| 名称 | Tenofovir Disoproxil Fumarate |
| 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. |
| 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. |
| 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. |
| 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. |
| 体外活性 | Tenofovir在MTT实验中对HK-2细胞的存活能力表现出细胞毒性效应（IC50: 9.21/2.77 μM在48/72小时）。该化合物降低HK-2细胞中的ATP水平，并在3.0-28.8 μM浓度范围内促进蛋白质羰基化和氧化应激。此外，Tenofovir还通过线粒体损伤促进HK-2细胞的凋亡。在0.25% HEC中配制的M48U1和Tenofovir能够抑制活化的PBMCs中X4-热性HIV-1IIIb与R5-热性HIV-1BaL的复制，并抑制患者源HIV-1分离物及多个实验室株。上述混合物对R5-热性HIV-1BaL感染表现出协同的抗逆转录病毒活性，对PBMCs无毒性。 |
| 体内活性 | Tenofovir Disoproxil Fumarate（20/50/140/300mg/kg）在BLT人源化小鼠的阴道HIV挑战实验中表现出剂量依赖性活性。Tenofovir Disoproxil Fumarate（50/140/300mg/kg）显著降低了BLT小鼠中HIV的传播率。此外，Tenofovir Disoproxil Fumarate（0.5/1.5/5.0 mg/kg/day，p.o.）在慢性感染WHV的旱獭中促进了血清病毒量剂量依赖性下降。Tenofovir Disoproxil Fumarate的应用在慢性HBV感染的旱獭模型中被证明是安全且有效的。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.15 mM), Sonication is recommended.
H2O : < 1 mg/mL (slightly soluble)
Ethanol : 44 mg/mL (69.24 mM), Sonication is recommended.
DMSO : 50 mg/mL (78.68 mM), Sonication is recommended.
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| 关键字 | Tenofovir Disoproxil Fumarate | Tenofovir Disoproxil | ReverseTranscriptase | Reverse Transcriptase | Inhibitor | inhibit | Human immunodeficiency virus | HIVProtease | HIV reverse transcriptase | HIV Protease | HIV | Hepatitis B virus | HBV | GS-4331 | GS4331 | GS 4331 | Bis(POC)-PMPA |
| 相关产品 | Tenofovir | Valproic Acid | Nicotinamide | (-)-Epigallocatechin Gallate | Emtricitabine | Dolutegravir intermediate-1 | Dextran sulfate sodium salt (MW 5000) | Lamivudine | 5-Fluorouracil | Decanedioic acid | Stavudine | Dimethyl fumarate |
| 相关库 | 抑制剂库 | 抗癌上市药物库 | 经典已知活性库 | 已知活性化合物库 | EMA 上市药物库 | FDA 上市药物库 | 抗病毒库 | 免疫/炎症分子化合物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库 | NMPA中国上市药物库 |