Dapansutrile

Dapansutrile

CAT N°: 24671
Price:

From 55.00 46.75

Dapansutrile is a ?-sulfonyl nitrile inhibitor of the NLRP3 inflammasome that inhibits the release of IL-1? and decreases caspase-1 levels in LPS-stimulated J774A.1 murine macrophages, human monocyte derived macrophages (HMDMs), and primary human blood neutrophils without affecting TNF-? release.{40704} It is selective for NLRP3 over NLRP4 and AIM2 inflammasomes at concentrations up to 100 ?M. Dapansutrile inhibits ASC oligomerization and NLRP3 association with caspase-1 and ASC in LPS- and nigericin-stimulated J774A.1 cells. In vivo, Dapansutrile reduces myeloperoxidase (MPO), CXCL1, and IL-6 levels in peritoneal fluid as well as IL-1? levels in liver, lung, spleen, and skeletal muscle in a mouse model of LPS-induced systemic inflammation. It decreases oxidized glutathione and oxaloacetate and increases reduced glutathione, ?-ketoglutarate, and citrate levels, markers of oxidative metabolism, in muscle in a mouse model of LPS-induced systemic inflammation. Dapansutrile also reduces IL-1? release in blood monocytes isolated from patients with cryopyrin-associated periodic syndrome (CAPS), an autoinflammatory disorder characterized by gain-of-function mutations in NLRP3.

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