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Tenofovir hydrate

Cat. No. M10364
Tenofovir hydrate Structure
Synonym:

GS 1278 hydrate; PMPA hydrate

Size Price Availability Quantity
10mM*1mL in DMSO USD 50  USD50 In stock
5mg USD 45  USD45 In stock
10mg USD 70  USD70 In stock
50mg USD 120  USD120 In stock
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Quality Control & Documentation
Biological Activity

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

Chemical Information
Molecular Weight 305.23
Formula C9H16N5O5P
CAS Number 206184-49-8
Solubility (25°C) DMSO 5 mg/mL
Storage 2-8°C, sealed
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] Victoria Pilkington, et al. AIDS. Tenofovir alafenamide vs. tenofovir disoproxil fumarate: an updated meta-analysis of 14 894 patients across 14 trials

[2] Cheng-Hao Tseng, et al. Lancet Gastroenterol Hepatol. Hepatocellular carcinoma incidence with tenofovir versus entecavir in chronic hepatitis B: a systematic review and meta-analysis

[3] James Riddell 4th, et al. JAMA. HIV Preexposure Prophylaxis: A Review

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

[5] Erik De Clercq. Biochem Pharmacol. Tenofovir alafenamide (TAF) as the successor of tenofovir disoproxil fumarate (TDF)

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Keywords: Tenofovir hydrate, GS 1278 hydrate; PMPA hydrate supplier, HIV Protease, inhibitors, activators

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