iNOs-IN-3

• 常用名: iNOs-IN-3
• 英文名: iNOs-IN-3
• CAS号: 2241674-94-0
• 分子量: 488.55
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₇H₂₄N₂O₅S
• 熔点: N/A
• 闪点: N/A

iNOs-IN-3用途

iNOs-IN-3(化合物2d)是一种口服活性一氧化氮合酶(iNOs)抑制剂(IC50=3.342µM)。iNOs-IN-3具有抗炎活性,可用于LPS诱导的急性肺损伤(ALI)研究[1]。

iNOs-IN-3名称

• 英文名: iNOs-IN-3

iNOs-IN-3生物活性

• 描述: iNOs-IN-3(化合物2d)是一种口服活性一氧化氮合酶(iNOs)抑制剂(IC50=3.342µM)。iNOs-IN-3具有抗炎活性,可用于LPS诱导的急性肺损伤(ALI)研究[1]。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 炎症/免疫
• 靶点实验:

  IC50: 3.342 µM (iNOS)[1]

• 体外研究: iNOs-IN-3(25μM；24小时)抑制LPS诱导的RAW 264.7细胞[1]。iNOs-IN-3(12.5μM；24小时)可降低iNOs的表达[1]。细胞活力测定[1]细胞系：RAW 264.7显微照片浓度：25μM孵育时间：24小时结果：在LPS诱导的RAW 264.7细胞中显示出较高的抑制活性(IC50=14.72μM)。细胞存活率测定[1]细胞系：RAW 264.7显微照片浓度：12.5μM孵育时间：24小时结果：明显抑制LPS诱导的iNOS mRNA表达。细胞活力测定[1]细胞系：RAW 264.7显微图像浓度：12.5μM孵育时间：24小时结果：在12.5µM时抑制TNF-α、IL-6和IL-1β的表达。
• 体内研究: iNOs-IN-3(口服给药；12.5 mg/kg；一次)治疗显示了对二甲苯诱导的小鼠耳水肿的抗炎活性[1]。iNOs-IN-3(口服给药；3.125 mg/kg、6.25 mg/kg和12.5 mg/kg；一次)可预防LPS诱导的急性肺损伤[1]。动物模型：二甲苯诱导小鼠[1]剂量：12.5mg/kg给药：口服给药；12.5mg/kg；一次结果：显示出比阳性对照更好的活性。动物模型：LPS诱导的急性肺损伤(ALI)小鼠[1]剂量：3.125mg/kg、6.25mg/kg、12.5mg/kg给药：口服给药；3.125 mg/kg、6.25 mg/kg和12.5 mg/kg；一次结果：剂量依赖性地减轻病理损伤,如减少炎症浸润和肺充血。剂量依赖性地抑制LPS诱导的肺水肿。
• 参考文献:

  [1]. Li Tang, et al. Design and synthesis of new disubstituted benzoxazolone derivatives that act as iNOS inhibitors with potent anti-inflammatory activity against LPS-induced acute lung injury (ALI). Bioorg Med Chem. 2020 Nov 1;28(21):115733.

iNOs-IN-3物理化学性质

• 分子式: C₂₇H₂₄N₂O₅S
• 分子量: 488.55

iNOs-IN-3靶点实验

查看更多实验

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实验名称：Anti-inflammatory activity against LPS-induced ALI Kunming mouse model assessed as re... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4672108

实验名称：Anti-inflammatory activity against LPS-induced ALI Kunming mouse model assessed as re... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4672111

实验名称：Anti-inflammatory activity against LPS-induced ALI Kunming mouse model assessed as re... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4672110

实验名称：Cytotoxicity against mouse RAW 264.7 cells assessed as reduction in cell proliferatio... 来源：ChEMBL 靶标：RAW264.7 External Id：CHEMBL4672123

实验名称：Inhibition of iNOS in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitr... 来源：ChEMBL 靶标：Nitric oxide synthase, inducible External Id：CHEMBL4672122

实验名称：Anti-inflammatory activity against LPS-induced ALI Kunming mouse model assessed as re... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4672113

实验名称：Anti-inflammatory activity against LPS-induced ALI Kunming mouse model assessed as re... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4672112

实验名称：Anti-inflammatory activity in Kunming mouse assessed as inhibition of xylene-induced ... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4672115

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