中文名 | GS 7340 富马酸盐 |
英文名 | GS-7340 Fumarate |
别名 | GS7340单盐 富马酸GS-7340 泰诺福韦艾拉酚胺半盐 GS 7340 富马酸盐 泰诺福韦艾拉酚胺富马酸盐 替诺福韦艾拉酚胺富马酸单盐 替诺福韦艾拉酚胺富马酸盐[单盐] |
英文别名 | vemlidy GS-7340 Fumarate GS-7340 (fuMarate) Tenofovir alafenamide-19 tenofovir alafenamide fumarate (TAF) |
CAS | 379270-38-9 |
EINECS | 223-388-5 |
化学式 | C25H33N6O9P |
分子量 | 592.55 |
溶解度 | DMSO: ≥ 36 mg/mL |
存储条件 | under inert gas (nitrogen or Argon) at 2-8°C |
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). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.688 ml | 8.438 ml | 16.877 ml |
5 mM | 0.338 ml | 1.688 ml | 3.375 ml |
10 mM | 0.169 ml | 0.844 ml | 1.688 ml |
5 mM | 0.034 ml | 0.169 ml | 0.338 ml |
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