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Tenofovir Disoproxil Fumarate

Cat. No. M5052
Tenofovir Disoproxil Fumarate Structure
Synonym:

Tenofovir DF

Size Price Availability Quantity
10mM*1mL in DMSO USD 50  USD50 In stock
10mg USD 45  USD45 In stock
50mg USD 100  USD100 In stock
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Quality Control & Documentation
Biological Activity

Tenofovir is eliminated from systemic circulation renally through a combination of glomerular filtration and active tubular secretion. Tenofovir is not a substrate for human organic cation transporter type 1 (hOCT1) or hOCT2. Tenofovir accumulates to fivefold lower levels in MRP4-overexpressing cells, and its accumulation could be increased by an MRP inhibitor.Tenofovir inhibits the proliferation of liver-derived HepG2 cells and normal skeletal muscle cells with CC(50) values of 398 mM and 870 mM, respectively. Tenofovir shows substantially weaker effects on proliferation and viability of renal proximal tubule epithelial cells than cidofovir, a related nucleotide analog with the potential to induce renal tubular dysfunction.

Chemical Information
Molecular Weight 635.51
Formula C19H30N5O10P.C4H4O4
CAS Number 202138-50-9
Solubility (25°C) DMSO 128 mg/mL
Water <1 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] Ray AS,et.al. Antimicrob Agents Chemother. Mechanism of active renal tubular efflux of tenofovir.

[2] Cihlar T,et.al. Antiviral Res. Tenofovir exhibits low cytotoxicity in various human cell types: comparison with other nucleoside reverse transcriptase inhibitors.

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Keywords: Tenofovir Disoproxil Fumarate, Tenofovir DF supplier, HIV Protease, inhibitors, activators


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