Dapansutrile (OLT1177)

For research use only.

Catalog No.S8907

Dapansutrile (OLT1177) Chemical Structure

Molecular Weight(MW): 133.17

Dapansutrile (OLT1177) is a novel and selective NLRP3 inflammasome inhibitor.

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Biological Activity

Description Dapansutrile (OLT1177) is a novel and selective NLRP3 inflammasome inhibitor.
Targets
NLRP3 inflammasome [1]
()
In vitro

In vitro, nanomolar concentrations of OLT1177 reduces IL-1β and IL-18 release following canonical and noncanonical NLRP3 inflammasome activation. In LPS-stimulated human blood-derived macrophages, OLT1177 decreases IL-1β levels by 60% and IL-18 by 70% at concentrations 100-fold lower in vitro than plasma concentrations safely reached in humans. OLT1177 also reduces IL-1β release and caspase-1 activity in freshly obtained human blood neutrophils.In monocytes isolated from patients with cryopyrin-associated periodic syndrome (CAPS), OLT1177 inhibits LPS-induced IL-1β release by 84% and 36%. [2]

In vivo

Treatment of mice with OLT1177 limits MSU crystal articular inflammation (p > 0.0001), which is associated with decreased synovial IL-1β, IL-6, myeloperoxidase, and CXCL1 levels (p < 0.01) compared with vehicle-treated mice. Oral OLT1177 is highly effective in ameliorating reactive as well as gouty arthritis.[3]

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (750.91 mM)
Water 100 mg/mL (750.91 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 133.17
Formula

C4H7NO2S

CAS No. 54863-37-5
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID