产品说明书
Tenofovir Disoproxil fumarate
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同义名 : | Tenofovir DF;Bis(POC)-PMPA fumarate;Bis(POC)-PMPA;Tenofovir Disoproxil (fumarate);GS 4331 fumarate |
| CAS号 : | 202138-50-9 | |
| 货号 : | A118576 | |
| 分子式 : | C23H34N5O14P | |
| 纯度 : | 99% | |
| 分子量 : | 635.515 | |
| MDL号 : | MFCD08141829 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(78.68 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 15 mg/mL(23.6 mM) |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Tenofovir Disoproxil fumarate (TVF), an antiviral drug, is a nucleotide reverse transcriptase inhibitor approved for treating HIV and chronic Hepatitis B. Tenofovir shows cytotoxic effects on cell viability in HK-2 cells, with IC50 values of 9.21 and 2.77 μM at 48 and 72 h in MTT assay, respectively. Moreover, experiments showed that TFV induced apoptosis in HK-2 cells, and that apoptosis is induced via mitochondrial damage[3]. Tenofovir Disoproxil fumarate (20, 50, 140, or 300 mg/kg) administered to BLT mice, shows dose dependent activity during vaginal HIV challenge in BLT humanized mice. Tenofovir Disoproxil fumarate (50, 140, 300 mg/kg) significantly reduces HIV transmission in BLT mice[4]. Tenofovir Disoproxil fumarate (0.5, 1.5, or 5.0 mg/kg/day, p.o.) induces a dose-dependent decline in serum viremia in woodchucks chronically infected with WHV. Tenofovir Disoproxil fumarate administration is safe and effective in the woodchuck model of chronic HBV infection[5]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| human bone marrow cells | Cytotoxic assay | 24 h | Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay, CC50=0.9 μM | 20439609 | |
| human HeLa P4/R5 cells | Function assay | Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=4.7 μM | 19596885 | ||
| human HeLa P4/R5 cells | Function assay | Antiviral activity against HIV1 harboring reverse transcriptase K65R mutant infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=11.4 μM | 19596885 | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01671982 | HIV | Phase 1 | Completed | - | Thailand ... 展开 >> Sanpatong Hospital Sanpatong, Chiang Mai, Thailand, 20120 HIV-NAT Bangkok, Thailand, 10330 Nakornping Hospital Chiang Mai, Thailand Chonburi Hospital Chonburi, Thailand, 20000 Phayao Hospital Phayao, Thailand, 56000 收起 << |
| NCT01745822 | Hepatitis B Chronic Infection ... 展开 >> Pregnancy 收起 << | Phase 3 | Active, not recruiting | October 2018 | Thailand ... 展开 >> Prapokklao Hospital Chantha Buri, Chanta Buri, Thailand, 22000 Mae Chan Hospital Mae Chan, Chiangrai, Thailand, 57110 Banglamung Hospital Bang Lamung, Chon Buri, Thailand, 20150 Maharat Nakhon Ratchasima Hospital Nakhon Ratchasima, Nakhon Ratchasrima, Thailand, 30000 Chiang Kham Hospital Chiang Kham, Phayao, Thailand, 56110 Bhumibol Adulyadej Hospital Bangkok, Thailand, 10220 Nopparat Rajathanee Hospital Bangkok, Thailand, 10230 Health Promotion Center Region 10 Chiang Mai, Thailand, 50100 Nakornping Hospital Chiang Mai, Thailand, 50180 Chiangrai Prachanukroh Hospital Chiang Rai, Thailand, 57000 Chonburi Regional Hospital Chon Buri, Thailand, 20000 Khon Kaen Hospital Khon Kaen, Thailand, 40000 Lampang Hospital Lampang, Thailand, 52000 Lamphun Hospital Lamphun, Thailand, 51000 Phayao Provincial Hospital Phayao, Thailand, 56000 Samutprakarn Hospital Samut Prakan, Thailand, 10280 Samutsakhon Hospital Samut Sakhon, Thailand, 74000 收起 << |
| NCT02174276 | Chronic Hepatitis B | Phase 2 | Completed | - | - |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.57mL 0.31mL 0.16mL |
7.87mL 1.57mL 0.79mL |
15.74mL 3.15mL 1.57mL |
| 参考文献 |
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