Tenofovir alafenamide fumarate

SKU: orb1905871

Description

Tenofovir alafenamide fumarate (GS-7340 fumarate) is an orally bioavailable prodrug of tenofovir with potent anti-HIV activity, applicable for both treatment and pre-exposure prophylaxis (PrEP) research. It is widely used in virology and pharmacology studies, demonstrating efficacy in both cellular assays and animal models of HIV infection.

Research Area

Infectious Disease & Virology, Pharmacology & Drug Discovery, Protein Biochemistry

Key Properties

• CAS Number: 379270-38-9
• MW: 592.54
• Purity: 99.99% (May vary between batches)
• Formula: C₂₅H₃₃N₆O₉P
• SMILES: OC(=O)\C=C\C(O)=O.CC(C)OC(=O)[C@H](C)N[P@](=O)(CO[C@H](C)Cn1cnc2c(N)ncnc12)Oc1ccccc1
• Target: Reverse Transcriptase,HIV Protease
• Solubility: H2O:25 mg/mL (42.19 mM);DMSO:200 mg/mL (337.53 mM)

Bioactivity

• In Vivo:
  Tenofovir alafenamide fumarate (GS-7340 fumarate), an amidate prodrug of Tenofovir, exhibits enhanced oral bioavailability and plasma stability compared to Tenofovir disoproxil fumarate (TDF) .
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• In Vitro:
  Tenofovir alafenamide fumarate antiviral activity was similar in all cell types, ranging from 5 to 7 nM, whereas CC50 varied from 4.7 to 42 μM for MT-4 and MT-2 cells. The antiviral activity of TAF was evaluated against a panel of HIV-1 and HIV-2 isolates, including HIV-1 M group subtypes A to G, as well as group N and O isolates. Overall, TAF EC50 ranged from 0.1 to 12 nM, with an average EC50 of 3.5 nM, compared to an average EC50 of 11.8 nM for AZT, used as an internal control, for 29 major HIV-1 isolates tested in PBMC. For HIV-2 isolates, the average EC50 is 1.8 nM for TAF and 6.4 nM for AZT.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HIVProtease, HIV Protease, HIV, GS 7340 Fumarate, GS7340 Fumarate, GS-7340 Fumarate, GS-7340 fumarate, Tenofovir alafenamide Fumarate

Compound Identifiers

PubChem CID

68516365