For research use only.

Catalog No.S7303 Synonyms: R278474, TMC278

9 publications

Rilpivirine Chemical Structure

CAS No. 500287-72-9

Rilpivirine (R278474, TMC27) is a non-nucleoside reverse transcriptase inhibitor (NNRTI), and used to treat HIV-1 infection.

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Biological Activity

Description Rilpivirine (R278474, TMC27) is a non-nucleoside reverse transcriptase inhibitor (NNRTI), and used to treat HIV-1 infection.
Features Approved anti-HIV drug with longer half-life and reduced side-effect profile than older NNRTIs.
Reverse transcriptase [1]
In vitro

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. [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. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MT4 cells M4rxfWZ2dmO2aX;uJIF{e2G7 NUflTGdpSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5Qhf2muZDD0fZBmKEiLVkGgUGFKKGmwZnXjeIVlKGmwIF3UOEBk\WyuczDifUBGT0[SIHLhd4VlKHKncHzpZ4F1cW:wIHHzd4F6NCCHQ{WwQVAvODBzIN88US=> NIT5XIsyPzJ{M{KzNC=>
MT4 cells NEDyRWdEgXSxdH;4bYNqfHliYYPzZZk> NH3GWoY{KGSjeYO= M1vHU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1VPCClZXzsd{Bi\nSncjCzJIRigXNiYomgSWdHWCCkYYPl[EBz\XCuaXPheIlwdiCjc4PhfUwhS0N3ME2yJO69VQ>? M1G4bFE4OjJ|MkOw
human PBMC cells NFTJN3VHfW6ldHnvckBie3OjeR?= MoXWRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTJVu[W5iaX3teY5w\GWoaXPp[Y5kgSC4aYL1d{AyKHO3YoT5dIUhTCCrc3;sZZRmKDl{VVewNFEhcW6oZXP0[YQhcW5iaIXtZY4hWEKPQzDj[YxteyCkeTDj[YxtKGKjc3XkJIF{e2G7LDDFR|UxRTBwMECwNlYh|ryP MXGxPVk{Ozd7Nx?=
human TZM-bl cells MVzDfZRwfG:6aXPpeJkh[XO|YYm= MYm0JIRigXN? MUTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDUXm0u[mxiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JHhVXCCjc4PhfUwhS0N3ME2xPU41KM7:TR?= MnrWNlI5PTZ3NEG=
human MT4 cells M2TLUGZ2dmO2aX;uJIF{e2G7 MmLCO|IhcA>? MXvBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDOUnJVUS2{ZYPpd5RidnRiSFnWNUBp[XKkb4LpcochemW4ZYLz[UB1emGwc3PybZB1[XOnIGmxPFhNKG23dHHueEBqdm[nY4Tl[EBqdiCqdX3hckBOXDRiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXKjbDDy[ZBtcWOjdHnvckBi\nSncjC3NkBpenNiYomgTIVN[S2FREStUHRTNWKndHGt[4FtKGG|c3H5MEBGSzVyPUCuNFA{PyEQvF2= MWWyN|E{PzN2MB?=
MT2 cells NYrY[mFQS3m2b4TvfIlkcXS7IHHzd4F6 NXXJOnFMS3m2b4TvfIlkcXS7IHnuJIh2dWGwIF3UNkBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToMEBESzVyPUig{txO NHL0ZXAzOzJ7OEiwPS=>
MT2 cells MYHGeY5kfGmxbjDhd5NigQ>? NH\CTIZCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJfW2jbjDpcY12dm:mZX\pZ4lmdmO7II\pdpV{KDFiTly0MlMhemW4ZYLz[UB1emGwc3PybZB1[XOnIFuxNFNPKGGwZDDZNVgySyCmb4XicIUhdXW2YX70JIlv\mWldHXkJIlvKGi3bXHuJG1VOiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJZqemGuIHnu[oVkfGmxbjygSWM2OD1yLkCwNkDPxE1? NVSwWoxVOjJyOEG5PVM>

... Click to View More Cell Line Experimental Data

In vivo After 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. [1]


Animal Research:[1]
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  • Animal Models: Sprague−Dawley rat, beagle dog, white New Zealand rabbit, and cynomolgus monkey.
  • Dosages: 4 mg/kg ( rat); 1.25 mg/kg (other species)
  • Administration: i.v., p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 73 mg/mL (199.22 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 366.42


CAS No. 500287-72-9
Storage powder
in solvent
Synonyms R278474, TMC278
Smiles CC1=CC(=CC(=C1NC2=NC(=NC=C2)NC3=CC=C(C=C3)C#N)C)C=CC#N

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04012931 Recruiting Drug: Rilpivirine|Drug: ARV Background Regimen HIV Janssen Research & Development LLC July 18 2019 Phase 2
NCT02494986 Recruiting Drug: Rilpivirine Human Immunodeficiency Virus Type 1 Janssen Sciences Ireland UC July 6 2015 Phase 2

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Reverse Transcriptase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID