Tenofovir alafenamide fumarate 是 HIV 逆转录酶核苷酸抑制剂替诺福韦的口服膦酰胺前药。
产品描述
Tenofovir alafenamide fumarate (TAF) is an oral phosphonoamidate prodrug of the HIV reverse transcriptase nucleotide inhibitor tenofovir (TFV)
体外活性
Tenofovir alafenamide fumarate (TAF) is an oral phosphonoamidate prodrug of the HIV reverse transcriptase nucleotide inhibitor tenofovir (TFV).?Overexpression of CatA or liver carboxylesterase 1 (Ces1) in HEK293T cells increased intracellular TAF hydrolysis 2- and 5-fold, respectively.?Knockdown of CatA expression with RNA interference (RNAi) in HeLa cells reduced intracellular TAF metabolism 5-fold.?Additionally, the anti-HIV activity and the rate of CatA hydrolysis showed good correlation within a large set of TFV phosphonoamidate prodrugs[1].
Cas No.
1392275-56-7
分子式
C21H29N6O5P·1/2C4H4O4
分子量
534.51
别名
替诺福韦艾拉酚胺富马酸盐;Tenofovir alafenamide fumarate;GS-7340 (hemifumarate)
储存和溶解度
DMSO:50 mg/mL (93.55 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years