Tenofovir Disoproxil Fumarate

Catalog No.S1400 Batch:S140003

Technical Data

Formula

C₁₉H₃₀N₅O₁₀P.C₄H₄O₄

Molecular Weight

635.51

CAS No.

202138-50-9

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (157.35 mM)

Ethanol

4 mg/mL (6.29 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	2.5mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Tenofovir Disoproxil Fumarate 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.

Targets

HIV reverse transcriptase ^[1]
(Cell-free assay)

In vitro

Tenofovir is eliminated from systemic circulation renally through a combination of glomerular filtration and active tubular secretion. Tenofovir is not a substrate for human organic cation transporter type 1 (hOCT1) or hOCT2. Tenofovir accumulates to fivefold lower levels in MRP4-overexpressing cells, and its accumulation could be increased by an MRP inhibitor. ^[1] Tenofovir produces no significant changes in mitochondrial DNA (mtDNA) levels in human hepatoblastoma (HepG2) cells, skeletal muscle cells (SkMCs), or renal proximal tubule epithelial cells. Tenofovir elevates lactate production by less than 20% in HepG2 cells or SkMCs. ^[2] Tenofovir is efficiently phosphorylated to tenofovir diphosphate (TFV-DP) in both HepG2 cells and primary human hepatocytes. Tenofovir has a 50% effective concentration of 1.1 mM against HBV in cell-based assays, and potency is improved > 50-fold by the addition of bis-isoproxil progroups. Tenofovir has previously demonstrated full activity against lamivudine-resistant HBV in vitro and clinically. ^[3] Tenofovir inhibits the proliferation of liver-derived HepG2 cells and normal skeletal muscle cells with CC(50) values of 398 μM and 870 μM, respectively. Tenofovir shows substantially weaker effects on proliferation and viability of renal proximal tubule epithelial cells than cidofovir, a related nucleotide analog with the potential to induce renal tubular dysfunction. ^[4]

Protocol (from reference)

Cell Assay:^{^[5]}	Cell lines VK2 cells Concentrations 450 μM or 1,350 μM Incubation Time 15 min to 12 h Method VK2 cells were exposed to TDF (90 μM or 450 μM) and TFV (450 μM or 1,350 μM) in serum-free RPMI 1640 at 37°C for 15 min to 12 h. At different times postexposure, cells were washed with ice-cold PBS and metabolites were extracted overnight in 70% (vol/vol) methanol, followed by centrifugation at 18,000 × g for 10 min at 4°C.
Animal Study:^{^[6]}	Animal Models BALB/c mice Dosages 50, 500, or 1000 mg/kg Administration oral administration

Cell Assay:^{^[5]}

Cell lines
VK2 cells
Concentrations
450 μM or 1,350 μM
Incubation Time
15 min to 12 h
Method
VK2 cells were exposed to TDF (90 μM or 450 μM) and TFV (450 μM or 1,350 μM) in serum-free RPMI 1640 at 37°C for 15 min to 12 h. At different times postexposure, cells were washed with ice-cold PBS and metabolites were extracted overnight in 70% (vol/vol) methanol, followed by centrifugation at 18,000 × g for 10 min at 4°C.

Animal Study:^{^[6]}

Animal Models
BALB/c mice
Dosages
50, 500, or 1000 mg/kg
Administration
oral administration

References

+ Expand

Customer Product Validation

: Data from [Data independently produced by , , Sci Transl Med, 2014, 6(262): 262ra157 ]

Selleck's Tenofovir Disoproxil Fumarate has been cited by 27 publications

IKAROS expression drives the aberrant metabolic phenotype of macrophages in chronic HIV infection [ Clin Immunol, 2024, 260:109915]	PubMed: 38286172
Broad synergistic antiviral efficacy between a novel elite controller-derived dipeptide and antiretrovirals against drug-resistant HIV-1 [ Front Cell Infect Microbiol, 2024, 14:1334126]	PubMed: 38915925
Preclinical Antiviral and Safety Profiling of the HBV RNA Destabilizer AB-161 [ Viruses, 2024, 16(3)323]	PubMed: 38543689
Acute antagonism in three-drug combinations for vaginal HIV prevention in humanized mice [ Sci Rep, 2023, 13(1):4594]	PubMed: 36944714
Establishment and characterization of a new cell culture system for hepatitis B virus replication and infection [ Virol Sin, 2022, S1995-820X(22)00081-5]	PubMed: 35568375
Reduction of CD8 T cell functionality but not inhibitory capacity by integrase inhibitors [ J Virol, 2022, JVI0173021]	PubMed: 35019724
Female Genital Fibroblasts Diminish the In Vitro Efficacy of PrEP against HIV [ Viruses, 2022, 14(8)1723]	PubMed: 36016345
Impaired differentiation of small airway basal stem/progenitor cells in people living with HIV [ Sci Rep, 2022, 12(1):2966]	PubMed: 35194053
Preclinical characterization of AB-506, an inhibitor of HBV replication targeting the viral core protein [ Antiviral Res, 2021, 197:105211]	PubMed: 34826506
People with HIV-1 demonstrate type 1 interferon refractoriness associated with upregulated USP18 [ J Virol, 2021, JVI.01777-20]	PubMed: 33658340

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.