Molecular Weight(MW): 224.68
INF39 is a nontoxic, irreversible NLRP3 inhibitor that counteracts NLRP3 activation through direct irreversible interaction with NLRP3 and partial inhibition of LPS-driven pro-inflammatory gene expression.
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|Description||INF39 is a nontoxic, irreversible NLRP3 inhibitor that counteracts NLRP3 activation through direct irreversible interaction with NLRP3 and partial inhibition of LPS-driven pro-inflammatory gene expression.|
INF39 inhibits NLRP3 ATPase in a concentration-dependent manner and prevents pyroptosis of THP-1 cells. It is able to efficiently inhibit NLRP3-dependent IL-1β release and reduce caspase-1 activation and pyroptosis (measured as extracellular LDH) in macrophages (BMDMs).
|In vivo||Oral Administration of INF39 reduces systemic and colonic inflammation in rats treated with 2,4-Dinitrobenzenesulfonic acid. Rats treated with INF39 display a significant reduction of macroscopic damage score. Oral administration of INF39 reduces colonic myeloperoxidase, IL-1β, and TNF Levels in DNBS-treated rats. INF39 can exert beneficial effects on colitis, by reducing MPO, IL-1β, and TNF pro inflammatory cytokine levels in colonic tissues from inflamed rats, thus suggesting that the blockade of NLPR3 activation could represent a suitable pharmacological target for the management of intestinal inflammation. INF39, following oral administration, is stable and is absorbed into the intestinal epithelium, where it can act locally and generate the nontoxic metabolites.|
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