化合物 T1649L T1649L

Product Introduction
Bioactivity


英文名: Tenofovir hydrate

描述: Tenofovir hydrate (GS 1278 hydrate) 是一种核苷酸逆转录酶抑制剂，用于治疗HIV 和慢性乙型肝炎 (HBV) 。

体外活性: Tenofovir exhibits 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 [1]. 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 [2].

体内活性: Tenofovir Disoproxil fumarate (20, 50, 140, or 300 mg/kg) administered to BLT mice, displays dose dependent activity during vaginal HIV challenge in BLT humanized mice. Tenofovir Disoproxil fumarate (50, 140, 300 mg/kg) significantly decreases HIV transmission in BLT mice [3]. 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 [4].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: Tenofovir Hydrate | Tenofovir hydrate

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途