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    Tenofovir (GS 1278)
    Tenofovir (GS 1278)

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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 #: V1811
    CAS #: 147127-20-6Purity ≥98%

    Description: Tenofovir (formerly also known as GS-1278; PMPA; TDF) is an approved anti-HIV drug that blocks reverse transcriptase and hepatitis B virus infections. Tenofovir is an antiretroviral medication used to prevent and treat HIV/AIDS and to treat chronic hepatitis B. Tenofovir reduces the viral cytopathic effect of HIV-1(IIIB), HIV-2(ROD) and HIV(EHO) with EC50 of 1.15 μg/mL, 1.12 μg/mL and 1.05 μg/mL in MT-4 cells. Tenofovir also reduces the viral cytopathic effect of SIV(mac251) , SIV(B670) ,SHIV(89.6) and SHIV(RTSHIV). Tenofovir is the active substance of tenofovir disoproxil which is a prodrug that is used because of its better absorption in the gut.

    References: Antivir Ther. 2004 Feb;9(1):57-65; Clin Microbiol Rev. 2003 Oct;16(4):569-96.

    Related CAS202138-50-9 (fumarate); 206184-49-8 (hydrate); 379270-37-8 (alafenamide); 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]; 1276030-80-8 (Tenofovir disoproxil maleate) 1453166-76-1 (Tenofovir disoproxil phosphate) 1637632-97-3 (Tenofovir disoproxil succinate); 147127-19-3 [(S)-Tenofovir]

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    Molecula Formula: C9H14N5O4P
    Exact Mass: 287.0783
    Molecular Weight: 287.2158
    Elemental Analysis: C, 37.64; H, 4.91; N, 24.38; O, 22.28; P, 10.78 

    Related CAS #: 202138-50-9 (fumarate); 206184-49-8 (hydrate); 379270-37-8 (alafenamide); 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];   

    Synonym: GS 1278; GS1278; GS-1278; PMPA; TDF;  GS1275; GS-1275; GS 1275; Tenofovir; TFV gel; PMPA

    Chemical Name: (R)-(((1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonic acid

    InChi Key: SGOIRFVFHAKUTI-ZCFIWIBFSA-N

    InChi Code: InChI=1S/C9H14N5O4P/c1-6(18-5-19(15,16)17)2-14-4-13-7-8(10)11-3-12-9(7)14/h3-4,6H,2,5H2,1H3,(H2,10,11,12)(H2,15,16,17)/t6-/m1/s1

    SMILES Code: C[[email protected]@H](OCP(O)(O)=O)CN1C=NC2=C(N)N=CN=C12           


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    In Vitro

    In vitro activity: Tenofovir reduces the viral cytopathic effect of HIV-1(IIIB), HIV-2(ROD) and HIV(EHO) with EC50 of 1.15 μg/mL, 1.12 μg/mL and 1.05 μg/mL in MT-4 cells. Tenofovir also reduces the viral cytopathic effect of SIV(mac251) , SIV(B670) ,SHIV(89.6) and SHIV(RTSHIV). Tenofovir is uniquely active against multinucleoside-resistant HIV expressing the Q151M mutation, but shows reduced susceptibility to the T69S insertion mutations. Tenofovir inhibits hepatitis B virus (HBV) activity in HepG2 2.2.15, HepAD38 and HepAD79 cells. Tenofovir (4 μM) completely inhibits the growth of HIVIIIB in MT-2 cells. Tenofovir inhibits synthesis of negative strand strong-stop DNA with IC50 of 9 µM for wild-type RT, 6 µM for M184V RT and 50 µM for K65R RT.


    Cell Assay: Cells are plated into 48-well tissue culture plates (39,000 cells/mL) and allowed to grow for 48 h followed by treatment with vehicle or Tenofovir. Following the treatment period, cell viability is assessed using the MTT assay. The MTT assay relies on the conversion of tetrazolium dye 3-(4,5-dimethlthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) to formazan by NAD(P)H-dependent oxidoreductases.

    In VivoTenofovir (30 mg/kg) completely prevents SIV infection in all macaques without toxicity. Tenofovir treatment reduces plasma viral RNA levels to undetectable, with parallel decreases in the infectivity of plasma and infectious cells in peripheral blood mononuclear cells and cerebrospinal fluid (CSF) and stabilization of CD4+ T-cell numbers. Tenofovir (30 mg/kg, s.c.) completely abrogates HIV infection via intravaginal exposure in pig-tailed macaques.
    Animal modelMacaques 
    Formulation & DosageDissolved in saline; 30 mg/kg; s.c. injection
    ReferencesAntivir Ther. 2004 Feb;9(1):57-65; Clin Microbiol Rev. 2003 Oct;16(4):569-96. 


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

    Tenofovir

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

    Tenofovir

    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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