Tenofovir Alafenamide Hemifumarate
- 体外研究:
- Tenofovir disoproxil fumarate (TDF) serves as a control for CatA-independent prodrug activation. Baseline antiviral activities (mean EC50±standard deviation) obtained in the absence of a protease inhibitors (PI) are determined from 6 independent donors for GS-7340 (EC50=5.3±1.2 nM) and TDF (EC50=2.8±1.1 nM) and are used to calculate fold change EC50s from four independent donors under conditions of PI pretreatment[1]. GS-7340 antiviral activities are similar across all cell types, ranging from 5 to 7 nM, while the CC50 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 EC50s range from 0.1 to 12 nM, with a mean EC50 of 3.5 nM compared to a mean EC50 of 11.8 nM for AZT, which is used as an internal control. For the HIV-2 isolates, the mean EC50s are
- 体内研究:
- GS-7340 is an amidate prodrug of Tenofovir with good oral bioavailability and increases plasma stability compared to Tenofovir disoproxil fumarate (TDF) [1].
- 简介:
- GS-7340(Tenofovir alafenamide) is a prodrug of tenofovir (TFV) that more efficiently delivers TFV into lymphoid cells and tissues than TFV disoproxil fumarate. HIV-1, NRTIs[1]
- 特异性:
- Target: HIV. Fields: GS-7340(Tenofovir alafenamide) is a prodrug of tenofovir (TFV) that more efficiently delivers TFV into lymphoid cells and tissues than TFV disoproxil fumarate. HIV-1, NRTIs[1]
- 储存:
- 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
- 其他名称:
- Tenofovir alafenamide; GS7340; GS 7340