Tenofovir Disoproxil Fumarate

A prodrug of the antiviral tenofovir

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25mg

￥450.00

360.00

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100mg

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1000.00

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货号: ajci14376
CAS: 202138-50-9
别名: 富马酸替诺福韦酯,Tenofovir DF; Bis(POC)-PMPA fumarate; GS 4331 fumarate
分子式: C19H30N5O10P.C4H4O4
分子量: 635.51
纯度: >98%
溶解度: ≥ 31.7755mg/mL in DMSO
储存: Store at -20°C
库存: 现货

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].

参考文献:
[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

Protocol

Cell experiment [1]:
Cell lines	MT-2 cells and PBMCs
Preparation method	The solubility of this compound in DMSO is > 31.8 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.
Reacting condition	0.007 μM or 0.005 μM
Applications	In MT-2 cells and PBMCs, Tenofovir Disoproxil Fumarate inhibited HIV replication with the EC50 values of 0.007 μM and 0.005 μM, respectively. The anti-HIV activity of Tenofovir Disoproxil Fumarate was shown to be 36- to 90-fold greater than that of Tenofovir.
参考文献: [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.