Name | R-PMPA |
Synonyms | 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 |
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 |
Molecular Formula | C9H16N5O5P |
Molar Mass | 305.23 |
Melting Point | 270-274oC |
Boling Point | 616.1℃ at 760mmHg |
Solubility | Aqueous Acid (Slightly), DMSO (Slightly) |
Appearance | Solid |
Color | White to Off-White |
Storage Condition | 2-8°C |
Stability | Hygroscopic |
In vitro study | 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. |
In vivo study | 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. |
HS Code | 2933599550 |
Application | TDF is used in adult CHB patients with evidence of viral replication and evidence of persistent elevation of serum transaminase (ALT or AST) or active liver disease. Includes HBeAg-positive or HBeAg-negative adult patients with compensated CHB. |
biological activity | Tenofovir hydrate (GS 1278 hydrate) is a nucleotide reverse transcriptase (nucleotide reverse transcriptase) inhibitor that can be used for HIV and chronic hepatitis B (Hepatitis B; HBV) research. |