中文名 | 9-[(R)-2-(磷酰甲氧基)丙基]腺嘌呤 |
英文名 | R-PMPA |
别名 | 替诺福韦单水合物 替诺福韦一水合物 替诺福韦一水化合物 9-[(R)-2-(磷酰甲氧基)丙基]腺嘌呤 9-[(R)-2-(磷酰甲氧基)丙基]腺嘌呤(含水) 9-[(R)-2-(磷酰甲氧基)丙基]腺嘌呤(一水物) 9-(R)-2-(磷酰甲氧基)丙基腺嘌呤(R-PMPA) 9-[(R)-2-(磷酰甲氧基)丙基]腺嘌呤 (R-PMPA) (R)-(((1-(6-氨基-9H-嘌呤-9-基)丙烷-2-基)氧基)甲基)磷酸 水合物 |
英文别名 | R-PMPA Unii-99yxe507il PMPA Monohydrate Tenofovir (15 mg) Tenofovir (hydrate) Tenofovir Monohydrate (R)-9-(2-phosphonylmethoxy propyl)adenine (R)-9-(2-phosphonylmethoxypropyl)adenine (R-PMPA) 9-[(R)-2-(Phosphonomethoxy)propyl]adenine monohydrate 9-[(R)-2-(Phosphonomethoxy)propyl]adenine monohydrate 9-[(R)-2-(Phosphonomethoxy)propyl]adenine monohydrate (R-PMPA) {[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl}phosphonic acid hydrate (R)-(((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonic acid hydrate [[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]phosphonic acid monohydrate (r)-[[2-(6-amino-9h-purin-9-yl)-1-methylethoxy]methyl]-phosphonic acid monohydrate |
CAS | 206184-49-8 |
EINECS | 808-956-8 |
化学式 | C9H16N5O5P |
分子量 | 305.23 |
InChI | InChI=1/C9H14N5O4P.H2O/c1-6(18-5-19(15,16)17)2-14-4-13-7-8(10)11-3-12-9(7)14;/h3-4,6H,2,5H2,1H3,(H2,10,11,12)(H2,15,16,17);1H2/t6-;/m1./s1 |
熔点 | 270-274oC |
沸点 | 616.1℃ at 760mmHg |
溶解度 | 酸水溶液 (微溶),DMSO (微溶) |
存储条件 | 2-8°C |
稳定性 | 吸湿性 |
外观 | 固体 |
颜色 | White to Off-White |
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. |
海关编号 | 2933599550 |