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1236287-04-9

中文名稱 1236287-04-9
英文名稱 Tenofovir (Maleate)
CAS 1236287-04-9
分子式 C13H18N5O8P
分子量 403.29
MOL 文件 1236287-04-9.mol
1236287-04-9 結(jié)構(gòu)式 1236287-04-9 結(jié)構(gòu)式

基本信息

中文別名
替諾福韋馬來酸鹽
英文別名
Tenofovir (Maleate)

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
溶解度溶于二甲基亞砜
形態(tài)粉末

常見問題列表

生物活性
Tenofovir maleate (GS 1278 maleate) 是一種核苷酸逆轉(zhuǎn)錄酶 (nucleotide reverse transcriptase) 抑制劑,有潛力用于艾滋病毒和慢性乙型肝炎的研究。
體外研究

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.

體內(nèi)研究

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.

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