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INF39

Catalog No.
B8216
A nontoxic, irreversible NLRP3 inhibitor
Grouped product items
SizePriceStock Qty
2mg
$66.00
In stock
5mg
$128.00
In stock
25mg
$391.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

INF39 is a nontoxic, irreversible inhibitor of the nucleotide-binding oligomerization domain, leucine-rich repeat and pyrin domain containing protein 3 (NLRP3). NLRP3 is an intracellular sensor that detects a variety of endogenous danger signals, microbial motifs as well as environmental irritants, resulting in the formation and activation of the NLRP3 inflammasome. Assembly of the NLRP3 inflammasome leads to caspase 1-dependent release of pro-inflammatory cytokines (e.g. IL-1β and IL-18), as well as to gasdermin D-induced pyroptotic cell death. Pharmacological inhibition of NLRP3 inflammasome activation has been shown to offer a new option in the treatment of inflammatory bowel disease. 

References:

1. Cocco M, Pellegrini C, Martínez-Banaclocha H, et al. Development of an acrylate derivative targeting the NLRP3 inflammasome for the treatment of inflammatory bowel disease. Journal of Medicinal Chemistry, 2017, 60(9): 3656-3671.

2. Swanson KV, Deng M, Ting JP. The NLRP3 inflammasome: molecular activation and regulation to therapeutics. Nature Reviews Immunology, 2019, 19(8): 477-489.

Chemical Properties

StorageStore at -20°C
M.Wt224.68
Cas No.866028-26-4
FormulaC12H13ClO2
Solubility≥22.5 mg/mL in DMSO; ≥41.9 mg/mL in H2O; ≥47.9 mg/mL in EtOH
Chemical Nameethyl 2-(2-chlorobenzyl)acrylate
SDFDownload SDF
Canonical SMILESCCOC(C(CC1=CC=CC=C1Cl)=C)=O
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment:[1]

Cell lines

LPS-primed mouse bone marrow derived macrophages (BMDMs)

Reaction Conditions

10 or 100 μM INF39 for 1 h incubation

Applications

INF39 was able to significantly inhibit ATP- and nigericin-induced IL-1β release at 10 μM. Furthermore, INF39 reduced caspase-1 activation and pyroptosis in these macrophages.

Animal experiment:[1]

Animal models

Male Sprague-Dawley rats, 200 ~ 250 g

Dosage form

12.5, 25.0, 50.0 mg/kg

Once daily by intragastric route for 6 days

Applications

Oral administration of INF39 reduced systemic and colonic Inflammation in rats treated with 2,4-dinitrobenzenesulfonic acid (DNBS). Meanwhile, INF39 dose-dependently attenuated increment of spleen weight and decrease in colonic length caused by DNBS.

Note

The technical data provided above is for reference only.

References:

1. Cocco M, Pellegrini C, Martínez-Banaclocha H, et al. Development of an acrylate derivative targeting the NLRP3 inflammasome for the treatment of inflammatory bowel disease. Journal of Medicinal Chemistry, 2017, 60(9): 3656-3671.

2. Swanson KV, Deng M, Ting JP. The NLRP3 inflammasome: molecular activation and regulation to therapeutics. Nature Reviews Immunology, 2019, 19(8): 477-489.

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