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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. Form:Solid IC50& Target:CYP3
中文名称
Pradefovir mesylate, DNA 聚合酶/逆转录酶抑制剂
英文名称
Pradefovir mesylate
中文别名
甲磺酸帕地福韦酯
英文别名
Pradefovir Mesylate | mb6866 | Pradefovir mesylate (Remofovir mesylate) | ICN-2001-3 | Pradefovir mesilate | PRADEFOVIR MESILATE [WHO-DD] | UNII-0D5204ZSIX | MB-06866 | 625095-61-6 | Q27095685 | DTXSID00211558 | 9-[2-[[(2R,4S)-4-(3-chlorophenyl)-2-oxo-1,3
CAS号
625095-61-6
分子式
C18H23ClN5O7PS
分子量
519.90 g/mol
精确质量
-
PSA
177.000 Ų
Logp
-
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Pradefovir mesylate 10mM in Water 1ml

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