Tenofovir alafenamide hemifumarate

SKU: orb1299952

Description

Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is a phosphonoamidate prodrug of tenofovir, designed for enhanced oral delivery and intracellular conversion to the active nucleotide analog against HIV reverse transcriptase. It is widely used in antiviral research for in vitro and in vivo studies of HIV-1 infection and treatment strategies.

Research Area

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

Key Properties

• CAS Number: 1392275-56-7
• MW: 534.51
• Purity: 99.96% (May vary between batches)
• Formula: C₂₁H₂₉N₆O₅P·1/2C₄H₄O₄
• SMILES: OC(/C=C/C(O)=O)=O.CC(C)OC([C@H](C)NP(CO[C@H](C)CN1C2=NC=NC(N)=C2N=C1)(OC3=CC=CC=C3)=O)=O.CC(C)OC([C@H](C)NP(CO[C@H](C)CN4C5=NC=NC(N)=C5N=C4)(OC6=CC=CC=C6)=O)=O
• Target: Reverse Transcriptase,HIV Protease
• Solubility: DMSO:50 mg/mL (93.54 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.74 mM)

Bioactivity

• In Vitro:
  Tenofovir alafenamide fumarate (TAF) is an oral phosphonoamidate prodrug of the HIV reverse transcriptase nucleotide inhibitor tenofovir (TFV). Overexpression of CatA or liver carboxylesterase 1 (Ces1) in HEK293T cells increased intracellular TAF hydrolysis 2- and 5-fold, respectively. Knockdown of CatA expression with RNA interference (RNAi) in HeLa cells reduced intracellular TAF metabolism 5-fold. Additionally, the anti-HIV activity and the rate of CatA hydrolysis showed good correlation within a large set of TFV phosphonoamidate prodrugs.
  Read more...

Storage & Handling

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

Alternative Names

inhibit, Inhibitor, HIV, HIV-1, HIV Protease, HIVProtease, Human immunodeficiency virus, GS7340, GS-7340 hemifumarate, GS-7340, GS-7340 (hemifumarate), GS 7340, Tenofovir alafenamide, Tenofovir alafenamide Fumarate, Tenofovir alafenamide fumarate, Tenofovir alafenamide hemifumarate, Tenofovir alafenamide Hemifumarate, Reverse Transcriptase, ReverseTranscriptase

Compound Identifiers

PubChem CID

134159228