Tenofovir hydrate (GS 1278 hydrate) is a nucleotide reverse transcriptase inhibitor with antiviral activity, inhibits EBV replication, and is used in the study of HIV and HBV.

HK-2 cells:9.21 μM (48 h)

Tenofovir hydrate exhibited cytotoxic effects in HK-2 cells, with IC50 values of 9.21 and 2.77 μM at 48 h and 72 h, respectively, in the MTT assay.Tenofovir hydrate decreased ATP levels in HK-2 cells and increased oxidative stress and protein carbonylation in the range of 3.0 to 28.8 μM. In addition, Tenofovir hydrate induced apoptosis in HK-2 cells through mitochondrial damage. [1]
The formulation of Tenofovir hydrate and M48U1 in 0.25% HEC inhibited replication of R5ophilic HIV-1BaL and X4ophilic HIV-1IIIb in activated PBMCs, as well as multiple laboratory strains and patient-derived HIV-1 strains. The combination of M48U1 and Tenofovir hydrate demonstrated synergistic antiviral activity against R5ophilic HIV-1BaL infection and was non-toxic to PBMCs. [2]

Tenofovir Disoproxil fumarate (20, 50, 140, or 300 mg/kg) administered to BLT mice shows dose-dependent activity against vaginal HIV challenge in BLT humanized mice, significantly decreasing HIV transmission at 50, 140, and 300 mg/kg [3]. Additionally, Tenofovir Disoproxil fumarate (0.5, 1.5, or 5.0 mg/kg/day, p.o.) causes a dose-dependent decline in serum viremia in woodchucks chronically infected with WHV, proving to be safe and effective in the woodchuck model of chronic HBV infection [4].