NLRP3-IN-8
NLRP3-IN-8 (compound 27) is an orally active, directly binding NLRP3 inflammasome inhibitor with an IC50 value of 1.23 μM against IL-1 β. NLRP3-IN-8 has good metabolic stability to liver microsomes (t1/2 = 138.63 min), and has almost no toxicity (against L02: IC50 > 100 μM).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2768650-56-0
- 分子式: C23H20N2O6
- 分子量:420.41
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
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NLRP3 |
NLRP3 inflammasome |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L02 | IC50 |
>100 μM
Compound: 27
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Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
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[PMID: 35428012] |
体外実験
NLRP3-IN-8 (compound 27) exhibits prominent anti-inflammatory activity with an IC50 of 1.23 μM[1].
NLRP3-IN-8 exhibits good metabolic stability through human liver microsomes (t1/2 = 138.63 min)[1].
NLRP3-IN-8 (0-10 μM, 1 h) significantly inhibits pyrolysis rate in a concentration-dependent manner[1].
NLRP3-IN-8 only inhibits the activation of NLRP3 inflammasomes, and could inhibit the activation of inflammasome by a variety of inducer[1].
NLRP3-IN-8 blocks NLRP3-induced ASC oligomerization[1].
NLRP3-IN-8 inhibits NLRP3 inflammasome assembly by blocking the interaction of NLRP3-NEK7 and NLRP3-ASC[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BMDMs cells
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Concentration:0.5, 1, and 2 μM
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Incubation Time:30 min, pretreated with LPS (200 ng/mL) for 3 h
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Result:Dose-dependently blocked IL-1 b secretion and caspase-1 cleavage at concentrations of 0.5-2 μM. Inhibited the maturation of intracellular caspase-1 (p20), and did not affect the expression of other constituent proteins of NLRP3 inflammasome, such as pro-IL-1 β, pro-caspase-1 (p45), NLRP3, ASC and NEK7.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DSS-induced acute colitis model in C57BL/6 male mice[1].
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Dosage:20 mg/kg and 10 mg/kg dissolved in 0.5% sodium carboxymethyl cellulose aqueous solution.
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Administration:Intragastric administration, once a day, 7 days.
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Result:Reduced the weight loss during the onset of colitis in mice, and decreased the disease activity index (DAI) in a dose-dependent manner. Reduced colon shortening, pathological index score, the expression of TNF-a, IL-6 and IL-1 β in the tissues and inhibited the decrease of goblet cells.
化学情報
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CAS 番号 2768650-56-0
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分子量 420.41
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分子式 C23H20N2O6
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SMILES
COC1=CC(OC)=C(C(/C=C/C2=CC=C(C=C2)NC(C3=CC=CO3)=O)=C1)/C=C/[N+]([O-])=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
NLRP3-IN-8 関連分類
HY-146594 関連分類
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