| Identification | Back Directory | [Name]
N-[4-[(1E)-2-[3,5-Dimethoxy-2-[(1E)-2-nitroethenyl]phenyl]ethenyl]phenyl]-2-furancarboxamide | [CAS]
2768650-56-0 | [Synonyms]
N-[4-[(1E)-2-[3,5-Dimethoxy-2-[(1E)-2-nitroethenyl]phenyl]ethenyl]phenyl]-2-furancarboxamide | [Molecular Formula]
C23H20N2O6 | [MOL File]
2768650-56-0.mol | [Molecular Weight]
420.42 |
| Chemical Properties | Back Directory | [Boiling point ]
565.8±50.0 °C(Predicted) | [density ]
1.315±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted) | [pka]
12.58±0.70(Predicted) |
| Hazard Information | Back Directory | [Uses]
NLRP3-IN-8 (compound 27) is an orally active, directly binding NLRP3 inflammasome inhibitor with an IC50 value of 1.23 μM against IL-1 β. NLRP3-IN-8 has good metabolic stability to liver microsomes (t1/2 = 138.63 min), and has almost no toxicity (against L02: IC50 > 100 μM)[1]. | [in vivo]
NLRP3-IN-8 (compound 27) (DSS-induced C57BL/6 male mice; 0-20 mg/kg; intragastric; once a day, 7 days) effectively alleviates the severity of DSS-induced colitis in mouse[1]. | Animal Model: | DSS-induced acute colitis model in C57BL/6 male mice[1]. | | Dosage: | 20 mg/kg and 10 mg/kg dissolved in 0.5% sodium carboxymethyl cellulose aqueous solution. | | Administration: | Intragastric administration, once a day, 7 days. | | Result: | Reduced the weight loss during the onset of colitis in mice, and decreased the disease activity index (DAI) in a dose-dependent manner. Reduced colon shortening, pathological index score, the expression of TNF-a, IL-6 and IL-1 β in the tissues and inhibited the decrease of goblet cells. |
| [IC 50]
NLRP3; NLRP3 inflammasome | [References]
[1] Xing Xing Zhang, et al. Discovery of 4-((E)-3,5-dimethoxy-2-((E)-2-nitrovinyl)styryl)aniline derivatives as potent and orally active NLRP3 inflammasome inhibitors for colitis. Eur J Med Chem. 2022 Apr 7;236:114357. DOI:10.1016/j.ejmech.2022.114357 |
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