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检测方案
≥98% (HPLC)
形式
oil
颜色
colorless to light brown
储存温度
−20°C
SMILES字符串
ClC1=C(CC(C(OCC)=O)=C)C=CC=C1
生化/生理作用
INF39是一种口服活性丙烯酸酯衍生物以及无细胞毒性的INF4E类似物（在THP-1培养物中100 μM时无毒性，而INF4E在TC50 = 65 μM时无毒），它是针对NLRP3（含NACHT、LRR和PYD结构域蛋白3）ATP酶活性的一种不可逆抑制剂（100 μM INF39在15分钟内抑制52％；105 ng人类NLP3 & 250 μM ATP）对于NLRP3炎症小体组装和激活至关重要。INF39可有效降低培养中的鼠骨髓源性巨噬细胞中5 mM（30分钟）的ATP诱导的白介素1β（IL-1β）的释放和细胞焦亡（在对LPS引发的BMDM进行10 μM INF39的1小时处理后可分别降低55-58％和43-65％）并在2,4-二硝基苯磺酸（DNBS）诱导的结肠炎大鼠体内模型中减轻肠道相关的炎症（在0.2 mL橄榄油中12.5-50 mg/kg /天） 。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Mattia Cocco et al.
Journal of medicinal chemistry, 60(9), 3656-3671 (2017-04-15)
Pharmacological inhibition of NLRP3 inflammasome activation may offer a new option in the treatment of inflammatory bowel disease. In this work, we report the design, synthesis, and biological screening of a series of acrylate derivatives as NLRP3 inhibitors. The in
Design, Synthesis, and Evaluation of Acrylamide Derivatives as Direct NLRP3 Inflammasome Inhibitors.
Mattia Cocco et al.
ChemMedChem, 11(16), 1790-1803 (2016-03-19)
NLRP3 inflammasome plays a key role in the intracellular activation of caspase-1, processing of pro-inflammatory interleukin-1β (IL-1β), and pyroptotic cell death cascade. The overactivation of NLRP3 is implicated in the pathogenesis of autoinflammatory diseases, known as cryopyrin-associated periodic syndromes (CAPS)
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