NLRP3-IN-91
NLRP3-IN-91 is a potent NLRP3 inflammasome inhibitor with a Kd of 558.4 nM. NLRP3-IN-91 directly targets the NLRP3 NACHT domain, blocks inflammasome assembly and activation, and exerts anti-inflammatory effects. NLRP3-IN-91 increases survival time in a murine model of LPS (HY-D1056)-induced sepsis. NLRP3-IN-91 can be used for the research of sepsis.
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。
- 分子式: C27H27ClFN3O6S
- 分子量:576.04
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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
- 純度とドキュメンテーション
- 参考文献
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生物活性
製品説明
IC50 & Target
[1]|
NLRP3 inflammasome 558.4 nM (Kd) |
IL-1β 0.094 μM (IC50) |
Caspase-1 |
体外実験
NLRP3-IN-91 (compound D12) (0.04-10 μM; 30 min) potently inhibits NLRP3 inflammasome-mediated IL-1β secretion in J774A.1 murine macrophages with an IC50 of 0.094 μM[1].
NLRP3-IN-91 (24 h) shows low cytotoxicity in vitro, with CC50 values >30 μM in J774A.1 murine macrophages and >100 μM in AML-12 mouse normal hepatocytes[1].
NLRP3-IN-91 (0.2-5 μM; 2.5 h) dose-dependently inhibits NLRP3 inflammasome assembly and activation in J774A.1 murine macrophages by reducing cleaved caspase-1 (p20) and mature IL-1β production[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:J774A.1 murine macrophages
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Concentration:0.04, 0.12, 0.37, 1.11, 3.33, 10 μM
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Incubation Time:30 min
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Result:Inhibited IL-1β secretion by 80.2% at 1 μM.
Inhibited IL-1β secretion by 96.6% at 10 μM.
Exhibited an IC50 of 0.094 μM for NLRP3 inflammasome-mediated IL-1β release.
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Cell Line:J774A.1 murine macrophages
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Concentration:0.2, 1, and
5 μM -
Incubation Time:2.5 h
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Result:Suppressed the production of cleaved caspase-1 (p20 subunit) and mature IL-1β in a dose-dependent manner.
Did not affect levels of pro-caspase-1, pro-IL-1β, NLRP3, or GAPDH.
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:Male C57BL/6 mice (8 weeks old, 20-25 g) intraperitoneally injected with LPS (40 mg/kg)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose; 1 hour pre-LPS
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Result:Exceeded 40% survival rate at 72 hours post-LPS challenge.
化学情報
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分子量 576.04
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分子式 C27H27ClFN3O6S
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SMILES
O=C(N(CC1=CC(Cl)=CC=C1OCCOC)C2=NC3=CC(NS(=O)(CC)=O)=CC=C3O2)CC4=CC=C(F)C=C4
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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-91 関連分類
HY-183296 関連分類
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