替诺福韦阿拉芬酰胺富马酸酯
| 中文名称 | 替诺福韦阿拉芬酰胺富马酸酯 |
|---|---|
| 中文同义词 | 泰诺福韦艾拉酚胺富马酸盐;替诺福韦艾拉酚胺富马酸盐(1:1);替诺福韦艾拉酚胺富马酸单盐;富马酸GS-7340;GS 7340 富马酸盐;泰诺福韦艾拉酚胺半盐;替诺福韦艾拉酚胺富马酸盐[单盐];GS7340单盐 |
| 英文名称 | Tenofovir alafenamide fumarate |
| 英文同义词 | GS-7340 (fuMarate);L-Alanine, N-[(S)-[[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]phenoxyphosphinyl]-, 1-methylethyl ester, (2E)-2-butenedioate (1:1);N-[(S)-[[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]phenoxyphosphinyl]-L-llanine 1-methylethyl ester (2E)-2-butenedioate (1:1);Tenofovir alafenamide fumarate (1:1 salt);Tenofovir alafenamide-19;Tenofovir impurity 42/Tenofovir Alafenamide Fumarate/isopropyl ((R)-((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)-L-alaninate fumarate;tenofovir alafenamide fumarate (TAF);vemlidy |
| CAS号 | 379270-38-9 |
| 分子式 | C25H33N6O9P |
| 分子量 | 592.55 |
| EINECS号 | 223-388-5 |
| 相关类别 | 原料药;抗病毒药 |
| Mol文件 | 379270-38-9.mol |
| 结构式 |  |
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 |
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).