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 性质
| 储存条件 | under inert gas (nitrogen or Argon) at 2-8°C |
|---|---|
| 溶解度 | DMSO:68.0(最大浓度 mg/mL);114.56(最大浓度 mM) 乙醇:100.0(最大浓度 mg/mL);168.48(最大浓度 mM) 水:17.5(最大浓度 mg/mL);29.48(最大浓度 mM) |
| 形态 | 粉末 |
| 颜色 | 白色至米白色 |
| InChIKey | MEJAFWXKUKMUIR-GQDWUREHNA-N |
| SMILES | C(/C(=O)O)=C\C(=O)O.C(N1C=NC2=C(N=CN=C12)N)[C@@H](C)OCP(=O)(N[C@@H](C)C(=O)OC(C)C)OC1C=CC=CC=1 |&1:19,26,r| |
替诺福韦阿拉芬酰胺富马酸酯 用途与合成方法
HIV-1, NRTIs
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.
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).
