替诺福韦一水合物  99.99%

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包装规格:1g 5g 25g 100g in glass bottle 500g in poly bottle
溶解性:溶于DMSO(≥ 6 mg/mL)
产品描述:基本信息 产品编号:T10599 产品名称:Tenofovir hydrate CAS: 206184-49-8   储存条件 粉末 2-8℃ 四年 分子式: C9H14N5O4P.H2O 溶于液体 -80℃ 两年 分子量 305.23     化学名:  (R)-(((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonic acid hydrate   Solubility (25°C)   体外 DMSO Insoluble Ethanol Insoluble Water 10mg/mL (32.76mM) 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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.2762mL 16.3811mL 32.7622mL 5mM 0.6552mL 3.2762mL 6.5524mL 10mM 0.3276mL 1.6381mL 3.2762mL   生物活性 产品描述 一种核苷酸逆转录酶抑制剂,可用于 HIV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 48h 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 15.0mg/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 0.5 mg/kg/day, and (v) a placebo control. The woodchucks are treated daily for 4 weeks andobserved for an additional 12weeks following cessation of drug treatment.
保存条件:2-8℃