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    Rilpivirine HCl (TMC278; DB08864)
    Rilpivirine HCl (TMC278; DB08864)

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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 #: V2143
    CAS #: 700361-47-3Purity ≥98%

    Description: Rilpivirine HCl (TMC-278; R-278474 HCl; DB-08864; Edurant; Rekambys; Cabenuva), the hydrochloride salt of Rilpivirine, is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that has been approved for the treatment of HIV-1 infections. Rilpivirine is usually used in combination with other anti-HIV drugs such as cabotegravir (trade name Cabenuva for the combination of cabotegravir+Rilpivirine, approved in 2021). 

    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)402.88
    FormulaC22H19ClN6
    CAS No.700361-47-3 (HCl)
    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: (E)-4-((4-((4-(2-cyanovinyl)-2,6-dimethylphenyl)amino)pyrimidin-2-yl)amino)benzonitrile hydrochloride
    InChi Key: KZVVGZKAVZUACK-BJILWQEISA-N
    InChi Code: InChI=1S/C22H18N6.ClH/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);1H/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.[H]Cl
    SynonymsTMC-278; R-278474 HCl; DB-08864; DB08864, TMC278; D08864; TMC-278; R-278474; Edurant; Rekambys; Cabenuva; R-278474, R278474, D08864, TMC 278; Rilpivirine HCl; 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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