201341-05-1
基本信息
替諾福韋二吡呋酯
替諾福韋酯(富馬酸鹽)
(R)-9-(2-磷酸甲氧基丙基)腺嘌呤二(異丙氧羰基氧甲基)酯
SRY
Aids080741
Aids-080741
Bis(poc)pmpa
Pmpa prodrug
Tenofov ir Disoprox
Tenofovir disoproxil
Testis-determining factor
TenofivirDisoproxilFumarate
物理化學(xué)性質(zhì)
常見問題列表
替諾福韋酯口服吸收后很快水解為替諾福韋,后者可被細胞激酶磷酸化為具有藥理活性的代謝產(chǎn)物替諾福韋二磷酸,后者可與5'-三磷酸脫氧腺苷酸競爭,參與病毒DNA的合成,其進入病毒DNA鏈后,由于其缺乏3'-OH基團,因而可導(dǎo)致DNA延長受阻,進而阻斷病毒的復(fù)制。
Tenofovir shows cytotoxic effects on cell viability in HK-2 cells, with IC 50 values of 9.21 and 2.77 μM at 48 and 72 h in MTT assay, respectively. Tenofovir diminishes ATP levels in HK-2 cells. Tenofovir (3.0 to 28.8 μM) increases oxidative stress and protein carbonylation in HK-2 cells. Furthermore, Tenofovir induces apoptosis in HK-2 cells, and that apoptosis is induced via mitochondrial damage. Tenofovir and M48U1 formulated in 0.25% HEC each inhibits the replication of both R5-tropic HIV-1 BaL and X4-tropic HIV-1 IIIb in activated PBMCs, and inhibits several laboratory strains and patient-derived HIV-1 isolates. The combined formulation of M48U1 and tenofovir in 0.25% HEC exhibits synergistic antiretroviral activity against infection with R5-tropic HIV-1 BaL , and is not toxic to PBMCs.
Tenofovir Disoproxil Fumarate (20, 50, 140, or 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) significantly reduces HIV transmission in BLT mice. Tenofovir Disoproxil Fumarate (0.5, 1.5, or 5.0 mg/kg/day, p.o.) induces 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.