抗剂,但不是针对人类 II 型受体 (IC50=6.7 µM) 或鼠 I 型受体 (IC50>200 µM)。AF12198 抑制 IL-1 诱导的 IL-8 产生 (IC50=25 nM) 和 IL-1诱导的细胞间粘附分子 1 (ICAM-1) 表达 (IC50=9 nM)。AF12198 具有抗炎活性,并在体内阻断了对 IL-1 的反应。
产品来源: https://www.medchemexpress.cn/af12198.html
研究领域:Immunology/Inflammation
作用靶点:Interleukin Related
In Vitro: AF12198 competes for binding of?125I-IL-1α with an IC50?of 8.0 nM, nearly equal to that of IL-1ra, IC50 of 4.0 nM for the type I receptor.AF12198 (0-5 ng; 8 hours)? inhibits IL-6 induction with an IC50 of 15 μM whereas IL-1ra inhibits with an IC50?of 2 nM?in heparinized human?primate blood. Meanwhile, With blood from cynomolgus monkeys, the IC50?values are 17 μM for AF12198 and 30 nM for IL-1ra. Additionally, AF12198 or IL-1RA alone does not induce IL-6 in blood from either humans or cynomolgus monkeys.
In Vivo: AF12198 (intravenous infusion; 16?mg/kg; 30?min before LPS intravenous injection) significantly attenuates the increase in lung MPO activity induced by LPS in acute lung inflammation and it reduces the lung microvascular leakage from rats inflamed with LPS at the 4?h (32.6%), 12?h (50.1%) and 24?h (65.3%) after LPS.
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