Tenofovir Disoproxil Fumarate (Synonyms: Bis(POC)-PMPA) |
| رقم الكتالوجGC15067 |
Tenofovir Disoproxil fumarate هو مثبط للنيوكليوتيدات المنتسخة العكسية يستخدم لعلاج فيروس نقص المناعة البشرية والتهاب الكبد المزمن ب
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 202138-50-9
Sample solution is provided at 25 µL, 10mM.
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Tenofovir disoproxil fumarate is a nucleotide reverse transcriptase inhibitor that inhibits the replication of human immunodeficiency virus (HIV) in MT-2 cells and PBMC with the half maximal effective concentration EC50 values of 0.007 μmol/L and 0.005 μmol/L [1].
Shortly upon administration, tenofovir disoproxil fumarate rapidly goes through esterase hydrolysis removing the two ester groups and yielding tenofovir, which is a nucleotide analogue with anti-viral activity against retroviruses including HIV-1, HIV-2 and hepadnaviruses. Tenofovir is phosphorylated by cellular nucleotide kinase and adenylate kinase and eventually converted into its active anabolite tenofovir diphosphate, which inhibits HIV-1 reverse transcriptase and terminates the growing DNA chain [2].
References:
[1] Fung HB, Stone EA, Piacenti FJ. Tenofovir disoproxil fumarate: a nucleotide reverse transcriptase inhibitor for the treatment of HIV infection. Clin Ther. 2002 Oct;24(10):1515-48.
[2] Brian P. Kearney, John F. Flaherty, Jaymin Shah. Tenofovir Disoproxil Fumarate. Clinical Pharmacokinetics. August 2004, Volume 43, Issue 9, pp 595-612
| Cell experiment [1]: | |
|
Cell lines |
MT-2 cells and PBMCs |
|
Preparation method |
The solubility of this compound in DMSO is > 31.8 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
|
Reacting condition |
0.007 μM or 0.005 μM |
|
Applications |
In MT-2 cells and PBMCs, Tenofovir Disoproxil Fumarate inhibited HIV replication with the EC50 values of 0.007 μM and 0.005 μM, respectively. The anti-HIV activity of Tenofovir Disoproxil Fumarate was shown to be 36- to 90-fold greater than that of Tenofovir. |
|
References: [1]. Fung HB, Stone EA, Piacenti FJ. Tenofovir disoproxil fumarate: a nucleotide reverse transcriptase inhibitor for the treatment of HIV infection. Clin Ther. 2002 Oct;24(10):1515-48. | |
| Cas No. | 202138-50-9 | SDF | |
| المرادفات | Bis(POC)-PMPA | ||
| Chemical Name | [[(2R)-1-(6-aminopurin-9-yl)propan-2-yl]oxymethyl-(propan-2-yloxycarbonyloxymethoxy)phosphoryl]oxymethyl propan-2-yl carbonate;(E)-but-2-enedioic acid | ||
| Canonical SMILES | CC(C)OC(=O)OCOP(=O)(COC(C)CN1C=NC2=C1N=CN=C2N)OCOC(=O)OC(C)C.C(=CC(=O)O)C(=O)O | ||
| Formula | C19H30N5O10P.C4H4O4 | M.Wt | 635.51 |
| الذوبان | ≥ 31.7755mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5735 mL | 7.8677 mL | 15.7354 mL |
| 5 mM | 314.7 μL | 1.5735 mL | 3.1471 mL |
| 10 mM | 157.4 μL | 786.8 μL | 1.5735 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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