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Pradefovir mesylate

(Synonyms: Remofovir mesylate)

目录号: PL14539 纯度: ≥99%

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)，Km 为 60 μM。

CAS No. :625095-61-6

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中文名称	Pradefovir mesylate
英文名称	Pradefovir mesylate
英文别名	9-[2-[(2R,4S)-4-(3-Chlorophenyl)-2-oxido-1,3,2-dioxaphosphinan-2-ylmethoxy]ethyl]adenine mesylate;Pradefovir Mesilate;9-(2-{[(2R,4S)-4-(3-chlorophenyl)-2-oxido-1,3,2-dioxaphosphinan-2-yl]methoxy}ethyl)-9H-purin-6-amine methanesulfonate (1:1);9-[2-[[(2R,4S)-4-(3-chlorophenyl)-2-oxo-1,3,2λ⁵-dioxaphosphinan-2-yl]methoxy]ethyl]purin-6-amine,methanesulfonic acid;MB-06866,MB-6866,Hepavir B,Remofovir mesylate;Pradefovir mesylate
Cas No.	625095-61-6
分子式	C₁₇H₁₉N₅O₄PCl^.CH₄O₃S
分子量	519.90
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	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)，Km 为 60 μM。

产品详情

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。

生物活性

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.

性状

Solid

IC50 & Target[1][2]

CYP3

体外研究(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 Km of 60 μM, a maximum rate of metabolism of 228 pmol/min/mg protein, and an intrinsic clearance of about 359 L/min. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Lin CC, et al. Metabolic activation of Pradefovir by CYP3A4 and its potential as an inhibitor or inducer. Antimicrob Agents Chemother. 2006 Sep;50(9):2926-31.

溶解度数据	In Vitro: H₂O : 100 mg/mL (192.34 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

[1]. Lin CC, et al. Metabolic activation of Pradefovir by CYP3A4 and its potential as an inhibitor or inducer. Antimicrob Agents Chemother. 2006 Sep;50(9):2926-31.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Pradefovir mesylate

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