| Description | Tenofovir alafenamide (GS-7340) is a nucleotide reverse transcriptase inhibitor (NRTI) and a novel ester prodrug of the antiretroviral tenofovir. |
| In vitro | Tenofovir alafenamide具有强大的抗HIV活性，其IC50为0.005 μM。[1] 在人类血浆中，Tenofovir alafenamide的半衰期为90分钟，在37°C的MT-2细胞提取物中，其半衰期为28.3分钟。[2] Tenofovir alafenamide的肝脏摄取通过OATP1B1和OATP1B3分别促进。Tenofovir alafenamide在转化为药理活性形式TFV-DP后，能够抑制HBV反转录酶。[3] |
| In vivo | 在雄性比格尔犬中，GS 7340 (10 mg/kg, p.o.) 显著提高了至淋巴组织的分布。[2] |
| Synonyms | 替诺福韦艾拉酚胺, 替诺福韦, GS-7340 |
| molecular weight | 476.47 |
| Molecular formula | C21H29N6O5P |
| CAS | 379270-37-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (115.43 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 88 mg/mL (184.7 mM) |
| References | 1. Chapman H, et al. Nucleosides Nucleotides Nucleic Acids. 2001, 20(4-7), 1085-10[90. 2. Lee WA, et al. Antimicrob Agents Chemother. 2005, 49(5), 1898-1906. 3. Murakami E, et al. Antimicrob Agents Chemother. 2015, 59(6), 3563-3569. 4. Fical L. Vývoj UHPLC-MS/MS metody pro analýzu vybraných antivirotik v HILIC a RP módu[J]. 2020 5. Fical L, Khalikova M, Kočová Vlčková H, et al. Determination of Antiviral Drugs and Their Metabolites Using Micro-Solid Phase Extraction and UHPLC-MS/MS in Reversed-Phase and Hydrophilic Interaction Chromatography Modes[J]. Molecules. 2021, 26(8): 2123. |
| Citations | 1. Fical L, Khalikova M, Kočová Vlčková H, et al. Determination of Antiviral Drugs and Their Metabolites Using Micro-Solid Phase Extraction and UHPLC-MS/MS in Reversed-Phase and Hydrophilic Interaction Chromatography Modes. Molecules. 2021, 26(8): 2123. |