iNOs-IN-9
iNOs-IN-9 is a selective inducible nitric oxide synthase (iNOS) inhibitor with an IC50 of 82 nM against hiNOS. iNOs-IN-9 reduces cytokine-induced inflammatory responses and cell necrosis in inflammatory cell models. iNOs-IN-9 can be used for research related to psoriasis.
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: C16H13N5O3
- 分子量:323.31
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
iNOS 82 nM (IC50) |
体外実験
iNOs-IN-9 (Compound 10) (0.01-10 μM; 15 min preincubation, 30 min incubation at 37 °C) potently and selectively inhibits human iNOS with an IC50 of 82 nM, showing no significant inhibition of bovine eNOS at concentrations up to 10 μM and a selectivity ratio >116[1].
iNOs-IN-9 (10 μM; duration of cytokine stimulation) downregulates cytokine-induced inflammatory gene and membrane marker expression in primary human keratinocytes, with strong inhibitory effects on CXCL8, CCL2, CXCL10, ICAM-1, HLA-DR, and MHC class I[1].
iNOs-IN-9 (20 μM; 3 h) preserves histological integrity of healthy human skin explants and significantly reduces cytokine-induced inflammatory gene expression in this ex vivo model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HaCaT human keratinocytes (basal and pro-inflammatory conditions stimulated with TNF-α, IFN-γ, and IL-17)
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Concentration:0.1-100 μM
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Incubation Time:24 h, 48 h
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Result:Did not alter HaCaT cell metabolic activity at any tested concentration after 24 or 48 h under basal conditions.
Slightly but significantly restored cell metabolic activity at concentrations of 50 and 100 μM after 24 h, and at concentrations of 20, 50, and 100 μM after 48 h under pro-inflammatory conditions, compared to cytokine-stimulated controls.
Decreased nitric oxide release in cytokine-stimulated HaCaT cells after 24 h.
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:AB wild-type[1]
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Dosage:1 μM, 10 μM, 20 μM, 30 μM
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Administration:continuous immersion; duration dependent on exposure window (3-96 hpf or 48-120 hpf)
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Result:Resulted in 100% survival with very low malformation rates not statistically different from controls when administered at 10 μM and 20 μM during 48-120 hpf exposure window.
Caused significant mortality and sublethal effects when administered at 10 μM during 3-96 hpf exposure window.
Resulted in 100% mortality and severe malformations including pericardial edema, scoliosis, craniofacial defects, and yolk deformation when administered at 20 μM and 30 μM during 3-96 hpf exposure window.
化学情報
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分子量 323.31
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分子式 C16H13N5O3
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SMILES
O=C(NC1=CC2=C(N=C1)C=CC=C2)CNC3=NC=CC=C3[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)