替诺福韦酯
| 中文名称 | 替诺福韦酯 |
|---|---|
| 中文同义词 | 替诺福韦酯;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;替诺福韦二吡呋酯;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;TEND-API;泰诺福韦酯游离碱 |
| 英文名称 | Tenofovir disoproxil |
| 英文同义词 | (R)-(((((1-(6-AMino-9H-purin-9-yl)propan-2-yl)oxy)Methyl)phosphoryl)bis(oxy))bis(Methylene) diisopropyl dicarbonate;(R)-(((((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphoryl)-bis(oxy))bis(methylene) diis;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;TenofivirDisoproxilFumarate;SRY;Testis-determining factor;Tenofovir disoproxil, >=98%;Tenofovir disoproxil aspartate |
| CAS号 | 201341-05-1 |
| 分子式 | C19H30N5O10P |
| 分子量 | 519.44 |
| EINECS号 | 606-442-6 |
| 相关类别 | 医药原料;中间体;泰诺福韦中间体;原料药;有机中间体;产品-医药产品;化学试剂;化药杂质-替诺福韦酯;原料药及中间体 |
| Mol文件 | 201341-05-1.mol |
| 结构式 |  |
替诺福韦酯 性质
| 沸点 | 642.7±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.45±0.1 g/cm3(Predicted) |
| 储存条件 | Keep in dark place,Inert atmosphere,2-8°C |
| 溶解度 | 二甲基亚砜：≥38mg/mL（73.16mM） |
| 酸度系数(pKa) | 4.20±0.10(Predicted) |
| CAS 数据库 | 201341-05-1 |
替诺福韦酯口服吸收后很快水解为替诺福韦，后者可被细胞激酶磷酸化为具有药理活性的代谢产物替诺福韦二磷酸，后者可与5'-三磷酸脱氧腺苷酸竞争，参与病毒DNA的合成，其进入病毒DNA链后，由于其缺乏3'-OH基团，因而可导致DNA延长受阻，进而阻断病毒的复制。Tenofovir Disoproxil (Bis(POC)-PMPA) 是核苷酸逆转录酶抑制剂 (nucleotide reverse transcriptase inhibitor)，有潜力用于艾滋病和慢性乙型肝炎的研究。
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.
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.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-13782A | Tenofovir Disoproxil | 5 mg | 312元 | |
| 2024/01/25 | HY-13782A | 替诺福韦酯 Tenofovir Disoproxil | 201341-05-1 | 10mg | 500元 |