Tenofovir Disoproxil Fumarate

SKU: orb1305528

Description

Tenofovir Disoproxil Fumarate is the fumarate salt prodrug of tenofovir, an adenosine analog functioning as a nucleoside reverse transcriptase inhibitor. It is utilized in research for investigating antiviral mechanisms against HIV-1 and HBV in both cellular and animal models.

Research Area

Infectious Disease & Virology, Protein Biochemistry

Key Properties

• CAS Number: 202138-50-9
• MW: 635.51
• Purity: 99.02%
• Formula: C₁₉H₃₀N₅O₁₀P·C₄H₄O₄
• SMILES: OC(=O)\C=C\C(O)=O.CC(C)OC(=O)OCOP(=O)(CO[C@H](C)Cn1cnc2c(N)ncnc12)OCOC(=O)OC(C)C
• Target: Reverse Transcriptase,HBV,HIV Protease
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.15 mM);H2O:< 1 mg/mL (slightly soluble);Ethanol:44 mg/mL (69.24 mM);DMSO:50 mg/mL (78.68 mM)

Bioactivity

• In Vivo:
  Tenofovir Disoproxil Fumarate (20/50/140/300 mg/kg) administered to BLT mice, shows dose-dependent activity during vaginal HIV challenge in BLT humanized mice. Tenofovir Disoproxil Fumarate (50/140/300 mg/kg) obviously lowers HIV transmission in BLT mice. Tenofovir Disoproxil Fumarate (0.5/1.5/5.0 mg/kg/day, p.o.) promotes a dose-dependent decline in serum viremia in woodchucks chronically infected with WHV. Tenofovir Disoproxil Fumarate administration is safe and effective in the woodchuck model of chronic HBV infection.
• In Vitro:
  Tenofovir demonstrates cytotoxic effects on HK-2 cell viability in the MTT assay (IC50: 9.21/2.77 μM at 48/72 hours), reduces ATP levels, induces protein carbonylation, oxidative stress (3.0-28.8 μM), and promotes apoptosis via mitochondrial damage. Tenofovir and M48U1 in 0.25% HEC each inhibit X4-tropic HIV-1IIIb and R5-tropic HIV-1BaL replication in activated PBMCs, patient-derived HIV-1 isolates, and lab strains. This combination shows synergistic antiretroviral activity against R5-tropic HIV-1BaL without PBMC toxicity.
• Cell Research:
  Cells are plated into 48-well tissue culture plates (39,000 cells/mL) and allowed to grow for 48 h followed by treatment with vehicle or Tenofovir. Following the treatment period, cell viability is assessed using the MTT assay. The MTT assay relies on the conversion of tetrazolium dye 3-(4,5-dimethlthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) to formazan by NAD(P)H-dependent oxidoreductases.
• Animal Research:
  Tenofovir Disoproxil Fumarate is prepared in a placebo control. Twenty adult chronic WHV carrier woodchucks are stratified equally by age, sex, body weight, and serum GGT activity into five treatment groups consisting of four animals each: (i) Tenofovir Disoproxil Fumarate at 15.0 mg/kg once per day, (ii) Tenofovir Disoproxil Fumarate at 5.0 mg/kg/day, (iii) Tenofovir Disoproxil Fumarate at 1.5 mg/kg/day, (iv) Tenofovir Disoproxil Fumarate at 0.5 mg/kg/day, and (v) a placebo control. The woodchucks are treated daily for 4 weeks and observed for an additional 12 weeks following cessation of drug treatment.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Bis(POC)-PMPA, Hepatitis B virus, HBV, Inhibitor, Human immunodeficiency virus, HIVProtease, HIV Protease, HIV reverse transcriptase, HIV, GS4331, GS-4331, GS-1278 Disoproxil Fumarate, GS 4331, inhibit, Tenofovir Disoproxil, Tenofovir Disoproxil Fumarate, Tenofovir DF, ReverseTranscriptase, Reverse Transcriptase

Compound Identifiers

PubChem CID

6398764