Home Immunology & Inflammation NLRP3 inhibitor INF39

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INF39 NLRP3 inhibitor

Cat.No.S8559

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.
INF39 NLRP3 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 224.68

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Chemical Information, Storage & Stability

Molecular Weight 224.68 Formula

C12H13ClO2

 Storage (From the date of receipt) 2 years -80°C liquid
CAS No. 866028-26-4 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCOC(=O)C(=C)CC1=CC=CC=C1Cl

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Mechanism of Action

Targets/IC50/Ki
NLRP3 [1]
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 this compound display a significant reduction of macroscopic damage score. Oral administration of this chemical reduces colonic myeloperoxidase, IL-1β, and TNF Levels in DNBS-treated rats. It 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. This compound, following oral administration, is stable and is absorbed into the intestinal epithelium, where it can act locally and generate the nontoxic metabolites[1].
References

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