Powder: -20°C for 3 years | In solvent: -80°C for 1 year
RO6889678 是高效的 HBV 衣壳结构抑制剂,其吸收、分布、代谢和排泄特征较为复杂。它可通过 CYP3A4 介导的氧化作用进行代谢,以及通过 UDP-葡萄糖醛酸基转移酶 UGT1A3 和 UGT1A1 介导的直接葡萄糖醛酸化作用进行代谢。它是一种诱导剂,可作用于人肝细胞中 CYP3A4 和共调节蛋白。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 648 | 现货 | ||
2 mg | ¥ 947 | 现货 | ||
5 mg | ¥ 1,330 | 现货 | ||
10 mg | ¥ 1,910 | 现货 | ||
25 mg | ¥ 2,730 | 现货 | ||
50 mg | ¥ 3,970 | 现货 | ||
100 mg | ¥ 5,790 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,430 | 现货 |
产品描述 | RO6889678 is HBV inhibitor with a complex ADME profile. |
体外活性 | RO6889678, a novel inhibitor of HBV with a complex absorption, distribution, metabolism, and excretion (ADME) profile.?RO6889678 showed an intracellular enrichment of 78-fold in hepatocytes, with an apparent intrinsic clearance of 5.2 l/min per mg protein and uptake and biliary clearances of 2.6 and 1.6 l/min per mg protein, respectively.?When apparent intrinsic clearance was incorporated into a PBPK model, the simulated oral human profiles were in good agreement with observed data at low doses but were underestimated at high doses due to unexpected overproportional increases in exposure with dose.?In addition, the induction potential of RO6889678 on cytochrome P450 (P450) enzymes and transporters at steady state was assessed and cotreatment with ritonavir revealed a complex drug-drug interaction with concurrent P450 inhibition and moderate UDP-glucuronosyltransferase induction. |
分子量 | 494.92 |
分子式 | C21H20ClFN4O5S |
CAS No. | 1578153-27-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (111.13 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0205 mL | 10.1026 mL | 20.2053 mL | 50.5132 mL |
5 mM | 0.4041 mL | 2.0205 mL | 4.0411 mL | 10.1026 mL | |
10 mM | 0.2021 mL | 1.0103 mL | 2.0205 mL | 5.0513 mL | |
20 mM | 0.101 mL | 0.5051 mL | 1.0103 mL | 2.5257 mL | |
50 mM | 0.0404 mL | 0.2021 mL | 0.4041 mL | 1.0103 mL | |
100 mM | 0.0202 mL | 0.101 mL | 0.2021 mL | 0.5051 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。
RO6889678 1578153-27-1 Microbiology/Virology HBV RO 6889678 inhibit Hepatitis B virus coregulated protein UDP-glucuronosyltransferase HB capsid formation ADME CYP3A4 hepatocytes CYPs RO-6889678 Cytochrome P450 UGT1A3 oxidation UGT1A1 Inhibitor glucuronidation inhibitor