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替诺福韦阿拉芬酰胺富马酸酯

替诺福韦阿拉芬酰胺富马酸酯,379270-38-9,结构式
替诺福韦阿拉芬酰胺富马酸酯
  • CAS号:379270-38-9
  • 英文名:Tenofovir alafenamide fumarate
  • 中文名:替诺福韦阿拉芬酰胺富马酸酯
  • CBNumber:CB02715632
  • 分子式:C25H33N6O9P
  • 分子量:592.55
  • MOL File:379270-38-9.mol
替诺福韦阿拉芬酰胺富马酸酯化学性质
  • 储存条件 :under inert gas (nitrogen or Argon) at 2-8°C
  • 溶解度 :DMSO:68.0(Max Conc. mg/mL);114.56(Max Conc. mM)
    Ethanol:100.0(Max Conc. mg/mL);168.48(Max Conc. mM)
    Water:17.5(Max Conc. mg/mL);29.48(Max Conc. mM)
  • 形态 :Powder

替诺福韦阿拉芬酰胺富马酸酯性质、用途与生产工艺

  • 生物活性 Tenofovir alafenamide fumarate (GS-7340 fumarate) 是 Tenofovir 的前体,Tenofovir 是一种 HIV-1 核苷酸逆转录酶抑制剂。
  • 靶点

    HIV-1, NRTIs

  • 体外研究

    Tenofovir alafenamide fumarate (GS-7340 fumarate) antiviral activities are similar across all cell types, ranging from 5 to 7 nM, while the CC 50 varies from 4.7 to 42 μM for MT-4 and MT-2 cells, respectively. The antiviral activity of TAF is evaluated against a panel of HIV-1 and HIV-2 isolates, including HIV-1 group M subtypes A to G, as well as group N and O isolates. Overall, for the 29 primary HIV-1 isolates tested in PBMCs, TAF EC 50 s range from 0.1 to 12 nM, with a mean EC 50 of 3.5 nM compared to a mean EC 50 of 11.8 nM for AZT, which is used as an internal control. For the HIV-2 isolates, the mean EC 50 s are 1.8 nM for TAF and 6.4 nM for AZT.

  • 体内研究

    Tenofovir alafenamide fumarate (GS-7340 fumarate) is an amidate prodrug of Tenofovir with good oral bioavailability and increases plasma stability compared to Tenofovir disoproxil fumarate (TDF).

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