OLT1177 (54863-37-5) is a potent and specific inhibitor of the NLRP3 inflammasome. It significantly decreased IL-1β and IL-18 levels in LPS-stimulated human blood-derived macrophages as well as IL-1β release and caspase 1 activity in human blood neutrophils with no effect on TNFα levels. Active in vivo in both mice and humans. Oral administration to 35 healthy human subjects resulted in no adverse effects.
1) Marchetti et al. (2018), OLT1177, a β-sulfonyl nitrile compound, safe in humans, inhibits the NLRP3 inflammasome and reverses the metabolic cost of inflammation; Proc. Natl. Acad. Sci. USA 115 E1530