IP7e

• 常用名: IP7e
• 英文名: IP7e
• CAS号: 500164-74-9
• 分子量: 390.43
• 密度: 1.2±0.1 g/cm3
• 沸点: 611.8±55.0 °C at 760 mmHg
• 分子式: C₂₃H₂₂N₂O₄
• 熔点: N/A
• 闪点: 323.8±31.5 °C

IP7e用途

IP7e是一种有效的脑渗透剂和口服活性Nurr1激活剂,EC50值为3.9 nM[1]。

IP7e名称

• 中文名: IP7e,Nurr1激活剂
• 英文名: IP7e

IP7e生物活性

• 描述: IP7e是一种有效的脑渗透剂和口服活性Nurr1激活剂,EC50值为3.9 nM[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:

  EC50: 3.9 nM (Nurr1)[1]

• 体内研究: IP7e(异恶唑基吡啶酮7e；10 mg/kg；口服灌胃；每天两次)预防性治疗可降低MS小鼠模型的发病率和严重程度,即实验性自身免疫性脑脊髓炎(EAE)。IP7e通过NF-kB通路依赖性过程减轻EAE小鼠脊髓的炎症和神经退行性变[2]。动物模型：患有实验性自身免疫性脑脊髓炎(EAE)的雌性C57BL/6J小鼠(6-8周龄)[2]。剂量：10mg/kg给药：灌胃；一天两次；预防性给药(发病前)从7天到23天,治疗性给药(发病后)从21天到36天。结果：预防性给药延迟了EAE的发病,降低了EAE的发病率和严重程度,并减少了经治疗的EAE小鼠脊髓的神经炎症和组织病理学改变。相反,EAE的病程不受治疗剂量的影响。
• 参考文献:

  [1]. Samuel Hintermann, et al. Identification of a series of highly potent activators of the Nurr1 signaling pathway. Bioorg Med Chem Lett. 2007 Jan 1;17(1):193-6.

  [2]. Francesca Montarolo, et al. Effects of isoxazolo-pyridinone 7e, a potent activator of the Nurr1 signaling pathway, on experimental autoimmune encephalomyelitis in mice. PLoS One. 2014 Sep 29;9(9):e108791.

IP7e物理化学性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 611.8±55.0 °C at 760 mmHg
• 分子式: C₂₃H₂₂N₂O₄
• 分子量: 390.43
• 闪点: 323.8±31.5 °C
• 精确质量: 390.157959
• LogP: 2.61
• InChIKey: YCAACZFPADQMAR-UHFFFAOYSA-N
• SMILES: COCCOCc1ccc(-c2cc3onc(-c4ccccc4)c3c(=O)n2C)cc1
• 蒸汽压: 0.0±1.8 mmHg at 25°C
• 折射率: 1.593
• 储存条件: -20°C

IP7e靶点实验

查看更多实验

实验名称：Cytotoxicity in human HEK293T cells assessed as reduction in cell viability at 0.01 t... 来源：ChEMBL 靶标：HEK-293T External Id：CHEMBL5030678

实验名称：Cytotoxicity in rat PC-12 cells assessed as reduction in cell viability at 0.01 to 10... 来源：ChEMBL 靶标：PC-12 External Id：CHEMBL5030677

实验名称：Cytotoxicity in human SKNBE2 cells assessed as reduction in cell viability at 0.01 to... 来源：ChEMBL 靶标：SK-N-BE(2) External Id：CHEMBL5030676

实验名称：Modulation of full length human Nurr1 expressed in PC12 cells co-transfected with RXR... 来源：ChEMBL 靶标：Nuclear receptor subfamily 4 group A member 2 External Id：CHEMBL5030778

实验名称：Modulation of full length human Nurr1 expressed in SKNBE(2) cells co-transfected with... 来源：ChEMBL 靶标：Nuclear receptor subfamily 4 group A member 2 External Id：CHEMBL5030702

实验名称：Modulation of full length human Nurr1 expressed in SKNBE(2) cells co-transfected with... 来源：ChEMBL 靶标：Nuclear receptor subfamily 4 group A member 2 External Id：CHEMBL5030701

实验名称：Modulation of full length human Nurr1 expressed in HEK293T cells co-transfected with ... 来源：ChEMBL 靶标：Nuclear receptor subfamily 4 group A member 2 External Id：CHEMBL5030700

实验名称：Modulation of full length human Nurr1 expressed in HEK293T cells co-transfected with ... 来源：ChEMBL 靶标：Nuclear receptor subfamily 4 group A member 2 External Id：CHEMBL5030699

实验名称：Modulation of full length human Nurr1 expressed in HEK293T cells co-transfected with ... 来源：ChEMBL 靶标：Nuclear receptor subfamily 4 group A member 2 External Id：CHEMBL5030706

实验名称：Modulation of full length human Nurr1 expressed in HEK293T cells co-transfected with ... 来源：ChEMBL 靶标：Nuclear receptor subfamily 4 group A member 2 External Id：CHEMBL5030705

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IP7e英文别名

• 6-{4-[(2-Methoxyethoxy)methyl]phenyl}-5-methyl-3-phenyl[1,2]oxazolo[4,5-c]pyridin-4(5H)-one
• IP7e
• MFCD30182349