Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pradefovir mesylate (Hepavir B) 是一种肝脏 CYP3A4 底物。在人肝微粒体中,Pradefovir 能够转化为 9-[2-(磷酸甲氧基)乙基]腺嘌呤,其Km=60 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,630 | 现货 | ||
5 mg | ¥ 4,130 | 现货 | ||
10 mg | ¥ 5,880 | 现货 | ||
25 mg | ¥ 8,980 | 现货 | ||
50 mg | ¥ 11,900 | 现货 | ||
100 mg | ¥ 16,300 | 现货 |
产品描述 | Pradefovir mesylate (Hepavir B) is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with Km of 60 μM. |
靶点活性 | CYP3A4:60 μM(Km,liver) |
体外活性 | Pradefovir was converted to PMEA in human liver microsomes with a K(m) 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. |
体内活性 | 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[1].? |
别名 | Pradefovir mesilate, Remofovir mesylate, Hepavir B, 甲磺酸帕拉德福韦 |
分子量 | 519.9 |
分子式 | C18H23ClN5O7PS |
CAS No. | 625095-61-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 120 mg/mL (230.81 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O | 1 mM | 1.9234 mL | 9.6172 mL | 19.2345 mL | 48.0862 mL |
5 mM | 0.3847 mL | 1.9234 mL | 3.8469 mL | 9.6172 mL | |
10 mM | 0.1923 mL | 0.9617 mL | 1.9234 mL | 4.8086 mL | |
20 mM | 0.0962 mL | 0.4809 mL | 0.9617 mL | 2.4043 mL | |
50 mM | 0.0385 mL | 0.1923 mL | 0.3847 mL | 0.9617 mL | |
100 mM | 0.0192 mL | 0.0962 mL | 0.1923 mL | 0.4809 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Pradefovir mesylate 625095-61-6 Metabolism P450 Pradefovir Cytochrome P450 Remofovir Mesylate Pradefovir mesilate Remofovir mesylate CYPs Inhibitor Hepavir B Pradefovir Mesylate Remofovir inhibit 甲磺酸帕拉德福韦 inhibitor