| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 5g |
|
||
| Other Sizes |
|
Purity: ≥98%
Tenofovir Alafenamide (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 |
The antiviral activity of tenofovir alafenamide (GS-7340) ranged from 5 to 7 nM in all cell types, although the CC50 for MT-4 and MT-2 cells varied from 4.7 to 42 μM. A panel of HIV-1 and HIV-2 isolates, comprising HIV-1 M group subtypes A to G and group N and O isolates, were used to assess the antiviral activity of TAF. The average TAF EC50 was 3.5 nM, with a range of 0.1 to 12 nM. In contrast, the average EC50 of AZT, the internal control, was 11.8 nM for 29 main HIV-1 strains evaluated in PBMC. TAF's average EC50 for HIV-2 isolates is 1.8 nM, while AZT's average EC50 is 6.4 nM [2].
|
||
|---|---|---|---|
| ln Vivo |
When compared to Tenofovir disoproxil fumarate (TDF), Tenofovir alafenamide (GS-7340) hemifumarate, the amidate prodrug of Tenofovir, exhibits better oral bioavailability and plasma stability [1].
|
||
| Animal Protocol |
|
||
| 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 |
C21H29N6O5P
|
|
|---|---|---|
| Molecular Weight |
476.47
|
|
| CAS # |
379270-37-8
|
|
| Related CAS # |
Tenofovir alafenamide fumarate;379270-38-9;Tenofovir alafenamide hemifumarate;1392275-56-7
|
|
| SMILES |
[P@](C([H])([H])OC([H])(C([H])([H])[H])C([H])([H])N1C([H])=NC2=C(N([H])[H])N=C([H])N=C12)(N([H])C([H])(C(=O)OC([H])(C([H])([H])[H])C([H])([H])[H])C([H])([H])[H])(=O)OC1C([H])=C([H])C([H])=C([H])C=1[H]
|
|
| InChi Key |
LDEKQSIMHVQZJK-AZFZMOAFSA-N
|
|
| InChi Code |
InChI=1S/C21H29N6O5P/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/h5-9,11-12,14-16H,10,13H2,1-4H3,(H,26,29)(H2,22,23,24)/t15-,16+,33?/m1/s1
|
|
| Chemical Name |
(S)-isopropyl 2-(((S)-((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate
|
|
| Synonyms |
|
|
| 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)
|
| Solubility (In Vitro) |
|
|---|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0988 mL | 10.4938 mL | 20.9877 mL | |
| 5 mM | 0.4198 mL | 2.0988 mL | 4.1975 mL | |
| 10 mM | 0.2099 mL | 1.0494 mL | 2.0988 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.
|
|---|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
