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
颜色 :White to off-white

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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