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.

Pradefovir is a cyclodiester prodrug of PMEA. It is one of the Hep Direct prodrugs, which are designed to be efficiently and specifically activated through an oxidative reaction catalyzed by CYP3A4, which is located mainly in the liver.Pradefovir is converted to PMEA in human liver microsomes with a Km of 60 μM, a maximum rate of metabolism of 228 pmol/min/mg protein, and an intrinsic clearance of about 359 L/min.

Daily oral dosing of Pradefovir (300 mg/kg) to rats for 8 days does not affect body weight; liver weight; liver weight-body weight ratio; liver microsomal protein content; total CYP content; enzyme activities for CYP1A, CYP2B, and CYP3A; and apoprotein contents for CYP1A1, CYP2B1/2, CYP3A1/2, and CYP4A1/3, indicating that Pradefovir is not a CYP inducer in rats.

Remofovir mesylate | Hepavir B | Pradefovir mesilate

Metabolic Enzyme/Protease

P450

ACAT

——

——

625095-61-6

519.89

C18H23ClN5O7PS

>98% (HPLC)

In Vitro:?H2O : 100 mg/mL (192.34 mM)

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

——

(-20℃)

With Ice Pack

≥ 2 years