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Tenofovir (GS 1278) Disoproxil Fumarate
Catalog No.S1400 Synonyms: Tenofovir DF
For research use only.
Tenofovir Disoproxil Fumarate (GS-1278, Tenofovir DF) 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.
CAS No. 202138-50-9
Selleck's Tenofovir (GS 1278) Disoproxil Fumarate has been cited by 21 publications
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Biological Activity
| Description | Tenofovir Disoproxil Fumarate (GS-1278, Tenofovir DF) 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. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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] |
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Solubility (25°C)
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Chemical Information
| Molecular Weight | 635.51 | ||
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| Formula | C19H30N5O10P.C4H4O4 |
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| CAS No. | 202138-50-9 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | CC(C)OC(=O)OCOP(=O)(COC(C)CN1C=NC2=C(N=CN=C21)N)OCOC(=O)OC(C)C.C(=CC(=O)O)C(=O)O | ||
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Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT03576066 | Completed | Drug: ABI-H0731|Drug: SOC NUC|Drug: Placebo Oral Tablet | Chronic Hepatitis B | Assembly Biosciences | June 11 2018 | Phase 2 |
| NCT03361956 | Completed | Drug: JNJ-56136379|Drug: Placebo|Drug: NA (ETV or TDF) | Hepatitis B | Janssen Sciences Ireland UC | February 13 2018 | Phase 2 |
| NCT02985996 | Completed | Drug: Truvada|Drug: Genvoya | HIV Infections | Emory University|Centers for Disease Control and Prevention | February 6 2017 | Phase 1 |
| NCT03043326 | Recruiting | Drug: Tenofovir Disoproxil Fumarate and Emtricitabine | HIV Prevention | Asociación Civil Impacta Salud y Educación Peru|Gilead Sciences | January 23 2017 | -- |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
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