INF39

Catalog No.S8559

INF39 Chemical Structure

Molecular Weight(MW): 224.68

INF39 is a nontoxic, irreversible NLRP3 inhibitor that counteracts NLRP3 activation through direct irreversible interaction with NLRP3 and partial inhibition of LPS-driven pro-inflammatory gene expression.

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Biological Activity

Description INF39 is a nontoxic, irreversible NLRP3 inhibitor that counteracts NLRP3 activation through direct irreversible interaction with NLRP3 and partial inhibition of LPS-driven pro-inflammatory gene expression.
Targets
NLRP3 [1]
(Cell-free assay)
In vitro

INF39 inhibits NLRP3 ATPase in a concentration-dependent manner and prevents pyroptosis of THP-1 cells. It is able to efficiently inhibit NLRP3-dependent IL-1β release and reduce caspase-1 activation and pyroptosis (measured as extracellular LDH) in macrophages (BMDMs)[1].

In vivo Oral Administration of INF39 reduces systemic and colonic inflammation in rats treated with 2,4-Dinitrobenzenesulfonic acid. Rats treated with INF39 display a significant reduction of macroscopic damage score. Oral administration of INF39 reduces colonic myeloperoxidase, IL-1β, and TNF Levels in DNBS-treated rats. INF39 can exert beneficial effects on colitis, by reducing MPO, IL-1β, and TNF pro inflammatory cytokine levels in colonic tissues from inflamed rats, thus suggesting that the blockade of NLPR3 activation could represent a suitable pharmacological target for the management of intestinal inflammation. INF39, following oral administration, is stable and is absorbed into the intestinal epithelium, where it can act locally and generate the nontoxic metabolites[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: THP-1 cells
  • Concentrations: 0.1−100 μM
  • Incubation Time: 72 h
  • Method:

    Human THP-1 cells were exposed to increasing concentrations of the synthesized compounds (0.1−100 μM, 72 h), and then cell viability was evaluated by the MTT assay


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Male Sprague−Dawley rats
  • Formulation: olive oil
  • Dosages: 12.5, 25.0, 50.0 mg/kg/day
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

Chemical Information

Molecular Weight 224.68
Formula

C12H13ClO2

CAS No. 866028-26-4
Storage powder
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID