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替诺福韦马来酸盐  ≥98%

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包装规格：5mg 10mg in glass bottle
产品描述：基本信息 产品编号：T10662 产品名称：Tenofovir maleate CAS: 1236287-04-9   储存条件 粉末 -20℃ 四年 分子式： C13H18N5O8P 分子量 403.28 化学名：  [(2R)-1-(6-aminopurin-9-yl)propan-2-yl]oxymethylphosphonic acid;(Z)-but-2-enedioic acid   Solubility (25°C)   体外 DMSO   Ethanol   Water   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，有潜力用于艾滋病毒和慢性乙型肝炎的研究。 靶点/IC50 HIV 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 MTTassay, respectively. Tenofovir diminishes ATP levels in HK-2 cells. Tenofovir (3.0 to 28.8μM) increases oxidative stress andprotein carbonylation in HK-2 cells. Furthermore, Tenofovir induces apoptosis in HK-2 cells, and that apoptosis is inducedvia mitochondrial damage. Tenofovir and M48U1 formulated in 0.25% HEC each inhibits the replication of both R5-tropicHIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, and inhibits several laboratory strains and patient-derived HIV-1isolates. The combined formulation of M48U1 and tenofovir in 0.25% HEC exhibits synergistic antiretroviral activity againstinfection 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 duringvaginal HIV challenge in BLT humanized mice. Tenofovir Disoproxil Fumarate (50, 140, 300mg/kg) significantly reduces HIVtransmission in BLT mice. Tenofovir Disoproxil Fumarate (0.5, 1.5, or 5.0mg/kg/day, p.o.) induces a dose-dependentdecline in serum viremia in woodchucks chronically infected with WHV. Tenofovir Disoproxil Fumarate administration is safeand 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 withvehicle or Tenofovir. Following the treatment period, cell viability is assessed using the MTT assay. The MTT assay relies onthe conversion of tetrazolium dye 3-(4,5-dimethlthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) to formazan byNAD(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 intofive 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) TenofovirDisoproxil Fumarate at 0.5mg/kg/day, and (v) a placebo control. The woodchucks are treated daily for 4weeks andobserved for an additional 12weeks following cessation of drug treatment.
保存条件：-20℃

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