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Synonyms | N/A | Storage (From the date of receipt) |
2 years -80°C liquid | |
化学式 | C12H13ClO2 |
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分子量 | 224.68 | CAS No. | 866028-26-4 | |
Solubility (25°C)* | 体外 | |||
* <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. |
製品説明 | 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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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]. | |||||
密度 | 1.1 g/mL |
細胞アッセイ | 細胞株 | THP-1 cells |
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濃度 | 0.1−100 μM | |
反応時間 | 72 h | |
実験の流れ | 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 |
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動物実験 | 動物モデル | Male Sprague−Dawley rats |
投薬量 | 12.5, 25.0, 50.0 mg/kg/day | |
投与方法 | oral administration |
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]
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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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