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Pradefovir mesylate

CAS No. : 625095-61-6

MCE 站：Pradefovir mesylate

产品活性：Pradefovir mesylate 是肝脏 CYP3A4 的良好底物。Pradefovir 在人肝微粒体中转化为 9-[2-(磷酸甲氧基)乙基]腺嘌呤 (PMEA)，K_m 为 60 μM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Cytochrome P450

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.

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.

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