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替诺福韦酯  98.2%

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包装规格：1g 5g 25g 100g 500g in poly bottle
溶解性：溶于DMSO（≥ 38 mg/mL)
产品描述：基本信息 产品编号：T10589 产品名称：Tenofovir (Disoproxil) CAS: 201341-05-1 储存条件 粉末 -20℃ 四年     分子式： C19H30N5O10P 溶于液体 -80℃ 两年 分子量 519.44 -20℃ 一个月 化学名：  9-((R)-2-((Bis(((isopropoxycarbonyl)oxy)methoxy)phosphinyl)methoxy)propyl)adenine   Solubility (25°C)   体外 DMSO 100mg/mL (192.51mM) Ethanol ''100mg/mL Water Insoluble 体内 现配现用   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   生物活性 产品描述 一种核苷酸逆转录酶抑制剂，有潜力用于艾滋病和慢性乙型肝炎的研究。 靶点/IC50 Reverse Transcriptase ()   体外研究 Tenofovir shows cytotoxic effects on cell viability in HK-2 cells, with IC50 values of 9.21 and 2.77μM at 48 and 72h in MTT assay, respectively. Tenofovir diminishes ATP levels in HK-2 cells. Tenofovir (3.0 to 28.8μM) increases oxidative stress and protein carbonylation in HK-2 cells. Furthermore, Tenofovir induces apoptosis in HK-2 cells, and that apoptosis is induced via mitochondrial damage. Tenofovir and M48U1 formulated in 0.25% HEC each inhibits the replication of both R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, and inhibits several laboratory strains and patient-derived HIV-1 isolates. The combined formulation of M48U1 and tenofovir in 0.25% HEC exhibits synergistic antiretroviral activity against infection with R5-tropic HIV-1BaL, and is not toxic to PBMCs. 体内研究 Tenofovir Disoproxil Fumarate (20, 50, 140, or 300mg/kg) administered to BLT mice, shows dose dependent activity during vaginal HIV challenge in BLT humanized mice. Tenofovir Disoproxil Fumarate (50, 140, 300mg/kg) significantly reduces HIV transmission in BLT mice. Tenofovir Disoproxil Fumarate (0.5, 1.5, or 5.0mg/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.   推荐实验方法(仅供参考) 细胞实验:   Cell Assay 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:   Animal Administration 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 5.0mg/kg/day, (iii) Tenofovir Disoproxil Fumarate at 1.5mg/kg/day, (iv) Tenofovir Disoproxil Fumarate at 0.5mg/kg/day, and (v) a placebo control. The woodchucks are treated daily for 4weeks and observed for an additional 12 weeks following cessation of drug treatment.
保存条件：-20℃

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