Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tenofovir Disoproxil Fumarate (GS-1278 Disoproxil Fumarate) 是一种核苷酸逆转录酶抑制剂,有潜力研究艾滋病和慢性乙型肝炎。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
10 mg | ¥ 397 | 现货 | ||
50 mg | ¥ 843 | 现货 | ||
100 mg | ¥ 1,240 | 现货 | ||
200 mg | ¥ 1,675 | 现货 | ||
500 mg | ¥ 3,355 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 373 | 现货 |
产品描述 | Tenofovir Disoproxil Fumarate (GS-1278 Disoproxil Fumarate) is a pro-drug, fumaric acid salt form of tenofovir, a nucleoside reverse transcriptase inhibitor analog of adenosine. Tenofovir disoproxil fumarate is prescribed to treat HIV and chronic hepatitis B virus (HBV) in adults. |
体外活性 | Tenofovir shows cytotoxic effects on cell viability in HK-2 cells in MTT assay (IC50: 9.21/2.77 μM at 48/72 h). Tenofovir lowers ATP levels in HK-2 cells. Tenofovir (3.0-28.8 μM) promotes protein carbonylation and oxidative stress in HK-2 cells. In addition, Tenofovir promotes apoptosis induced via mitochondrial damage in HK-2 cells. M48U1 and Tenofovir formulated in 0.25% HEC each inhibits the replication of both X4-tropic HIV-1IIIb and R5-tropic HIV-1BaL in activated PBMCs and inhibits patient-derived HIV-1 isolates and several laboratory strains. Aforesaid mixture exhibits synergistic antiretroviral activity against infection with R5-tropic HIV-1BaL and is not toxic to PBMCs. |
体内活性 | Tenofovir Disoproxil Fumarate (20/50/140/300?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) obviously lowers HIV transmission in BLT mice. Tenofovir Disoproxil Fumarate (0.5/1.5/5.0 mg/kg/day, p.o.) promotes 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. |
激酶实验 | HAT and HDAC Activity Assays :After homogenization of cardiac tissues, nucleoproteins are extracted using a Nuclear Extract Kit according to the manufacturer's instructions. HAT and HDAC activities of the nuclear protein extracts are determined using a colorimetric assay included in the HAT and HDAC assay kits. |
细胞实验 | Cells are plated into 48-well tissue culture plates (39,000 cells/mL) and allowed to grow for 48 h followed by treatment with vehicle or Tenofovir. Following the treatment period, cell viability is assessed using the MTT assay. The MTT assay relies on the conversion of tetrazolium dye 3-(4,5-dimethlthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) to formazan by NAD(P)H-dependent oxidoreductases. |
动物实验 | Tenofovir Disoproxil Fumarate is prepared in a placebo control. Twenty adult chronic WHV carrier woodchucks are stratified equally by age, sex, body weight, and serum GGT activity into five treatment groups consisting of four animals each: (i) Tenofovir Disoproxil Fumarate at 15.0 mg/kg once per day, (ii) Tenofovir Disoproxil Fumarate at 5.0 mg/kg/day, (iii) Tenofovir Disoproxil Fumarate at 1.5 mg/kg/day, (iv) Tenofovir Disoproxil Fumarate at 0.5 mg/kg/day, and (v) a placebo control. The woodchucks are treated daily for 4 weeks and observed for an additional 12 weeks following cessation of drug treatment. |
别名 | GS-1278 Disoproxil Fumarate, Tenofovir DF, 富马酸替诺福韦酯 |
分子量 | 635.51 |
分子式 | C19H30N5O10P·C4H4O4 |
CAS No. | 202138-50-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 44 mg/mL (69.23 mM)
DMSO: 128 mg/mL (201.41 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.5735 mL | 7.8677 mL | 15.7354 mL | 39.3385 mL |
5 mM | 0.3147 mL | 1.5735 mL | 3.1471 mL | 7.8677 mL | |
10 mM | 0.1574 mL | 0.7868 mL | 1.5735 mL | 3.9338 mL | |
20 mM | 0.0787 mL | 0.3934 mL | 0.7868 mL | 1.9669 mL | |
50 mM | 0.0315 mL | 0.1574 mL | 0.3147 mL | 0.7868 mL | |
DMSO | 100 mM | 0.0157 mL | 0.0787 mL | 0.1574 mL | 0.3934 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Tenofovir Disoproxil Fumarate 202138-50-9 Microbiology/Virology Proteases/Proteasome HBV HIV Protease Reverse Transcriptase Hepatitis B virus HIV GS-1278 Disoproxil Fumarate GS 4331 Inhibitor GS4331 Tenofovir DF 富马酸替诺福韦酯 GS-4331 inhibit Tenofovir Disoproxil Bis(POC)-PMPA Human immunodeficiency virus inhibitor