Rilpivirine

Catalog No.S7303 Synonyms: R278474, TMC278

Rilpivirine Chemical Structure

Molecular Weight(MW): 366.42

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

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Biological Activity

Description Rilpivirine 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 Mnu0SpVv[3Srb36gZZN{[Xl? MYfBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDD3bYxlKHS7cHWgTGlXOSCOQVmgbY5n\WO2ZXSgbY4hVVR2IHPlcIx{KGK7IFXHSnAh[mG|ZXSgdoVxdGmlYYTpc44h[XO|YYmsJGVEPTB;MD6wNFEh|ryP NFPMPIwyPzJ{M{KzNC=>
MT4 cells NFjpOphEgXSxdH;4bYNqfHliYYPzZZk> NW[xcFNyOyCmYYnz MUjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNWFQh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IFXHSnAh[mG|ZXSgdoVxdGmlYYTpc44h[XO|YYmsJGNEPTB;MjFOwG0> NUjhdGJTOTd{MkOyN|A>
human PBMC cells MlPLSpVv[3Srb36gZZN{[Xl? M4Kwc2FvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGh2dWGwIHntcZVvd2SnZnnjbYVv[3lidnnyeZMhOSC|dXL0fZBmKERiaYPvcIF1\SB7MmXHNFAyKGmwZnXjeIVlKGmwIHj1cYFvKFCETVOgZ4VtdHNiYomgZ4VtdCCkYYPl[EBie3OjeTygSWM2OD1yLkCwNFI3KM7:TR?= MYGxPVk{Ozd7Nx?=
human TZM-bl cells MWjDfZRwfG:6aXPpeJkh[XO|YYm= M1[yfVQh\GG7cx?= M2Hvd2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHRbVS2kbDDj[YxteyCjZoTldkA1KGSjeYOgZpkhYFSWIHHzd4F6NCCFQ{WwQVE6NjRizszN NIn1WI0zOjh3NkW0NS=>
human MT4 cells MYLGeY5kfGmxbjDhd5NigQ>? M4OwdFczKGh? MVrBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDOUnJVUS2{ZYPpd5RidnRiSFnWNUBp[XKkb4LpcochemW4ZYLz[UB1emGwc3PybZB1[XOnIGmxPFhNKG23dHHueEBqdm[nY4Tl[EBqdiCqdX3hckBOXDRiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXKjbDDy[ZBtcWOjdHnvckBi\nSncjC3NkBpenNiYomgTIVN[S2FREStUHRTNWKndHGt[4FtKGG|c3H5MEBGSzVyPUCuNFA{PyEQvF2= NV\RV2ZROjNzM{ezOFA>
MT2 cells MYnDfZRwfG:6aXPpeJkh[XO|YYm= M37GRWN6fG:2b4jpZ4l1gSCrbjDoeY1idiCPVEKgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDygR2M2OD16IN88US=> MlTmNlMzQTh6MEm=
MT2 cells MWTGeY5kfGmxbjDhd5NigQ>? NWfFXJluSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUHWvYX6gbY1ufW6xZHXmbYNq\W6leTD2bZJ2eyBzIF7MOE4{KHKndnXyd4UhfHKjboPjdolxfGG|ZTDLNVA{ViCjbnSgXVE5OUNiZH;1ZoxmKG23dHHueEBqdm[nY4Tl[EBqdiCqdX3hckBOXDJiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXKjbDDpcoZm[3Srb36sJGVEPTB;MD6wNFIh|ryP MXyyNlA5OTl7Mx?=

... 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]

Protocol

Animal Research:[1]
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  • Animal Models: Sprague−Dawley rat, beagle dog, white New Zealand rabbit, and cynomolgus monkey.
  • Formulation: PEG 400
  • 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 powder
in solvent
Synonyms R278474, TMC278

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03497676 Recruiting HIV Infections National Institute of Allergy and Infectious Diseases (NIAID) March 19 2019 Phase 1|Phase 2
NCT03497676 Recruiting HIV Infections National Institute of Allergy and Infectious Diseases (NIAID) March 19 2019 Phase 1|Phase 2
NCT02882230 Suspended HIV Fondation Ophtalmologique Adolphe de Rothschild November 19 2018 --
NCT03782142 Recruiting AIDS Sabyasachi Sen|George Washington University November 1 2018 --
NCT02882230 Suspended HIV Fondation Ophtalmologique Adolphe de Rothschild November 19 2018 --
NCT03782142 Recruiting AIDS Sabyasachi Sen|George Washington University November 1 2018 --

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.

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Reverse Transcriptase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID