推荐产品
方案
≥98% (HPLC)
表单
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
InChI
1S/C12H13ClO2/c1-3-15-12(14)9(2)8-10-6-4-5-7-11(10)13/h4-7H,2-3,8H2,1H3
InChI key
VTAOWWAFBSFWSG-UHFFFAOYSA-N
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) 。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
从最新的版本中选择一种:
Design, Synthesis, and Evaluation of Acrylamide Derivatives as Direct NLRP3 Inflammasome Inhibitors.
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)
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
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