Pradefovir mesylate 是一种肝脏 CYP3A4 底物。在人肝微粒体中，Pradefovir 能够转化为 9-[2-(磷酸甲氧基)乙基]腺嘌呤，其Km=60 μM。

Pradefovir mesylate is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with Km of 60 μM.

Pradefovir was converted to PMEA in human liver microsomes with a K(m) of 60 microM, a maximum rate of metabolism of 228 pmol/min/mg protein, and an intrinsic clearance of about 359 ml/min.?Addition of ketoconazole and monoclonal antibody 3A4 significantly inhibits the conversion of pradefovir to PMEA in human liver microsomes, suggesting the predominant role of CYP3A4 in the metabolic activation of pradefovir.?Pradefovir at 0.2, 2, and 20 microM was neither a direct inhibitor nor a mechanism-based inhibitor of CYP3A4, CYP2D6, CYP2C9, CYP2C19, CYP2E1, and CYP1A2 in human liver microsomes.

In rats, the liver was the site of metabolic activation of pradefovir, whereas the small intestine did not play a significant role in the metabolic conversion of pradefovir to PMEA.?Daily oral dosing (300 mg/kg) to rats for 8 days showed that pradefovir was not an inducer of P450 enzymes in rats[1].?

625095-61-6

C18H23ClN5O7PS

519.9

Hepavir B;Remofovir mesylate;甲磺酸帕拉德福韦;Pradefovir mesilate

H2O:120 mg/mL (230.81 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years