生物活性
Peramivir Trihydrate is a trihydrate of the anti-infection agent Peramivir Trihydrate which is a transition-state analogue and a potent, specific influenza viral neuraminidase inhibitor with an IC50 of median 0.09 nM. The IC50 for Peramivir Trihydrate is markedly lower than that for either zanamivir or oseltamivir. Peramivir Trihydrate increases survival in preclinical influenza models, including mouse and ferret models of highly pathogenic avian influenza H5N1. One day of treatment with Peramivir Trihydrate is active, and multiple days of treatment rescues most or all mice with H5N1. Similar data have been obtained in ongoing murine experiments with seasonal influenza A (H1N1)/H274Y. After parenteral administration,Peramivir Trihydrate reaches very high plasma concentrations. Peramivir Trihydrate is not metabolized, and is cleared by the means of renal filtration. It has a long half-life, especially in comparison with other neuraminidase inhibitors. Due to the failure of the metabolism of the antivirus compound Peramivir Trihydrate, as well as its wide distribution and the excretion in the unchanged form in urine, dosing regimens can be adapted easily for patients with renal impairment and for pediatric populations. Peramivir Trihydrate is originally developed by BioCryst Pharmaceuticals. And Peramivir Trihydrate is designed to aim to an antiviral agent. Peramivir Trihydrate has been performed phase III clinical trials for the treatment of influenza.
化学数据
分子量 | 382.45 |
分子式 | C15H28N4O4.3H2O |
CAS号 | 1041434-82-5 |
纯度 | >99% |
溶解性(25°C) | Water 4 mg/mL (Need ultrasonic) |
储存和运输条件 | 固体粉末: -20°C 冷藏长期储存 常温运输及临时存放 |
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
| 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。
储备液配制
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 | 2.6147 mL | 13.0736 mL | 26.1472 mL |
5 mM | 0.5229 mL | 2.6147 mL | 5.2294 mL |
10 mM | 0.2615 mL | 1.3074 mL | 2.6147 mL |