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Tenofovir Disoproxil Fumarate

现货
Catalog No.
A1755
抗逆转录制剂(HIV-1 RT 抑制剂)
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 700.00
现货
25mg
¥ 500.00
现货
100mg
¥ 1,500.00
现货

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Background

Tenofovir disoproxil fumarate is a nucleotide reverse transcriptase inhibitor that inhibits the replication of human immunodeficiency virus (HIV) in MT-2 cells and PBMC with the half maximal effective concentration EC50 values of 0.007 μmol/L and 0.005 μmol/L [1].

Shortly upon administration, tenofovir disoproxil fumarate rapidly goes through esterase hydrolysis removing the two ester groups and yielding tenofovir, which is a nucleotide analogue with anti-viral activity against retroviruses including HIV-1, HIV-2 and hepadnaviruses. Tenofovir is phosphorylated by cellular nucleotide kinase and adenylate kinase and eventually converted into its active anabolite tenofovir diphosphate, which inhibits HIV-1 reverse transcriptase and terminates the growing DNA chain [2].

References:
[1] Fung HB, Stone EA, Piacenti FJ. Tenofovir disoproxil fumarate: a nucleotide reverse transcriptase inhibitor for the treatment of HIV infection. Clin Ther. 2002 Oct;24(10):1515-48.
[2] Brian P. Kearney, John F. Flaherty, Jaymin Shah. Tenofovir Disoproxil Fumarate. Clinical Pharmacokinetics. August 2004, Volume 43, Issue 9, pp 595-612

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt635.51
Cas No.202138-50-9
FormulaC19H30N5O10P.C4H4O4
Solubility≥31.7755mg/mL in DMSO
Chemical Name[[(2R)-1-(6-aminopurin-9-yl)propan-2-yl]oxymethyl-(propan-2-yloxycarbonyloxymethoxy)phosphoryl]oxymethyl propan-2-yl carbonate;(E)-but-2-enedioic acid
SDFDownload SDF
Canonical SMILESCC(C)OC(=O)OCOP(=O)(COC(C)CN1C=NC2=C1N=CN=C2N)OCOC(=O)OC(C)C.C(=CC(=O)O)C(=O)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

MT-2细胞和PBMCs

制备方法

在DMSO中的溶解度大于31.8 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

0.007 μM或0.005 μM

实验结果

在MT-2细胞和PBMC中,Tenofovir Disoproxil Fumarate抑制HIV复制,其EC50值分别为0.007 μM和0.005 μM。Tenofovir Disoproxil Fumarate的抗HIV活性比Tenofovir高36 ~ 90倍。

References:

[1]. Fung HB, Stone EA, Piacenti FJ. Tenofovir disoproxil fumarate: a nucleotide reverse transcriptase inhibitor for the treatment of HIV infection. Clin Ther. 2002 Oct;24(10):1515-48.

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