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      Tenofovir Alafenamide (GS-7340)
      Tenofovir Alafenamide (GS-7340)

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V1818
      CAS #: 379270-37-8Purity ≥98%

      Description: Tenofovir Alafenamide (formerly also known as TAF and GS-7340) is a novel prodrug of tenofovir, which is a potent reverse transcriptase inhibitor [nucleotide reverse transcriptase inhibitor (NRTIs)], it is used for the treatment of HIV and Hepatitis B. By blocking reverse transcriptase, Tenofovir Alafenamide prevent HIV from multiplying and can reduce the amount of HIV in the body. Tenofovir alafenamide is a prodrug that it is inactive in the parent form, and has to be converted to tenofovir diphosphate (TFV-DP) in vivo. 

      References: Nucleosides Nucleotides Nucleic Acids. 2001;20:1085-90; Antimicrob Agents Chemother. 2005;49:1898-906.

      Related CAS#: 147127-20-6 (Tenofovir); 202138-50-9 (fumarate); 206184-49-8 (hydrate); 206184-49-8 (hydrate); 1571075-19-8 (aspartate); 201341-05-1 Tenofovir dsoproxil); 1236287-04-9 (Tenofovir maleate); 1392275-56-7 (Tenofovir alafenamide hemifumarate); 379270-38-9 (Tenofovir alafenamide fumarate); 1464851-21-5 [(Z)-9-Propenyladenine; (Z)-Mutagenic Impurity of Tenofovir Disoproxil]; 1446486-33-4 [9-Propenyladenine; Mutagenic Impurity of Tenofovir Disoproxil; Tenofovir Impurity 2]

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      Molecular Weight (MW)476.47
      FormulaC21H29N6O5P
      CAS No.379270-37-8
      Storage-20℃ for 3 years in powder form
      -80℃ for 2 years in solvent
      Solubility (In vitro)DMSO: 95 mg/mL (199.4 mM)
      Water:<1 mg/mL
      Ethanol: 95 mg/mL (199.4 mM)
      Other infoChemical Name: (S)-isopropyl 2-(((S)-((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate
      InChi Key: LDEKQSIMHVQZJK-AZFZMOAFSA-N
      InChi Code: InChI=1S/C21H29N6O5P/c1-14(2)31-21(28)16(4)26-33(29,32-17-8-6-5-7-9-17)13-30-15(3)10-27-12-25-18-19(22)23-11-24-20(18)27/h5-9,11-12,14-16H,10,13H2,1-4H3,(H,26,29)(H2,22,23,24)/t15-,16+,33?/m1/s1
      SMILES Code: C[[email protected]](N[[email protected]@](OC1=CC=CC=C1)(CO[[email protected]](C)CN2C=NC3=C(N)N=CN=C23)=O)C(OC(C)C)=O
      SynonymsGS7340; GS-7340; GS 7340; Genvoya


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      In Vitro

      In vitro activity: GS-7340 has a potent anti-HIV activity with IC50 of 0.005 μM. GS 7340 has a half-life of 90 min in human plasma and a half-life of 28.3 min in an MT-2 cell extract at 37°C. the hepatic uptake of GS-7340 isfacilitated by OATP1B1 and OATP1B3, respectively. GS-7340 inhibits HBV reverse transcriptase after being converted to the pharmacologically active form, TFV-DP. 

      Cell Assay: Tenofovir alafenamide antiviral activities are similar across all cell types, ranging from 5 to 7 nM, while the CC50 varies from 4.7 to 42 μM for MT-4 and MT-2 cells, respectively. The antiviral activity of TAF is evaluated against a panel of HIV-1 and HIV-2 isolates, including HIV-1 group M subtypes A to G, as well as group N and O isolates. Overall, for the 29 primary HIV-1 isolates tested in PBMCs, TAF EC50s range from 0.1 to 12 nM, with a mean EC50 of 3.5 nM compared to a mean EC50 of 11.8 nM for AZT, which is used as an internal control. For the HIV-2 isolates, the mean EC50s are 1.8 nM for TAF and 6.4 nM for AZT.

      In VivoIn male beagle dogs, GS 7340 (10 mg/kg, p.o.) results in an enhanced distribution to lymphatic tissue. 
      Animal modelBeagle dogs
      Formulation & Dosage10 mg/kg, p.o.
      ReferencesNucleosides Nucleotides Nucleic Acids. 2001 Apr-Jul;20(4-7):1085-90; Antimicrob Agents Chemother. 2005 May;49(5):1898-906.

      These protocols are for reference only. InvivoChem does not independently validate these methods.

      Tenofovir Alafenamide (GS-7340)

      Effects of tenofovir and other NRTIs on mtDNA content in skeletal muscle cells. Antimicrob Agents Chemother. 2002 Mar;46(3):716-23.

      Tenofovir Alafenamide (GS-7340)

      Effects of ddC, ddI, and tenofovir on the expression of COX II and COX IV in HepG2 cells. Antimicrob Agents Chemother. 2002 Mar;46(3):716-23.

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