An NLRP3 inflammasome inhibitor; inhibits the release of IL-1β and decreases caspase-1 levels in LPS-stimulated J774A.1 murine macrophages

Dapansutrile – 250 mg

Brand:
Cayman
CAS:
54863-37-5
Storage:
-20
UN-No:
Non-Hazardous - /

Dapansutrile is a β-sulfonyl nitrile inhibitor of the NLRP3 inflammasome that inhibits the release of IL-1β 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-α release.{40704} It is selective for NLRP3 over NLRP4 and AIM2 inflammasomes at concentrations up to 100 μM. 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-1β 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, α-ketoglutarate, and citrate levels, markers of oxidative metabolism, in muscle in a mouse model of LPS-induced systemic inflammation. Dapansutrile also reduces IL-1β 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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Description

An NLRP3 inflammasome inhibitor; inhibits the release of IL-1β and decreases caspase-1 levels in LPS-stimulated J774A.1 murine macrophages, HMDMs, and primary human blood neutrophils; selective for NLRP3 over NLRP4 and AIM2 inflammasomes at concentrations up to 100 μM; inhibits ASC oligomerization and NLRP3 association with caspase-1 and ASC in LPS- and nigericin-stimulated J774A.1 cells; reduces MPO, CXCL1, and IL-6 levels in peritoneal fluid as well as IL-1β levels in liver, lung, spleen, and skeletal muscle in a mouse model of LPS-induced systemic inflammation; increases markers of oxidative metabolism in muscle in mouse model of LPS-induced systemic inflammation; reduces IL-1β release in blood monocytes isolated from patients with CAPS

Formal name: 3-(methylsulfonyl)-propanenitrile

Synonyms:  3-methanesulfonyl Propanenitrile

Molecular weight: 133.2

CAS: 54863-37-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Immunology & Inflammation|Autoimmunity||Research Area|Immunology & Inflammation|Innate Immunity

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