| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| Other Sizes |
|
Purity: ≥98%
Tenofovir Alafenamide hemifumarate (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 hemifumarate (GS-7340 hemifumarate) exhibited comparable antiviral activity across all cell types, with CC50s ranging from 4.7 to 42 μM, respectively, for MT-4 and MT-2 cells. 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].
|
|---|---|
| ln Vivo |
The amidate prodrug of tenofovir, tenofovir alafenamide hemifumarate (GS-7340 hemifumarate), is comparable to tenofovir disoproxil fumarate. (TDF) has enhanced plasma stability and a favorable oral bioavailability profile [1].
|
| 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. |
| Molecular Formula |
C46H62N12O14P2
|
|---|---|
| Molecular Weight |
1069.0195
|
| CAS # |
1392275-56-7
|
| Related CAS # |
Tenofovir alafenamide;379270-37-8
|
| SMILES |
O=C(O)/C=C/C(O)=O.C[C@H](N[P@@](OC1=CC=CC=C1)(CO[C@H](C)CN2C=NC3=C(N)N=CN=C23)=O)C(OC(C)C)=O.C[C@H](N[P@@](OC4=CC=CC=C4)(CO[C@H](C)CN5C=NC6=C(N)N=CN=C56)=O)C(OC(C)C)=O
|
| InChi Key |
SVUJNSGGPUCLQZ-FQQAACOVSA-N
|
| InChi Code |
InChI=1S/2C21H29N6O5P.C4H4O4/c2*1-14(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)275-3(6)1-2-4(7)8/h2*5-9,11-12,14-16H,10,13H2,1-4H3,(H,26,29)(H2,22,23,24)1-2H,(H,5,6)(H,7,8)/b2-1+/t2*15-,16+,33+/m11./s1
|
| Chemical Name |
isopropyl ((S)-((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)-L-alaninate hemifumarate
|
| Synonyms |
GS734 GS-734 GS 734 GS 7340 GS-7340 GS7340 TAF Tenofovir alafenamide hemifumarate Tenofovir alafenamide fumarate
(2
|
| 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) |
DMSO : ~50 mg/mL (~93.55 mM)
H2O : ~20 mg/mL (~37.42 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.68 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (4.68 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 4.55 mg/mL (8.51 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9354 mL | 4.6772 mL | 9.3544 mL | |
| 5 mM | 0.1871 mL | 0.9354 mL | 1.8709 mL | |
| 10 mM | 0.0935 mL | 0.4677 mL | 0.9354 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