INF39 is a nontoxic, irreversible NLRP3 inhibitor able to decrease interleukin-1β release from macrophages. INF39 (INF39) significantly inhibits ATP- and nigericin-induced IL-1β release. INF39 potentially reacts with Cys-SH residues in the active site of cysteine protease caspase-1, but does not directly target caspase-1 activity. The inhibition of NLRP3 inflammasome complex with INF39 dose-dependently attenuates the decrease in colonic length (-19, -13 and -8% at 12.5, 25, 50 mg/kg, respectively). Rats treated with INF39 displays a significant reduction of macroscopic damage score (4.7 at 12.5 mg/kg, 3.1 at 25 mg/kg, and 2.8 at 50 mg/kg). Oral administration of INF39 reduces colonic myeloperoxidase, IL-1β, and TNF Levels in DNBS-treated rats.
<span style='color:#ff0000;'><strong>*The compound is unstable in solutions, freshly prepared is recommended</strong></span>
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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