生物活性 靶点 体外研究 体内研究 2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)- 试剂级价格
ChemicalBook  CAS数据库列表  2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)-

2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)-

2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)-,1373765-19-5,结构式
2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)-
  • CAS号:1373765-19-5
  • 英文名:2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)-
  • 中文名:2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)-
  • CBNumber:CB12667396
  • 分子式:C23H27N5O2
  • 分子量:405.49
  • MOL File:1373765-19-5.mol
2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)-化学性质
  • 沸点 :702.0±70.0 °C(Predicted)
  • 密度 :1.32±0.1 g/cm3(Predicted)
  • 储存条件 :Store at -20°C
  • 溶解度 :DMSO:30.0(Max Conc. mg/mL);73.98(Max Conc. mM)
  • 形态 :A crystalline solid
  • 酸度系数(pKa) :16.94±0.30(Predicted)

2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)-性质、用途与生产工艺

  • 生物活性 IPSU是一种选择性,有口服活性和脑渗透性的OX2R拮抗剂,pKi值为7.85。
  • 靶点

    pKi: 7.85 (OX2R), 6.29 (OX1R)

  • 体外研究

    Orexin receptor antagonists represent attractive targets for the development of drugs for the treatment of insomnia. IPSU binds rapidly and reaches equilibrium very quickly in binding and/or functional assays.

  • 体内研究

    IPSU has low blood clearance, shows high maximal blood exposure and AUC after oral dosing. It exhibits an acceptable absolute oral bioavailability and a brain/blood concentration ratio that indicated favorable brain penetration. IPSU increases sleep when dosed during the mouse active phase (lights off); IPSU induces sleep primarily by increasing NREM sleep. IPSU shows a fast onset of action, with a clear increase in total sleep time during the first hour afterdosing. The effect lasts 4-5 h, after which time the total sleep time per hour is the same as on vehicle day .

2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)-上下游产品信息
上游原料
下游产品
2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)- 试剂级价格
  • 更新日期:2024/04/30
  • 产品编号:HY-13796
  • 产品名称:IPSU
  • CAS编号:
  • 包装:1 mg
  • 价格:420元
  • 更新日期:2024/04/30
  • 产品编号:HY-13796
  • 产品名称:2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)- IPSU
  • CAS编号:1373765-19-5
  • 包装:5mg
  • 价格:1100元
2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)-生产厂家
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