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Tenofovir alafenamide hemifumarate

Cat. No. M20783
Tenofovir alafenamide hemifumarate Structure
Synonym:

TAF hemifumarate, GS-7340 hemifumarate

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Biological Activity

Tenofovir alafenamide (TAF, GS-7340) hemifumarate is a prodrug of tenofovir but results in significantly higher intracellular tenofovir concentrations and lower serum levels. Tenofovir alafenamide is a novel nucleotide reverse transcriptase inhibitor for the treatment of HIV-1 infection.

Chemical Information
Molecular Weight 1069
Formula C46H62N12O14P2
CAS Number 1392275-56-7
Solubility (25°C) DMSO 100 mg/mL
Water 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Doris Zane, et al. Microbiol Spectr. A 28-Day Toxicity Study of Tenofovir Alafenamide Hemifumarate by Subcutaneous Infusion in Rats and Dogs

[2] Jian-Wei Wang, et al. Int J Mol Sci. On the Single-Crystal Structure of Tenofovir Alafenamide Mono-Fumarate: A Metastable Phase Featuring a Mixture of Co-Crystal and Salt

[3] Linying Li, et al. Pharmaceutics. Performance and Stability of Tenofovir Alafenamide Formulations within Subcutaneous Biodegradable Implants for HIV Pre-Exposure Prophylaxis (PrEP)

[4] Solange M Simpson, et al. Pharm Res. Design of a Drug-Eluting Subcutaneous Implant of the Antiretroviral Tenofovir Alafenamide Fumarate

[5] Hannes Lengauer, et al. Pharmaceutics. Co-crystals, Salts or Mixtures of Both? The Case of Tenofovir Alafenamide Fumarates

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Tenofovir alafenamide (TAF, GS-7340) fumarate is a prodrug of tenofovir but results in significantly higher intracellular tenofovir concentrations and lower serum levels. Tenofovir alafenamide is a novel nucleotide reverse transcriptase inhibitor for the treatment of HIV-1 infection.

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Keywords: Tenofovir alafenamide hemifumarate, TAF hemifumarate, GS-7340 hemifumarate supplier, Reverse Transcriptase, inhibitors, activators


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