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| 25mg |
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Purity: ≥98%
Tenofovir Alafenamide fumarate (formerly also known as TAF and GS-7340) is a novel prodrug of tenofovir, which is a potent reverse transcriptase inhibitor [nucleotide reverse transcriptase inhibitor (NRTIs)], it is used for the treatment of HIV and Hepatitis B. By blocking reverse transcriptase, Tenofovir Alafenamide prevent HIV from multiplying and can reduce the amount of HIV in the body. Tenofovir alafenamide is a prodrug that it is inactive in the parent form, and has to be converted to tenofovir diphosphate (TFV-DP) in vivo.
| ln Vitro |
Tenofovir alafenamide fumarate (GS-7340 fumarate) exhibited comparable antiviral activity across all cell types, with a CC50 ranging from 4.7 to 42 μM for MT-4 and MT-2 cells, respectively. The fumarate varied from 5 to 7 nM. A panel of HIV-1 and HIV-2 isolates, comprising HIV-1 M group A to G subtypes and group N and O isolates, were used to assess TAF's antiviral activity. The average EC50 of 3.5 nM was found for TAF among the 29 main HIV-1 isolates tested in PBMC, while the average EC50 of 11.8 nM was found for AZT, the internal control. The average EC50 for AZT was 6.4 nM and for TAF was 1.8 nM for HIV-2 isolates [2].
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| ln Vivo |
The amidate prodrug of tenofovir is called GS-7340 fumarate, or tenofovir alafenamide fumarate. It has better plasma stability and good oral bioavailability when compared to tenofovir disoproxil fumarate (TDF) [1].
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| References |
[1]. Babusis D, et al. Mechanism for effective lymphoid cell and tissue loading following oral administration of nucleotide prodrug GS-7340. Mol Pharm. 2013 Feb 4;10(2):459-66.
[2]. Ruane PJ, et al. Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of tenofovir alafenamide as 10-day monotherapy in HIV-1-positive adults. J Acquir Immune Defic Syndr. 2013 Aug 1;63(4):449-55. |
| Molecular Formula |
C25H33N6O9P
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|---|---|
| Molecular Weight |
593.55
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| CAS # |
379270-38-9
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| Related CAS # |
Tenofovir alafenamide;379270-37-8
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| SMILES |
C[C@@H](C(OC(C)C)=O)N[P@@](OC1=CC=CC=C1)(CO[C@@H](CN2C=NC3=C(N=CN=C23)N)C)=O.O=C(/C=C/C(O)=O)O
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| InChi Key |
MEJAFWXKUKMUIR-WIUYAKJJSA-N
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| InChi Code |
InChI=1S/C21H29N6O5P.C4H4O4/c1-14(2)31-21(28)16(4)26-33(29,32-17-8-6-5-7-9-17)13-30-15(3)10-27-12-25-18-19(22)23-11-24-20(18)27;5-3(6)1-2-4(7)8/h5-9,11-12,14-16H,10,13H2,1-4H3,(H,26,29)(H2,22,23,24);1-2H,(H,5,6)(H,7,8)/b;2-1+/t15-,16+,33?;/m1./s1
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| Chemical Name |
(S)-isopropyl 2-(((S)-((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate fumarate
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| Synonyms |
GS734; GS-734; GS 734; GS 7340; GS-7340; GS7340; TAF; Tenofovir alafenamide fumarate; trade name: Genvoya.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 36 mg/mL (~60.76 mM)
H2O : ≥ 25 mg/mL (~42.19 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 6.67 mg/mL (11.26 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6848 mL | 8.4239 mL | 16.8478 mL | |
| 5 mM | 0.3370 mL | 1.6848 mL | 3.3696 mL | |
| 10 mM | 0.1685 mL | 0.8424 mL | 1.6848 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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