For research use only.

Catalog No.S7303 Synonyms: R278474, TMC278, DB08864

12 publications

Rilpivirine Chemical Structure

CAS No. 500287-72-9

Rilpivirine (R278474, TMC27, DB08864) is a non-nucleoside reverse transcriptase inhibitor (NNRTI), and used to treat HIV-1 infection.

Selleck's Rilpivirine has been cited by 12 publications

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Biological Activity

Description Rilpivirine (R278474, TMC27, DB08864) 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 MkW4SpVv[3Srb36gZZN{[Xl? NILYZ2xCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEB4cWymIIT5dIUhUEmYMTDMRWkhcW6oZXP0[YQhcW5iTWS0JINmdGy|IHL5JGVITlBiYnHz[YQhemWybHnjZZRqd25iYYPzZZktKEWFNUC9NE4xODFizszN NWGyd21YOTd{MkOyN|A>
MT4 cells NVjVcI8yS3m2b4TvfIlkcXS7IHHzd4F6 NXXLcnZxOyCmYYnz M4[0UWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1VPCClZXzsd{Bi\nSncjCzJIRigXNiYomgSWdHWCCkYYPl[EBz\XCuaXPheIlwdiCjc4PhfUwhS0N3ME2yJO69VQ>? M2PqXFE4OjJ|MkOw
human PBMC cells NFO0[WNHfW6ldHnvckBie3OjeR?= NUD3N|NHSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUHWvYX6gbY1ufW6xZHXmbYNq\W6leTD2bZJ2eyBzIIP1ZpR6eGViRDDpd49t[XSnIEmyWWcxODFiaX7m[YN1\WRiaX6gbJVu[W5iUFLNR{Bk\WyuczDifUBk\WyuIHLhd4VlKGG|c3H5MEBGSzVyPUCuNFAxOjZizszN MW[xPVk{Ozd7Nx?=
human MT4 cells NITxOmtHfW6ldHnvckBie3OjeR?= NIfEd284OiCq NULOemxRSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhVk6UVFmtdoV{cXO2YX70JGhKXjFiaHHyZo9zcW6pIILleoVze2VidILhcpNkemmydHHz[UB[OTh6TDDteZRidnRiaX7m[YN1\WRiaX6gbJVu[W5iTWS0JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZidnnyZYwhemWybHnjZZRqd25iYX\0[ZIhPzJiaILzJIJ6KEinTHGtR2Q1NUyWUj3i[ZRiNWejbDDhd5NigSxiRVO1NF0xNjByM{eg{txO MmDZNlMyOzd|NEC=
MT2 cells MYLDfZRwfG:6aXPpeJkh[XO|YYm= M2jlWWN6fG:2b4jpZ4l1gSCrbjDoeY1idiCPVEKgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDygR2M2OD16IN88US=> MY[yN|I6QDhyOR?=
MT2 cells M1TQO2Z2dmO2aX;uJIF{e2G7 M3HESmFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGh2dWGwIHntcZVvd2SnZnnjbYVv[3lidnnyeZMhOSCQTESuN{Bz\X[ncoPlJJRz[W6|Y4LpdJRie2ViS{GwN24h[W6mIGmxPFFEKGSxdXLs[UBufXSjboSgbY5n\WO2ZXSgbY4hcHWvYX6gUXQzKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[geolz[WxiaX7m[YN1cW:wLDDFR|UxRTBwMECyJO69VQ>? MYSyNlA5OTl7Mx?=

... 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, DB08864
Smiles CC1=CC(=CC(=C1NC2=NC(=NC=C2)NC3=CC=C(C=C3)C#N)C)C=CC#N

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Mass Concentration Volume Molecular Weight

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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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Reverse Transcriptase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID