Dasabuvir (ABT-333) 是一种HCV非结构蛋白 5B (NS5B) 的非核苷抑制剂，抑制RNA依赖性的 HCV NS5B 基因编码的 RNA 聚合酶，IC50范围为 2.2 到 10.7 nM。
别名：Dasabuvir
ABT-333 is a nonnucleoside NS5B polymerase inhibitor for the treatment of HCV infection. An interferon-free combination of the protease inhibitor ABT-450 with ritonavir (ABT-450/r), the nonnucleoside polymerase inhibitor ABT-333, and ribavirin showed efficacy against the hepatitis C virus (HCV) in a pilot study involving patients with HCV genotype 1 infection. ABT-333 is currently under clinical trials for the treatment of Hepatitis C.
| 体外实验* | |
|---|---|
| 细胞系 | HCV replicon cells |
| 方法 | MTT analysis Both replicon-containing cell lines were maintained in Dulbecco’s modified Eagle’s medium (DMEM) containing 100 IU/ml penicillin, 100 g/ml streptomycin, and 200 g/ml G418 (all from Invitrogen, Carlsbad, CA) with 10% (vol/vol) fetal bovine serum (FBS).TheinhibitoryeffectsofdasabuvironHCVRNAreplication were determined in DMEM containing 5% FBS, with or without 40% human plasma (Bioreclamation, Westbury, NY), by measuring the activity of the luciferase reporter gene. The cells were incubated for 3 days in the presence of dasabuvir and subsequently were lysed and processed according to the manufacturer’s instructions (Promega, Madison, WI). The luciferase activity in the cells was measured using a Victor II luminometer (Perkin-Elmer, Waltham, MA); 50% effective concentration (EC50) values were calculated using nonlinear regression curve fitting to a 4-parameter logistic equation with GraphPad Prism 4 software. EC50s and standard deviations (SDs) were calculated from at least 3 experiments conducted in duplicate. The cytotoxicity of dasabuvir was determined with the colorimetric assay using MTT. |
| 浓度 | Dasabuvir inhibited replication of HCV subgenomic replicons in cell culture assays, with EC50 values of 7.7 and 1.8 nM against genotype 1a (H77) and 1b (Con1), respectively. |
| 处理时间 | 3 days |
*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。
| 体内实验* | |
|---|---|
| 动物模型 | none |
| 配制 | |
| 剂量 | |
| 给药处理 | |
*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。
| 分子量 | 493.57 |
| 分子式 | C26H27N3O5S |
| CAS号 | 1132935-63-7 |
| 溶解性（25°C） | DMSO 26 mg/mL |
| 储存条件 |
粉末型式 -20°C 3年；4°C 2年 溶于溶剂 -80°C 6个月；-20°C 1个月 |
| 运输方式 | 冰袋运输，根据产品的不同，可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.0261 mL | 10.1303 mL | 20.2606 mL |
| 5 mM | 0.4052 mL | 2.0261 mL | 4.0521 mL |
| 10 mM | 0.2026 mL | 1.013 mL | 2.0261 mL |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
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