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Tenofovir alafenamide hemifumarate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tenofovir alafenamide hemifumarate图片
CAS NO:1392275-56-7
规格:98%
分子量:534.5
包装与价格:
包装价格(元)
200mg电议
500mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) 是 Tenofovir 的前体,Tenofovir 是一种 HIV-1 核苷酸逆转录酶抑制剂。
CAS:1392275-56-7
分子式:C21H29N6O5P.1/2 C4H4O4
分子量:534.5
纯度:98%
存储:Store at -20°C

Background:

Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor. HIV-1, NRTIs[1]


Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) antiviral activities are similar across all cell types, ranging from 5 to 7 nM, while the CC50 varies from 4.7 to 42 μM for MT-4 and MT-2 cells, respectively. The antiviral activity of TAF is evaluated against a panel of HIV-1 and HIV-2 isolates, including HIV-1 group M subtypes A to G, as well as group N and O isolates. Overall, for the 29 primary HIV-1 isolates tested in PBMCs, TAF EC50s range from 0.1 to 12 nM, with a mean EC50 of 3.5 nM compared to a mean EC50 of 11.8 nM for AZT, which is used as an internal control. For the HIV-2 isolates, the mean EC50s are 1.8 nM for TAF and 6.4 nM for AZT[2].


Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an amidate prodrug of Tenofovir with good oral bioavailability and increases plasma stability compared to Tenofovir disoproxil fumarate (TDF) [1].


[1]. Birkus G, et al. Intracellular Activation of Tenofovir Alafenamide and the Effect of Viral and Host Protease Inhibitors. Antimicrob Agents Chemother. 2015 Oct 26;60(1):316-22. [2]. Callebaut C, et al. In Vitro Virology Profile of Tenofovir Alafenamide, a Novel Oral Prodrug of Tenofovir with Improved Antiviral Activity Compared to That of Tenofovir Disoproxil Fumarate. Antimicrob Agents Chemother. 2015 Oct;59(10):5909-16.