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富马酸替诺福韦酯 /Tenofovir Disoproxil fumarate {[allProObj[0].p_purity_real_show]}

货号:A118576 同义名: Tenofovir DF;Bis(POC)-PMPA fumarate

Tenofovir disoproxil fumarate can block reverse transcriptase which has antiviral activity against HBV and HIV-1.

Tenofovir Disoproxil fumarate 化学结构 CAS号:202138-50-9
Tenofovir Disoproxil fumarate 化学结构
CAS号:202138-50-9
Tenofovir Disoproxil fumarate 3D分子结构
CAS号:202138-50-9
Tenofovir Disoproxil fumarate 化学结构 CAS号:202138-50-9
Tenofovir Disoproxil fumarate 3D分子结构 CAS号:202138-50-9
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Tenofovir Disoproxil fumarate 纯度/质量文件 产品仅供科研

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Tenofovir Disoproxil fumarate 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].

Tenofovir Disoproxil fumarate 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
human HeLaT4 cells Cytotoxic assay Cytotoxicity against human HeLaT4 cells by WST-1 assay, CC50=34 μM 21060108

Tenofovir Disoproxil fumarate 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 - -

Tenofovir Disoproxil fumarate 参考文献

[1]Chen JZ, Liao ZW, et al. Efficacy and safety of tenofovir disoproxil fumarate in preventing vertical transmission of hepatitis B in pregnancies with high viral load. Sci Rep. 2017 Jun 23;7(1):4132.

[2]Birkus G, Hitchcock MJ, Cihlar T. Assessment of mitochondrial toxicity in human cells treated with tenofovir: comparison with other nucleoside reverse transcriptase inhibitors. Antimicrob Agents Chemother. 2002 Mar;46(3):716-23.

[3] Murphy RA, Stafford RM, Petrasovits BA, Boone MA, Valentovic MA. Establishment of HK-2 Cells as a Relevant Model to Study Tenofovir-Induced Cytotoxicity. Int J Mol Sci. 2017 Mar 1;18(3):531.

[4]Musumeci G, Bon I, Lembo D, et al. M48U1 and Tenofovir combination synergistically inhibits HIV infection in activated PBMCs and human cervicovaginal histocultures. Sci Rep. 2017;7:41018.

[5]Wahl A, Ho PT, Denton PW, et al. Predicting HIV Pre-exposure Prophylaxis Efficacy for Women using a Preclinical Pharmacokinetic-Pharmacodynamic In Vivo Model. Sci Rep. 2017;7:41098.

Tenofovir Disoproxil fumarate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.57mL

0.31mL

0.16mL

7.87mL

1.57mL

0.79mL

15.74mL

3.15mL

1.57mL

Tenofovir Disoproxil fumarate 技术信息

CAS号202138-50-9
分子式C23H34N5O14P
分子量 635.515
别名 Tenofovir DF;Bis(POC)-PMPA fumarate;Bis(POC)-PMPA;Tenofovir Disoproxil (fumarate);GS 4331 fumarate
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

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)

动物实验配方
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