中文名 | 替诺福韦酯 |
英文名 | Tenofovir disoproxil |
别名 | 替诺福韦 泰诺福韦酯 替诺福韦酯 替诺福韦二吡呋酯 替诺福韦酯(富马酸盐) (R)-9-(2-磷酸甲氧基丙基)腺嘌呤二(异丙氧羰基氧甲基)酯 核苷酸逆转录酶抑制剂(TENOFOVIR DISOPROXIL) (R)-(((((1-(6-氨基-9H-嘌呤-9-基)丙-2-基)氧基)甲基)磷酰基)双(氧基)双(亚甲基) 二异丙基二碳酸酯 |
英文别名 | TD SRY TEND-API Tenofovir disoproxil Testis-determining factor TenofivirDisoproxilFumarate Tenofovir disoproxil aspartate 9-((R)-2-((Bis(((isopropoxycarbonyl)oxy)methoxy)phosphinyl)methoxy)propyl)adenine (R)-(((((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphoryl)-bis(oxy))bis(methylene) diis bis({[(1-methylethoxy)carbonyl]oxy}methyl) {[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl}phosphonate (R)-(((((1-(6-AMino-9H-purin-9-yl)propan-2-yl)oxy)Methyl)phosphoryl)bis(oxy))bis(Methylene) diisopropyl dicarbonate 2,4,6,8-Tetraoxa-5-phosphanonanedioicacid, 5-[[(1R)-2-(6-aMino-9H-purin-9-yl)-1-Methylethoxy]Methyl]-,1,9-bis(1-Methylethyl) ester, 5-oxide |
CAS | 201341-05-1 |
EINECS | 606-442-6 |
化学式 | C19H30N5O10P |
分子量 | 519.44 |
InChI | InChI=1/C19H30N5O10P/c1-12(2)33-18(25)28-9-31-35(27,32-10-29-19(26)34-13(3)4)11-30-14(5)6-24-8-23-15-16(20)21-7-22-17(15)24/h7-8,12-14H,6,9-11H2,1-5H3,(H2,20,21,22)/t14-/m1/s1 |
密度 | 1.45±0.1 g/cm3(Predicted) |
沸点 | 642.7±65.0 °C(Predicted) |
闪点 | 342.5°C |
蒸汽压 | 2.06E-16mmHg at 25°C |
折射率 | 1.578 |
酸度系数 | 4.20±0.10(Predicted) |
存储条件 | Keep in dark place,Inert atmosphere,2-8°C |
体外研究 | 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. |
体内研究 | 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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