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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].

NLRP3; NLRP3 inflammasome

[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