Tenofovir Disoproxil fumarate 是一种核苷酸逆转录酶抑制剂，有潜力研究艾滋病和慢性乙型肝炎。

Tenofovir Disoproxil Fumarate is a pro-drug, fumaric acid salt form of tenofovir, a nucleoside reverse transcriptase inhibitor analog of adenosine. Tenofovir disoproxil fumarate is prescribed to treat HIV and chronic hepatitis B virus (HBV) in adults.

Tenofovir shows cytotoxic effects on cell viability in HK-2 cells in MTT assay (IC50: 9.21/2.77 μM at 48/72 h). Tenofovir lowers ATP levels in HK-2 cells. Tenofovir (3.0-28.8 μM) promotes protein carbonylation and oxidative stress in HK-2 cells. In addition, Tenofovir promotes apoptosis induced via mitochondrial damage in HK-2 cells. M48U1 and Tenofovir formulated in 0.25% HEC each inhibits the replication of both X4-tropic HIV-1IIIb and R5-tropic HIV-1BaL in activated PBMCs and inhibits patient-derived HIV-1 isolates and several laboratory strains. Aforesaid mixture exhibits synergistic antiretroviral activity against infection with R5-tropic HIV-1BaL and is not toxic to PBMCs.

Tenofovir Disoproxil Fumarate (20/50/140/300?mg/kg) administered to BLT mice, shows dose-dependent activity during vaginal HIV challenge in BLT humanized mice. Tenofovir Disoproxil Fumarate (50/140/300?mg/kg) obviously lowers HIV transmission in BLT mice. Tenofovir Disoproxil Fumarate (0.5/1.5/5.0 mg/kg/day, p.o.) promotes a dose-dependent decline in serum viremia in woodchucks chronically infected with WHV. Tenofovir Disoproxil Fumarate administration is safe and effective in the woodchuck model of chronic HBV infection.

HAT and HDAC Activity Assays :After homogenization of cardiac tissues, nucleoproteins are extracted using a Nuclear Extract Kit according to the manufacturer's instructions. HAT and HDAC activities of the nuclear protein extracts are determined using a colorimetric assay included in the HAT and HDAC assay kits.

Cells are plated into 48-well tissue culture plates (39,000 cells/mL) and allowed to grow for 48 h followed by treatment with vehicle or Tenofovir. Following the treatment period, cell viability is assessed using the MTT assay. The MTT assay relies on the conversion of tetrazolium dye 3-(4,5-dimethlthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) to formazan by NAD(P)H-dependent oxidoreductases.

Tenofovir Disoproxil Fumarate is prepared in a placebo control. Twenty adult chronic WHV carrier woodchucks are stratified equally by age, sex, body weight, and serum GGT activity into five treatment groups consisting of four animals each: (i) Tenofovir Disoproxil Fumarate at 15.0 mg/kg once per day, (ii) Tenofovir Disoproxil Fumarate at 5.0 mg/kg/day, (iii) Tenofovir Disoproxil Fumarate at 1.5 mg/kg/day, (iv) Tenofovir Disoproxil Fumarate at 0.5 mg/kg/day, and (v) a placebo control. The woodchucks are treated daily for 4 weeks and observed for an additional 12 weeks following cessation of drug treatment.

202138-50-9

C19H30N5O10P·C4H4O4

635.51

GS-1278 Disoproxil Fumarate;富马酸替诺福韦酯;Tenofovir DF

Ethanol:44 mg/mL (69.23 mM)
DMSO:128 mg/mL (201.41 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years