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    Rilpivirine (R278474; TMC278)
    Rilpivirine (R278474; TMC278)

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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 #: V1819
    CAS #: 500287-72-9 Purity ≥98%

    Description: Rilpivirine (formerly known as R278474; TMC278; DB08864), an approved HIV drug, is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that has been widely used for the treatment of HIV-1 infection. Rilpivirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with higher potency, longer half-life and reduced side-effect profile compared with older NNRTIs, such as efavirenz. Rilpivirine showed inhibitory activities to both wild-type HIV (with EC50 value of 0.51 nM) and NNRTI-resistant strains. The conformational flexibility of rilpivirine allowed it to adjust different mutations of the reverse transcriptase. For the singly mutant HIV strains such as L100I, G190S, G190A and V106A, rilpivirine showed higher retained potency than efavirenz and low EC50 values blow 1 nM.

    References: J Med Chem. 2005 Mar 24;48(6):1901-9; Antimicrob Agents Chemother. 2010 Feb;54(2):718-27. 

    Related CAS#: 700361-47-3 (HCl); 500287-72-9 (free base)

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    Molecular Weight (MW)366.42
    FormulaC22H18N6
    CAS No.500287-72-9 (free base); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 73 mg/mL (199.2 mM)
    Water:<1 mg/mL
    Ethanol: <1 mg/mL
    Other infoChemical Name: 4-{[4-({4-[(E)-2-cyanovinyl]-2,6-dimethylphenyl}amino)pyrimidin-2-yl]amino}benzonitrile
    InChi Key: YIBOMRUWOWDFLG-ONEGZZNKSA-N
    InChi Code: InChI=1S/C22H18N6/c1-15-12-18(4-3-10-23)13-16(2)21(15)27-20-9-11-25-22(28-20)26-19-7-5-17(14-24)6-8-19/h3-9,11-13H,1-2H3,(H2,25,26,27,28)/b4-3+
    SMILES Code: N#CC1=CC=C(NC2=NC=CC(NC3=C(C)C=C(/C=C/C#N)C=C3C)=N2)C=C1 
    SynonymsR-278474, R 278474, R278474, D08864, D08864, DB08864, TMC278; TMC-278; TMC 278; Rilpivirine; Edurant.


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    In Vitro

    In vitro activity: Rilpivirine shows antiviral activity with EC50 ranging from 0.1 nM to 2 nM against wild-type and selected site-directed single and double mutants of HIV-1. Rilpivirine inhibits viral replication at concentrations at which first-generation NNRTIs could not suppress replication, and produces a high genetic barrier to resistance development.

    In VivoAfter iv administration of Rilpivirine, Elimination half-life ranges from 4.4 h in rat to 31 h in dog. After oral administration of Rilpivirine in PEG 400, half-life ranges between 2.8 h in rat and 39 h in dog. 
    Animal modelSprague−Dawley rat, beagle dog, white New Zealand rabbit, and cynomolgus monkey. 
    Formulation & DosageDissolved in PEG 400; 4 mg/kg ( rat); 1.25 mg/kg (other species); i.v. or p.o.
    ReferencesJ Med Chem. 2005 Mar 24;48(6):1901-9; Antimicrob Agents Chemother. 2010 Feb;54(2):718-27. 


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

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