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    Etravirine (R165335; TMC125)
    Etravirine (R165335; TMC125)

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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 #: V1828
    CAS #: 269055-15-4 Purity ≥98%

    Description: Etravirine (also known as TMC125 and R 165335, ) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV. It was also approved in 2008. Etravirine, in combination with other anti-retrovirals, is indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in antiretroviral treatment-experienced adult patients, who have evidence of viral replication and HIV-1 strains resistant to a NNRTI and other antiretroviral agents. 

    References: J Med Chem. 2004 May 6;47(10):2550-60; Antimicrob Agents Chemother. 2004 Dec;48(12):4680-6.

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    Molecular Weight (MW)435.28 
    FormulaC20H15BrN6O 
    CAS No.269055-15-4 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 42 mg/mL (96.5 mM) 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: 4-(6-Amino-5-bromo-2-(4-cyanoanilino)pyrimidin-4-yloxy)-3,5-dimethylbenzonitrile

    InChi Key: PYGWGZALEOIKDF-UHFFFAOYSA-N

    InChi Code: InChI=1S/C20H15BrN6O/c1-11-7-14(10-23)8-12(2)17(11)28-19-16(21)18(24)26-20(27-19)25-15-5-3-13(9-22)4-6-15/h3-8H,1-2H3,(H3,24,25,26,27)

    SMILES Code: N#CC1=CC(C)=C(OC2=NC(NC3=CC=C(C#N)C=C3)=NC(N)=C2Br)C(C)=C1

    SynonymsR-165335; R165335; R 165335; TMC 125; TMC-125; TMC125; Etravirine. Intelence.


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    In Vitro

    In vitro activity: Etravirine (TMC125), is highly active against wild-type HIV-1 with EC50 of 1.4 nM to 4.8 nM and shows some activity against HIV-2 with EC50 of 3.5 μM. TMC125 also inhibits a series of HIV-1 group M subtypes and circulating recombinant forms and a group O virus.

    In VivoEtravirine has a high genetic barrier to the development of resistance. In phase IIb trials in treatment-experienced patients, including those infected with virus resistant to NNRTIs and protease inhibitors (PIs), TMC125 is active against HIV resistant to currently available NNRTIs, with a similar tolerability profile to that of the control group. 
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    References

     J Med Chem. 2004 May 6;47(10):2550-60; Antimicrob Agents Chemother. 2004 Dec;48(12):4680-6; Lancet. 2007 Jul 7;370(9581):39-48. 


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

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