product name Tenofovir Disoproxil Fumarate
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. It is an antiretroviral medication used to prevent and treat HIV/AIDS and to treat chronic hepatitis B. 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 HIV-1/2.
References: Antimicrob Agents Chemother. 2006 Oct;50(10):3297-304; Antimicrob Agents Chemother. 2002 Mar;46(3):716-23.
635.51
Formula
C19H30N5O10P.C4H4O4
CAS No.
202138-50-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 128 mg/mL (201.4 mM)
Water: <1 mg/mL
Ethanol: 44 mg/mL (69.2 mM)
Solubility (In vivo)
Synonyms
GS-1278 Disoproxil Fumarate
other peoduct :
| In Vitro |
In vitro activity: 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. 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. 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. Tenofovir inhibits the proliferation of liver-derived HepG2 cells and normal skeletal muscle cells with CC(50) values of 398 mM and 870 mM, 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 Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Tenofovir (30 mg/kg) completely prevents SIV infection in all macaques without toxicity. Tenofovir treatment reduces plasma viral RNA levels to undetectable, with parallel decreases in the infectivity of plasma and infectious cells in peripheral blood mononuclear cells and cerebrospinal fluid (CSF) and stabilization of CD4+ T-cell numbers. Tenofovir (30 mg/kg, s.c.) completely abrogates HIV infection via intravaginal exposure in pig-tailed macaques. |
| Animal model | Macaques |
| Formulation & Dosage | Dissolved in saline; 30 mg/kg; s.c. injection |
| References | Antivir Ther. 2004 Feb;9(1):57-65; Clin Microbiol Rev. 2003 Oct;16(4):569-96; Antimicrob Agents Chemother. 2006 Oct;50(10):3297-304; Antimicrob Agents Chemother. 2002 Mar;46(3):716-23. |
Integrin Antagonist 4 (hydrochloride)
