INF39

Catalog No.S8559 Batch:S855901

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Technical Data

Formula

C12H13ClO2

Molecular Weight 224.68 CAS No. 866028-26-4
Solubility (25°C)* In vitro
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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]
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].
Density 1.1 g/mL

Protocol (from reference)

Cell Assay:

[1]

  • 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

Animal Study:

[1]

  • Animal Models

    Male Sprague−Dawley rats

  • Dosages

    12.5, 25.0, 50.0 mg/kg/day

  • Administration

    oral administration

Customer Product Validation

Data from [Data independently produced by , , Front Pharmacol, 2017, 8:944]

Data from [Data independently produced by , , Biomed Res Int, 2018, doi:10.1155/2018/1294951]

Selleck's INF39 has been cited by 8 publications

A new cell death program regulated by toll-like receptor 9 through p38 mitogen-activated protein kinase signaling pathway in a neonatal rat model with sepsis associated encephalopathy [ Chin Med J (Engl), 2022, 135(12):1474-1485] PubMed: 35261352
A Novel Inhibitor INF 39 Promotes Osteogenesis via Blocking the NLRP3/IL-1β Axis [ Biomed Res Int, 2022, 2022:7250578] PubMed: 35872849
NLRP3 inflammasome inhibitor INF39 attenuated NLRP3 assembly in macrophages [ Int Immunopharmacol, 2021, 92:107358] PubMed: 33508701
TRIM31 inhibits NLRP3 inflammasome and pyroptosis of retinal pigment epithelial cells through ubiquitination of NLRP3 [ Cell Biol Int, 2020, 10.1002/cbin.11429] PubMed: 32716108
Astragaloside IV Suppresses High Glucose-Induced NLRP3 Inflammasome Activation by Inhibiting TLR4/NF-κB and CaSR. [ Mediators Inflamm, 2019, 2019:1082497] PubMed: 30906223
NLRP3 Deficiency Alleviates Severe Acute Pancreatitis and Pancreatitis-Associated Lung Injury in a Mouse Model. [ Biomed Res Int, 2018, 2018:1294951] PubMed: 30622955
NLRP3 Deficiency Alleviates Severe Acute Pancreatitis and Pancreatitis-Associated Lung Injury in a Mouse Model [Qiang Fu, et al. Biomed Res Int, 2018, 10.1155/2018/1294951]
Yupingfeng San Inhibits NLRP3 Inflammasome to Attenuate the Inflammatory Response in Asthma Mice [Liu X, et al. Front Pharmacol, 2017, 8:944] PubMed: 29311942

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.