Tenofovir alafenamide fumarate (GS-7340 fumarate) 是 Tenofovir 的口服前体药物。Tenofovir 是一种HIV-1核苷酸逆转录酶抑制剂。
产品描述
Tenofovir alafenamide fumarate (GS-7340 fumarate) is an investigational oral prodrug of Tenofovir. Tenofovir is an inhibitor of HIV-1 nucleotide reverse transcriptase.
体外活性
The antiviral activities of Tenofovir alafenamide fumarate (GS-7340 fumarate) 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 [2].
体内活性
Tenofovir alafenamide fumarate (GS-7340 fumarate), an amidate prodrug of Tenofovir, has good oral bioavailability and increases plasma stability compared to Tenofovir disoproxil fumarate (TDF) [1].
Cas No.
379270-38-9
分子式
C25H33N6O9P
分子量
592.54
别名
Tenofovir alafenamide fumarate
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years