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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。
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 | 库存 | 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 x 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。 |
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 | 富马酸替诺福韦酯, Tenofovir DF, GS-1278 Disoproxil Fumarate |
分子量 | 635.51 |
分子式 | C19H30N5O10P·C4H4O4 |
CAS No. | 202138-50-9 |
Smiles | OC(=O)\C=C\C(O)=O.CC(C)OC(=O)OCOP(=O)(CO[C@H](C)Cn1cnc2c(N)ncnc12)OCOC(=O)OC(C)C |
密度 | 1.45 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 44 mg/mL (69.23 mM) DMSO: 50 mg/mL (78.68 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
Ethanol/DMSO
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