1. Anti-infection
  2. HIV
    Reverse Transcriptase
    HBV

Tenofovir Disoproxil Fumarate (Synonyms: Tenofovir DF)

Cat. No.: HY-13782 Purity: 99.46%
Data Sheet SDS Handling Instructions

Tenofovir Disoproxil Fumarate is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.

For research use only. We do not sell to patients.
Tenofovir Disoproxil Fumarate Chemical Structure

Tenofovir Disoproxil Fumarate Chemical Structure

CAS No. : 202138-50-9

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Description

Tenofovir Disoproxil Fumarate is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.

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
NCT Number Sponsor Condition Start Date Phase
NCT02479880 Gilead Sciences Hepatitis B July 30, 2015 Phase 4
NCT00507507 Gilead Sciences Chronic Hepatitis B September 2007 Phase 2
NCT00352053 Gilead Sciences HIV Infections June 2006 Phase 3
NCT02039362 Hopital Lariboisière Pregnancy|HBV July 2012 Phase 4
NCT01334567 Gilead Sciences Hepatitis B August 2010 Phase 2
NCT00648817 Gilead Sciences HIV Infections July 2006 Phase 4
NCT00036634 Gilead Sciences HIV Infections March 2002 Phase 1|Phase 2
NCT01651403 Gilead Sciences Chronic Hepatitis B Infection December 2012 Phase 3
NCT00078182 National Institute of Allergy and Infectious Diseases (NIAID)|NCHADS - Ministry of Health of Cambodia|Kirby Institute HIV Infections|HIV Seronegativity Phase 2|Phase 3
NCT00528957 Gilead Sciences HIV Infections December 28, 2006 Phase 3
NCT00391638 French National Agency for Research on AIDS and Viral Hepatitis|Gilead Sciences|Roche Pharma AG|French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS) Hepatitis B|HIV Infections January 2007 Phase 2|Phase 3
NCT00024986 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) HIV Infection October 2001 Phase 1
NCT01737359 RFS Pharma, LLC Human Immunodeficiency Virus Infection December 2012 Phase 2
NCT00307489 Gilead Sciences Chronic Hepatitis B March 2006 Phase 2
NCT00106379 Gilead Sciences HIV Infections October 2004 Phase 4
NCT00298363 Gilead Sciences Chronic Hepatitis B April 2006 Phase 2
NCT00647946 Gilead Sciences Lipodystrophy February 2003 Phase 2
NCT00365612 Gilead Sciences|Bristol-Myers Squibb HIV Infections July 2006 Phase 4
NCT01855867 Kenneth H. Mayer, MD|Gilead Sciences|Fenway Community Health Human Immunodeficiency Virus May 2013 Phase 4
NCT00038220 Abbott HIV Infections July 2000 Phase 2
NCT00323544 Gilead Sciences HIV Infections October 2004 Phase 3
NCT00115609 French National Agency for Research on AIDS and Viral Hepatitis HIV Infections|Tuberculosis January 2006 Phase 3
NCT02180438 University of Washington|Clinique des Maladies Infectieuses Ibrahima DIOP Mar/CRCF, Centre Hospitalier Universitaire de Fann|Gilead Sciences HIV-2 Infection September 2014 Phase 4
NCT00043966 Abbott HIV Infections July 2002 Phase 3
NCT00221286 University Hospital, Bonn|Hoffmann-La Roche Chronic Hepatitis B|HIV Infections September 2004 Phase 3
NCT01602822 Kenneth H. Mayer, MD|Bristol-Myers Squibb|Gilead Sciences|Abbott|Fenway Community Health HIV February 2012 Phase 4
NCT00234910 Abbott HIV Infection January 2005 Phase 3
NCT00552240 Boehringer Ingelheim HIV Infections September 2007 Phase 4
NCT00863668 University of Minnesota - Clinical and Translational Science Institute|Merck Sharp & Dohme Corp. HIV Infection|HIV Infections March 2009
NCT00036452 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.5735 mL 7.8677 mL 15.7354 mL
5 mM 0.3147 mL 1.5735 mL 3.1471 mL
10 mM 0.1574 mL 0.7868 mL 1.5735 mL
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

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

References
M.Wt

635.51

Formula

C₂₃H₃₄N₅O₁₄P

CAS No.

202138-50-9

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Tenofovir Disoproxil Fumarate
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