Description | Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an oral phosphonoamidate prodrug of the HIV reverse transcriptase nucleotide inhibitor tenofovir (TFV) |
In vitro | Tenofovir alafenamide hemifumarate(TAF)是一种口服的HIV逆转录酶核苷酸抑制剂替诺福韦(TFV)的磷酰胺前体化合物。在HEK293T细胞中过表达CatA或肝羧酸酯酶1(Ces1)可分别使细胞内TAF水解增加2倍和5倍。利用RNA干扰(RNAi)技术在HeLa细胞中敲减CatA表达,可使细胞内TAF代谢减少5倍。此外,抗HIV活性与CatA水解速率在一大组TFV磷酰胺前体化合物中显示了良好的相关性[1]。 |
Synonyms | GS-7340 (hemifumarate), Tenofovir alafenamide fumarate, 替诺福韦艾拉酚胺富马酸盐 |
molecular weight | 534.51 |
Molecular formula | C21H29N6O5P·1/2C4H4O4 |
CAS | 1392275-56-7 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
Solubility | DMSO: 50 mg/mL (93.54 mM) |
References | 1. Birkus G, Bam RA, Willkom M,et al.Intracellular Activation of Tenofovir Alafenamide and the Effect of Viral and Host Protease Inhibitors[J].Antimicrob Agents Chemother. 2015 Oct 26;60(1):316-22. 2. Callebaut C , Stepan G , Tian Y , et al. In Vitro Virology Profile of Tenofovir Alafenamide, a Novel Oral Prodrug of Tenofovir with Improved Antiviral Activity Compared to Tenofovir Disoproxil Fumarate[J]. Antimicrobial Agents and Chemotherapy, 2015:AAC.01152-15. |