Pradefovir mesylate

Research use only, not for human use.

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

Pradefovir mesylate is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with Km of 60 μM.(In Vitro):Pradefovir was converted to PMEA in human liver microsomes with a Km 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 Vivo):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.?

Remofovir mesylate; Hepavir B; Pradefovir mesilate

Metabolic Enzyme/Protease

P450

ACAT

——

——

625095-61-6

519.9

C18H23ClN5O7PS

>98% (HPLC)

——

CS(O)(=O)=O.Nc1ncnc2n(CCOC[P@@]3(=O)OCC[C@H](O3)c3cccc(Cl)c3)cnc12

——

(-20℃)

With Ice Pack

≥ 2 years