1. Anti-infection
  2. Reverse Transcriptase
    HIV
    HBV
  3. Tenofovir

Tenofovir (Synonyms: GS 1278; PMPA; TDF)

Cat. No.: HY-13910 Purity: 99.81%
Handling Instructions

Tenofovir (GS 1278) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV).

For research use only. We do not sell to patients.

Tenofovir Chemical Structure

Tenofovir Chemical Structure

CAS No. : 147127-20-6

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Based on 5 publication(s) in Google Scholar

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Description

Tenofovir (GS 1278) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV)[1].

In Vitro

Tenofovir shows cytotoxic effects on cell viability in HK-2 cells, with IC50 values of 9.21 and 2.77 μM at 48 and 72 h in MTT assay, respectively. Tenofovir diminishes ATP levels in HK-2 cells. Tenofovir (3.0 to 28.8 μM) increases oxidative stress and protein carbonylation in HK-2 cells. Furthermore, Tenofovir induces apoptosis in HK-2 cells, and that apoptosis is induced via mitochondrial damage[1]. Tenofovir and M48U1 formulated in 0.25% HEC each inhibits the replication of both R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, and inhibits several laboratory strains and patient-derived HIV-1 isolates. The combined formulation of M48U1 and tenofovir in 0.25% HEC exhibits synergistic antiretroviral activity against infection with R5-tropic HIV-1BaL, and is not toxic to PBMCs[2].

In Vivo

Tenofovir Disoproxil Fumarate (20, 50, 140, or 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) significantly reduces HIV transmission in BLT mice[3]. Tenofovir Disoproxil Fumarate (0.5, 1.5, or 5.0 mg/kg/day, p.o.) induces 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[4].

Clinical Trial
Molecular Weight

287.21

Formula

C₉H₁₄N₅O₄P

CAS No.

147127-20-6

SMILES

C[[email protected]@H](OCP(O)(O)=O)CN1C=NC2=C(N)N=CN=C12

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 2 mg/mL (6.96 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4818 mL 17.4089 mL 34.8177 mL
5 mM 0.6964 mL 3.4818 mL 6.9635 mL
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

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[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

TenofovirGS 1278PMPATDFGS1278GS-1278Reverse TranscriptaseHIVHBVHuman immunodeficiency virusHepatitis B virusInhibitorinhibitorinhibit

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