| CAS NO: | 1216941-48-8 |
| 包装: | 10mg, 50mg |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
Paritaprevir (ABT-450)是一种NS3/4A抑制剂。Paritaprevir对HCV 1a和1b的EC50值分别为1 和0.21 nM。
The CC50 of ABT-450 is more than 37 μM, resulting in an in vitro selectivity index of ≥37,000-fold. ABT-450 demonstrates activity across multiple HCV genotypes, with an EC50 of 5.3 nM against the genotype 2a JFH-1 subgenomic replicon and EC50s of 19, 0.09, and 0.69 nM against replicons containing NS3 protease from genotypes 3a, 4a, and 6a, respectively.
After oral administration, paritaprevir reaches maximum concentrations in a mean of 4-5 h with increases in exposure more than dose proportional. Absolute bioavailability is about 50% after administering with food. It displays high (about 97-99.9 %) plasma protein binding and has apparent volumes of distribution of 16.7L. Paritaprevir metabolism occurs via CYP3A4 (predominantly) and CYP3A5.
| 分子量 | 765.88 |
| 分子式 | C40H43N7O7S |
| CAS号 | 1216941-48-8 |
| 纯度 | >99% |
| 溶解性（25°C） | DMSO: ≥ 90 mg/mL |
| 储存和运输条件 | 2-8°C, dry, protect from light, sealed 常温运输及临时存放 |
| 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。
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.3057 mL | 6.5284 mL | 13.0569 mL |
| 5 mM | 0.2611 mL | 1.3057 mL | 2.6114 mL |
| 10 mM | 0.1306 mL | 0.6528 mL | 1.3057 mL |
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