Tenofovir Alafenamide Hemifumarate Datasheet DC Chemicals
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Cat.No DC9294
Name Tenofovir Alafenamide Hemifumarate

Chemical Properties

CAS 1392275-56-7
Formula 2[C21H29N6O5P].C4H4O4
MW 1069.00408
Storage 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological activity

Description CAS NO.：1392275-56-7
Product Name：GS7340（Tenofovir Alafenamide Fumarate）
Synonyms：GS7340（Tenofovir Alafenamide Fumarate）;GS-7340 Hemifumarate;Tenofovir alafenamide fumarate, 2:1;L-Alanine,N-((S)-(((1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy)methyl)phenoxyphosphinyl)-,1-methylethyl ester,(2E)-2-butenedioate (2:1);GS-7340-03;1-Methylethyl N-((S)-(((1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy)methyl)phenoxyphosphinoyl)-L-alaninate,(2E)-2-butenedioate;(E)-but-2-enedioic acid,propan-2-yl (2S)-2-[[1-(6-aminopurin-9-yl)propan-2-yloxymethyl-phenoxyphosphoryl]amino]propanoate;(S)-Isopropyl 2-(((S)-((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate fumarate(2:1);Tenofovir Alafenamide Fumarate;Tenofovir alafenamide fumarate(2:1);GS7340 hemifumarate;Tenofovir alafenamide hemifumarate;N-[(S)-[[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]phenoxyphosphinyl]-L-alanine 1-methylethyl ester (2E)-2-butenedioate (2:1);GS 7340-03;GS-7340 (hemifumarate)
EINEC:
Molecular Formula：2[C21H29N6O5P].C4H4O4
Molecular Weight：1069.00408
Target:
In Vivo Tenofovir alafenamide (GS-7340) is an amidate prodrug of Tenofovir with good oral bioavailability and increases plasma stability compared to Tenofovir disoproxil fumarate (TDF) [1].
In Vitro Tenofovir alafenamide (GS-7340) 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].
Kinase Assay
Cell Assay
Animal Administration

References

[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.
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