Tenofovir alafenamide 是一种核苷酸逆转录酶抑制剂和抗逆转录病毒替诺福韦的新型酯类前药。
产品描述
Tenofovir Alafenamide (GS-7340) is a nucleotide reverse transcriptase inhibitor (NRTI) and a novel ester prodrug of the antiretroviral tenofovir.
体外活性
GS-7340 has a potent anti-HIV activity with IC50 of 0.005 μM. [1] GS 7340 has a half-life of 90 min in human plasma and a half-life of 28.3 min in an MT-2 cell extract at 37°C. [2] the hepatic uptake of GS-7340 isfacilitated by OATP1B1 and OATP1B3, respectively. GS-7340 inhibits HBV reverse transcriptase after being converted to the pharmacologically active form, TFV-DP. [3]
体内活性
In male beagle dogs, GS 7340 (10 mg/kg, p.o.) results in an enhanced distribution to lymphatic tissue. [2]
Cas No.
379270-37-8
分子式
C21H29N6O5P
分子量
476.47
别名
替诺福韦艾拉酚胺;替诺福韦;GS-7340
储存和溶解度
DMSO:88 mg/mL (184.7 mM)
H2O:<1 mgml
Ethanol:88 mg/mL (184.7 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years