| Description | Tenofovir alafenamide fumarate (GS-7340 fumarate) is an orally available Tenofovir precursor compound Tenofovir alafenamide fumarate has anti-HIV activity and can be used to prevent HIV infection. |
| In vitro | Tenofovir alafenamide fumarate (TAF) 在各种细胞类型中的抗病毒活性相似，范围在5至7 nM之间，而在MT-4和MT-2细胞中CC50的变化范围为4.7至42 μM。针对包括HIV-1 M组亚型A至G以及N和O组分离物在内的一系列HIV-1和HIV-2分离物，评估了TAF的抗病毒活性。总体而言，TAF的EC50范围为0.1至12 nM，平均EC50为3.5 nM，与用作内部对照的AZT的平均EC50为11.8 nM相比，这是对在PBMC中测试的29个主要HIV-1分离物得出的结果。对于HIV-2分离物，TAF的平均EC50为1.8 nM，而AZT为6.4 nM。[2] |
| In vivo | Tenofovir alafenamide fumarate（GS-7340 fumarate）作为Tenofovir的酰胺前药，相较于Tenofovir disoproxil fumarate（TDF）[1]，具有良好的口服生物利用度并增强了血浆稳定性。 |
| Synonyms | GS-7340 fumarate |
| molecular weight | 592.54 |
| Molecular formula | C25H33N6O9P |
| CAS | 379270-38-9 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 25 mg/mL (42.19 mM), Sonication is recommended. DMSO: 200 mg/mL (337.53 mM), Sonication is recommended. |
| References | 1. Babusis D, et al. Mechanism for effective lymphoid cell and tissue loading following oral administration of nucleotide prodrug GS-7340. Mol Pharm. 2013 Feb 4;10(2):459-66. 2. Ruane PJ, et al. Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of tenofovir alafenamide as 10-day monotherapy in HIV-1-positive adults. J Acquir Immune Defic Syndr. 2013 Aug 1;63(4):449-55. |
Tenofovir alafenamide fumarate
CAS No.: 379270-38-9
Tenofovir alafenamide fumarate (GS-7340 fumarate) is an orally available Tenofovir precursor compound Tenofovir alafenam
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