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Tenofovir alafenamide fumarate

Cat. No. M20784
Tenofovir alafenamide fumarate Structure
Synonym:

TAF fumarate, GS-7340 fumarate

Size Price Availability Quantity
5mg USD 55  USD55 In stock
10mg USD 75  USD75 In stock
25mg USD 130  USD130 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 592.54
Formula C25H33N6O9P
CAS Number 379270-38-9
Solubility (25°C) DMSO 100 mg/mL
Water 10 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] William A Lee, et al. Antivir Ther. Tenofovir alafenamide fumarate

[2] Shahin Lockman, et al. Lancet. Efficacy and safety of dolutegravir with emtricitabine and tenofovir alafenamide fumarate or tenofovir disoproxil fumarate, and efavirenz, emtricitabine, and tenofovir disoproxil fumarate HIV antiretroviral therapy regimens started in pregnancy (IMPAACT 2䲧皬Ỵ皭㧀皫羹癆甿ᅸڳƌڳĀ�癈嶁癄Ѐ瑖噔

[3] Kenneth H Mayer, et al. Lancet. Emtricitabine and tenofovir alafenamide vs emtricitabine and tenofovir disoproxil fumarate for HIV pre-exposure prophylaxis (DISCOVER): primary results from a randomised, double-blind, multicentre, active-controlled, phase 3, non-inferiority trial

[4] Kosh Agarwal, et al. J Hepatol. 96 weeks treatment of tenofovir alafenamide vs. tenofovir disoproxil fumarate for hepatitis B virus infection

[5] Blandine Aloy, et al. AIDS Rev. Is Tenofovir Alafenamide Safer than Tenofovir Disoproxil Fumarate for the Kidneys?

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Tenofovir alafenamide hemifumarate

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.

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


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