NLRP3i

NLRP3i is an intermediate in the synthesis of glyburide (Item No. 15009) and an inhibitor of the NOD-, LRR-, and pyrin domain-containing protein 3 (NLRP3) inflammasome.¹ It is selective for NLRP3 over NLRP4 and absent in melanoma 2 (AIM2) inflammasomes at 400 µM. NLRPi inhibits LPS-induced IL-1β release and apoptosis-associated speck-like protein containing a CARD (ASC) oligomerization in J774A.1 mouse macrophages. In vivo, NLRP3i (100 mg/kg) reduces infarct size and cardiac levels of troponin I in a mouse model of acute myocardial infarction. It reduces peritoneal leukocyte infiltration in a mouse model of peritonitis induced by zymosan A (Item No. 21175) in a dose-dependent manner. NLRP3i (100 mg/kg) also decreases plasma IL-18 levels and reduces systolic and diastolic dysfunction in a mouse model of Western diet-induced obesity.²

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1. Marchetti, C., Chojnacki, J., Toldo, S., et al. A novel pharmacologic inhibitor of the NLRP3 inflammasome limits myocardial injury following ischemia-reperfusion in the mouse. J. Cardiovasc. Pharmacol. 63(4), 316-322 (2015).

2. Carbone, S., Mauro, A.G., Prestamburgo, A., et al. An orally available NLRP3 inflammasome inhibitor prevents western diet-induced cardiac dysfunction in mice. J. Cardiovasc. Pharmacol. 72(6), 303-307 (2018).