生物活性
Cidofovir通过选择性抑制病毒DNA的合成而抑制病毒复制。Cidofovir处理培养的细胞,抑制人类巨细胞病毒(HCMV)感染。Cidofovir抑制巨细胞病毒(CMV)蚀斑形成,即使是感染后48小时后加入到细胞中,作用于Davis和AD-169株时IC50分别为0.9 μg/mL和1.6 μg/mL。 Cidofovir也抑制单纯疱疹病毒感染。
化学数据
分子量 | 279.19 |
分子式 | C8H14N3O6P |
CAS号 | 113852-37-2 |
纯度 | >99% |
溶解性(25°C) | DMSO |
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 |
实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验 |
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细胞系 | Madin–Darby Canine Kidney or Vero cells |
方法 | In vitro efficacy of cidofovir against CHV-1 Madin–Darby Canine Kidney or Vero cells were plated into 96-well plates at 1*104 cells/well and maintained in Dulbecco’s minimal essential medium with 1 g/L glucose, l-glutamine, and sodium pyruvate (Cell Grow; Corning, Manassas, VA) containing 10% fetal bovine serum (Atlanta Biological, Flowery Branch, GA) and penicillin (200 U/mL)/ streptomycin (200 mg/mL) (Life Technologies, Grand Island, NY) for 24 h until confluent. Monolayers were infected with 5 PFU/well CHV-1 (a previously described field strain that was also utilized during the in vivo experimental study evaluating cidofovir) or HSV-1 strain F, respectively. After 2 h of incubation at 37 C, virus supernatants were removed, cells were rinsed once with phosphate-buffered saline (PBS), and 100 mL of sequential 2-fold serial dilutions of cidofovir (starting at 625 mM) was added to each well. Infection controls without cidofovir and noninfected drug-treated controls were also included. Plates were incubated at 37 C until a cytopathic effect (CPE) was visible in the infected nontreated controls, which was *72 hours postinfection (hpi) for CHV-1 and 48 hpi for HSV-1, respectively. Plates were rinsed 3 times with PBS, fixed in 80% ethanol for 10 min at -20 C, and stained with crystal violet (Fisher Scientific, Fair Lawn, NJ). Virusinduced CPE was scored as the percent of wells per dilution with observable plaque formation, and EC50 values were calculated using GraphPad Prism. |
浓度 | 0~625μM |
处理时间 | 72 hours postinfection (hpi) for CHV-1 and 48 hpi for HSV-1 |
动物实验 |
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动物模型 | Recurrent ocular CHV-1 infection in dogs by administration of systemic prednisolone (3.0 mg/kg PO q24 h) for 7 consecutive days beginning on study day 1. |
配制 | 0.9% sodium chloride solution |
剂量 | 1 drop of 0.5% cidofovir ophthalmic solution |
给药处理 | eyes drop |
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 |
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1 mM | 3.5818 mL | 17.909 mL | 35.8179 mL |
5 mM | 0.7164 mL | 3.5818 mL | 7.1636 mL |
10 mM | 0.3582 mL | 1.7909 mL | 3.5818 mL |