中文名称: 替诺福韦酯
英文名称: Tenofovir (Disoproxil)
CAS No: 201341-05-1
分子式: C19H30N5O10P
分子量: 519.44
T10589 替诺福韦酯 ≥98% (psaitong)
包装规格:
1g 5g 25g in glass 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℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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摩尔浓度计算公式

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稀释公式

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  • 计算结果

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):