Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a K m of 60 μM.
Storage Temp
Desiccated,Store at -80°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Action Type
INHIBITOR
Mechanism of action
DNA polymerase/reverse transcriptase inhibitor
Product Description
Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a K m of 60 μM.
In Vitro
Pradefovir is a cyclodiester prodrug of PMEA. It is one of the HepDirect 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 K m of 60 μM, a maximum rate of metabolism of 228 pmol/min/mg protein, and an intrinsic clearance of about 359 L/min. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
