Rilpivirine

Catalog No.S7303 Synonyms: R278474, TMC278, DB08864

For research use only.

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

Rilpivirine Chemical Structure

CAS No. 500287-72-9

Selleck's Rilpivirine has been cited by 13 publications

Purity & Quality Control

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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.
Targets
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 M4eyTGZ2dmO2aX;uJIF{e2G7 NXL1TmE{SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5Qhf2muZDD0fZBmKEiLVkGgUGFKKGmwZnXjeIVlKGmwIF3UOEBk\WyuczDifUBGT0[SIHLhd4VlKHKncHzpZ4F1cW:wIHHzd4F6NCCHQ{WwQVAvODBzIN88US=> MmrQNVczOjN{M{C=
MT4 cells NXTTOHptS3m2b4TvfIlkcXS7IHHzd4F6 MXizJIRigXN? MVzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNWFQh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IFXHSnAh[mG|ZXSgdoVxdGmlYYTpc44h[XO|YYmsJGNEPTB;MjFOwG0> MkfkNVczOjN{M{C=
human PBMC cells M2[1SGZ2dmO2aX;uJIF{e2G7 NXzvSpNCSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUHWvYX6gbY1ufW6xZHXmbYNq\W6leTD2bZJ2eyBzIIP1ZpR6eGViRDDpd49t[XSnIEmyWWcxODFiaX7m[YN1\WRiaX6gbJVu[W5iUFLNR{Bk\WyuczDifUBk\WyuIHLhd4VlKGG|c3H5MEBGSzVyPUCuNFAxOjZizszN NYnve2w2OTl7M{O3PVc>
human TZM-bl cells MVrDfZRwfG:6aXPpeJkh[XO|YYm= MWK0JIRigXN? MYfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDUXm0u[mxiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JHhVXCCjc4PhfUwhS0N3ME2xPU41KM7:TR?= NFf6eGszOjh3NkW0NS=>
human MT4 cells MX3GeY5kfGmxbjDhd5NigQ>? M4LnfFczKGh? NELZO3VCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBPVlKWST3y[ZNqe3SjboSgTGlXOSCqYYLic5JqdmdicnX2[ZJ{\SC2cnHud4NzcXC2YYPlJHkyQDiOIH31eIFvfCCrbn\lZ5Rm\CCrbjDoeY1idiCPVESgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iC4aYLhcEBz\XCuaXPheIlwdiCjZoTldkA4OiCqcoOgZpkhUGWOYT3DSFQuVFSULXLleIEu\2GuIHHzd4F6NCCHQ{WwQVAvODB|NzFOwG0> M1rUflI{OTN5M{Sw
MT2 cells M4TY[WN6fG:2b4jpZ4l1gSCjc4PhfS=> MXnDfZRwfG:6aXPpeJkhcW5iaIXtZY4hVVR{IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDndo94fGhuIFPDOVA:QCEQvF2= NHPMSnIzOzJ7OEiwPS=>
MT2 cells NGPPd|NHfW6ldHnvckBie3OjeR?= MkfhRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTJVu[W5iaX3teY5w\GWoaXPp[Y5kgSC4aYL1d{AyKE6OND6zJJJmfmW{c3WgeJJidnOlcnnweIF{\SCNMUCzUkBidmRiWUG4NWMh\G:3YnzlJI12fGGwdDDpcoZm[3SnZDDpckBpfW2jbjDNWFIh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD2bZJidCCrbn\lZ5Rqd25uIFXDOVA:OC5yMEKg{txO NEHwUZAzOjB6MUm5Ny=>
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]

Protocol (from reference)

Animal Research:[1]
  • 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
Formula

C22H18N6

CAS No. 500287-72-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=CC(=C1NC2=NC(=NC=C2)NC3=CC=C(C=C3)C#N)C)C=CC#N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05112939 Recruiting Drug: RPV LA Healthy Janssen Research & Development LLC November 16 2021 Phase 1
NCT04012931 Recruiting Drug: Rilpivirine|Drug: ARV Background Regimen HIV Janssen Research & Development LLC July 18 2019 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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.

Handling Instructions

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