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Tenofovir Disoproxil Fumarate

Catalog No. T2409L   CAS 202138-50-9
Synonyms: GS-1278 Disoproxil Fumarate, Tenofovir DF

Tenofovir Disoproxil Fumarate (GS-1278 Disoproxil Fumarate) is a pro-drug, fumaric acid salt form of tenofovir, a nucleoside reverse transcriptase inhibitor analog of adenosine. Tenofovir disoproxil fumarate is prescribed to treat HIV and chronic hepatitis B virus (HBV) in adults.

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Tenofovir Disoproxil Fumarate Chemical Structure
Tenofovir Disoproxil Fumarate, CAS 202138-50-9
Pack Size Availability Price/USD Quantity
10 mg In stock $ 46.00
25 mg In stock $ 68.00
50 mg In stock $ 92.00
100 mg In stock $ 126.00
200 mg In stock $ 171.00
500 mg In stock $ 252.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.86%
Purity: 99.16%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Tenofovir Disoproxil Fumarate (GS-1278 Disoproxil Fumarate) is a pro-drug, fumaric acid salt form of tenofovir, a nucleoside reverse transcriptase inhibitor analog of adenosine. Tenofovir disoproxil fumarate is prescribed to treat HIV and chronic hepatitis B virus (HBV) in adults.
In vitro Tenofovir shows cytotoxic effects on cell viability in HK-2 cells in MTT assay (IC50: 9.21/2.77 μM at 48/72 h). Tenofovir lowers ATP levels in HK-2 cells. Tenofovir (3.0-28.8 μM) promotes protein carbonylation and oxidative stress in HK-2 cells. In addition, Tenofovir promotes apoptosis induced via mitochondrial damage in HK-2 cells. M48U1 and Tenofovir formulated in 0.25% HEC each inhibits the replication of both X4-tropic HIV-1IIIb and R5-tropic HIV-1BaL in activated PBMCs and inhibits patient-derived HIV-1 isolates and several laboratory strains. Aforesaid mixture exhibits synergistic antiretroviral activity against infection with R5-tropic HIV-1BaL and is not toxic to PBMCs.
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.
Kinase Assay HAT and HDAC Activity Assays :After homogenization of cardiac tissues, nucleoproteins are extracted using a Nuclear Extract Kit according to the manufacturer's instructions. HAT and HDAC activities of the nuclear protein extracts are determined using a colorimetric assay included in the HAT and HDAC assay kits.
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.
Synonyms GS-1278 Disoproxil Fumarate, Tenofovir DF
Molecular Weight 635.51
Formula C19H30N5O10P·C4H4O4
CAS No. 202138-50-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 44 mg/mL (69.23 mM)

DMSO: 128 mg/mL (201.41 mM)

TargetMolReferences and Literature

1. Ray AS, et al. Antimicrob Agents Chemother, 2006, 50(10), 3297-3304. 2. Birkus G, et al. Antimicrob Agents Chemother, 2002, 46(3), 716-723. 3. Delaney WE 4th, et al. Antimicrob Agents Chemother, 2006, 50(7), 2471-2477. 4. Cihlar T, et al. Antiviral Res, 2002, 54(1), 37-45. 5. Wahl A, et al. Predicting HIV Pre-exposure Prophylaxis Efficacy for Women using a Preclinical Pharmacokinetic-Pharmacodynamic In Vivo Model. Sci Rep. 2017 Feb 1;7:41098.

TargetMolCitations

1. Wu M, Li M, Liu W, et al.Nucleoporin Seh1 maintains Schwann cell homeostasis by regulating genome stability and necroptosis.Cell Reports.2023, 42(7): 112802.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Viral Compound Library Orally Active Compound Library Pediatric Drug Library Anti-Cancer Compound Library FDA-Approved Drug Library Immunology/Inflammation Compound Library FDA-Approved & Pharmacopeia Drug Library

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Keywords

Tenofovir Disoproxil Fumarate 202138-50-9 Microbiology/Virology Proteases/Proteasome Reverse Transcriptase HIV Protease HBV Hepatitis B virus HIV GS-1278 Disoproxil Fumarate GS 4331 Inhibitor GS4331 Tenofovir DF GS-4331 inhibit Tenofovir Disoproxil Bis(POC)-PMPA Human immunodeficiency virus inhibitor

 

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