Tenofovir Disoproxil Fumarate (Tenofovir DF)

Alias: GS4331-05;GS-1278 Disoproxil Fumarate;Tenofovir DF; TDF; GS-4331-05; GS 4331-05; Tenofovir Disoproxil Fumarate; PMPA prodrug; Tenofovir DF; GS-433105;Viread; Bis(POC)-PMPA
Cat No.:V1812 Purity: ≥98%
Tenofovir Disoproxil Fumarate (TDF; GS-433105;Viread;Tenofovir DF), theFumarate salt of tenofovir, belongs to a class of antiretroviral drugs, it inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5-triphosphate and, after incorporation into DNA, by DNA chain termination.
Tenofovir Disoproxil Fumarate (Tenofovir DF) Chemical Structure CAS No.: 202138-50-9
Product category: Reverse Transcriptase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
25mg
50mg
100mg
250mg
500mg
Other Sizes

Other Forms of Tenofovir Disoproxil Fumarate (Tenofovir DF):

  • Tenofovir disoproxil (GS 4331)
  • Tenofovir (GS 1278)
  • Tenofovir maleate (GS 1278)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Tenofovir Disoproxil Fumarate (TDF; GS-433105; Viread; Tenofovir DF), the Fumarate salt of tenofovir, belongs to a class of antiretroviral drugs, it inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5'-triphosphate and, after incorporation into DNA, by DNA chain termination. It is an antiretroviral medication used to prevent and treat HIV/AIDS and to treat chronic hepatitis B. As a prodrug of Tenofovir, 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 HIV-1/2.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
In the MTT experiment, tenofovir exhibits cytotoxic effects on HK-2 cell viability, with IC50 values of 2.77 μM at 48 and 72 hours, respectively. Tenofovir causes HK-2 cells' ATP levels to drop. In HK-2 cells, tenofovir (3.0 to 28.8 μM) elevates protein carbonylation and oxidative stress. Moreover, tenofovir causes HK-2 cells to undergo apoptosis, and this process is brought on by mitochondrial damage[1]. The replication of R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs is inhibited by tenofovir and M48U1, when compounded in 0.25% HEC. Additionally, various laboratory strains and patient-derived HIV-1 isolates are inhibited. Infection with R5-tropic HIV-1BaL is inhibited by the synergistic antiretroviral action of M48U1 and tenofovir coupled in 0.25% HEC, and this formulation is not harmful to PBMCs[2].
ln Vivo
When given to BLT mice (20, 50, 140, or 300 mg/kg), tenofovir Disoproxil fumarate exhibits dose-dependent efficacy in response to a vaginal HIV challenge in BLT humanized mice. In BLT mice, tenofovir Disoproxil fumarate (50, 140, or 300 mg/kg) dramatically lowers HIV transmission[3]. In woodchucks with a chronic WHV infection, tenofovir Disoproxil fumarate (0.5, 1.5, or 5.0 mg/kg/day, po) causes a dose-dependent decrease in serum viremia. The treatment of tenofovir Disoproxil fumarate in the woodchuck model of chronic HBV infection is both safe and effective[4].
Animal Protocol
Dissolved in saline; 30 mg/kg; s.c. injection
Macaques
References
[1]. Murphy RA, et al. Establishment of HK-2 Cells as a Relevant Model to Study Tenofovir-Induced Cytotoxicity. Int J Mol Sci. 2017 Mar 1;18(3)
[2]. Xu P, et al. Combined Medication of Antiretroviral Drugs Tenofovir Disoproxil Fumarate, Emtricitabine, and Raltegravir Reduces Neural Progenitor Cell Proliferation In Vivo and In Vitro. J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692.
[3]. Musumeci G, et al. M48U1 and Tenofovir combination synergistically inhibits HIV infection in activated PBMCs and human cervicovaginal histocultures. Sci Rep. 2017 Feb 1;7:41018
[4]. Wahl A, et al. Predicting HIV Pre-exposure Prophylaxis Efficacy for Women using a Preclinical Pharmacokinetic-Pharmacodynamic In Vivo Model. Sci Rep. 2017 Feb 1;7:41098
[5]. Menne S, Cote PJ, Korba BE, Antiviral effect of oral administration of tenofovir disoproxil fumarate in woodchucks with chronic woodchuck hepatitis virus infection. Antimicrob Agents Chemother. 2005 Jul;49(7):2720-8
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H30N5O10P.C4H4O4
Molecular Weight
635.51
CAS #
202138-50-9
SMILES
P(C([H])([H])O[C@]([H])(C([H])([H])[H])C([H])([H])N1C([H])=NC2=C(N([H])[H])N=C([H])N=C12)(=O)(OC([H])([H])OC(=O)OC([H])(C([H])([H])[H])C([H])([H])[H])OC([H])([H])OC(=O)OC([H])(C([H])([H])[H])C([H])([H])[H].O([H])C(C([H])=C([H])C(=O)O[H])=O
InChi Key
VCMJCVGFSROFHV-WZGZYPNHSA-N
InChi Code
InChI=1S/C19H30N5O10P.C4H4O4/c1-12(2)33-18(25)28-9-31-35(27,32-10-29-19(26)34-13(3)4)11-30-14(5)6-24-8-23-15-16(20)21-7-22-17(15)24;5-3(6)1-2-4(7)8/h7-8,12-14H,6,9-11H2,1-5H3,(H2,20,21,22);1-2H,(H,5,6)(H,7,8)/b;2-1+/t14-;/m1./s1
Chemical Name
9-((R)-2-((Bis(((isopropoxycarbonyl)oxy)methoxy)phosphinyl)methoxy)propyl)adenine, fumarate
Synonyms
GS4331-05;GS-1278 Disoproxil Fumarate;Tenofovir DF; TDF; GS-4331-05; GS 4331-05; Tenofovir Disoproxil Fumarate; PMPA prodrug; Tenofovir DF; GS-433105;Viread; Bis(POC)-PMPA
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 Data
Solubility (In Vitro)
DMSO: 128 mg/mL (201.4 mM)
Water: 10-20 mg/mL (withultrasonic and warming)
Ethanol: 44 mg/mL (69.2 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.5735 mL 7.8677 mL 15.7354 mL
5 mM 0.3147 mL 1.5735 mL 3.1471 mL
10 mM 0.1574 mL 0.7868 mL 1.5735 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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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.

Biological Data
  • Tenofovir Disoproxil Fumarate

    Effects of tenofovir and other NRTIs on mtDNA content in skeletal muscle cells. Antimicrob Agents Chemother. 2002 Mar;46(3):716-23.
  • Tenofovir Disoproxil Fumarate

    Effects of ddC, ddI, and tenofovir on the expression of COX II and COX IV in HepG2 cells. Antimicrob Agents Chemother. 2002 Mar;46(3):716-23.
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