NLRP3-IN-17 is a potent, selective and orally active NLRP3 inflammasome inhibitor with an IC50 value of 7 nM. NLRP3-IN-17 significantly inhibits NLRP3 dependent IL-1β secretion in mice and can be used for chronic inflammatory diseases research[1].
in vivo
NLRP3-IN-17 (compound 15) (3 mg/kg; po) displays desired PK profile, the AUC, t and F% values are 4.2 μg.h/mL, 2.91 h, and 56%, respectively[1].
NLRP3-IN-17 (10 mg/kg; po; single dosage) significantly inhibit NLRP3 dependent IL-1β secretion in acute in vivo LPS+ATP
challenged model in female C57BL/6 mice, it decreases the IL-1β levels by 44%[1].
IC 50
NLRP3 inflammasome: 7 nM (IC50)
References
[1] Sameer Agarwal, et al. Discovery of N-Cyano-sulfoximineurea Derivatives as Potent and Orally Bioavailable NLRP3 Inflammasome Inhibitors. ACS Med Chem Lett. 2020 Feb 27;11(4):414-418. DOI:10.1021/acsmedchemlett.9b00433
