Home Microbiology Reverse Transcriptase inhibitor Etravirine For research use only.

Etravirine

Synonyms: TMC125, R-165335

Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.

Etravirine Chemical Structure

Etravirine Chemical Structure

CAS No. 269055-15-4

Purity & Quality Control

Etravirine Related Products

Signaling Pathway

Reverse Transcriptase Signaling Pathways

Reverse Transcriptase Signaling Pathway

Biological Activity

Description Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
Targets
Reverse transcriptase [1]
In vitro
In vitro Etravirine (TMC125), is highly active against wild-type HIV-1 with EC50 of 1.4 nM to 4.8 nM and shows some activity against HIV-2 with EC50 of 3.5 μM. TMC125 also inhibits a series of HIV-1 group M subtypes and circulating recombinant forms and a group O virus. [1] [2]
In Vivo
In vivo Etravirine has a high genetic barrier to the development of resistance. In phase IIb trials in treatment-experienced patients, including those infected with virus resistant to NNRTIs and protease inhibitors (PIs), TMC125 is active against HIV resistant to currently available NNRTIs, with a similar tolerability profile to that of the control group. [3]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04194021 Active not recruiting
HIV/AIDS
Elizabeth Glaser Pediatric AIDS Foundation|Janssen LP
 January 1 2019 --
NCT02818348 Completed
HIV-1 Infection
Fundación FLS de Lucha Contra el Sida las Enfermedades Infecciosas y la Promoción de la Salud y la Ciencia
 June 2016 Phase 1
NCT01427504 Completed
Hepatitis C|HIV
University of Colorado Denver
 August 2011 Not Applicable
NCT01347658 Completed
HIV
Fundación FLS de Lucha Contra el Sida las Enfermedades Infecciosas y la Promoción de la Salud y la Ciencia
 April 2011 Not Applicable
NCT01625169 Completed
HIV
University of Southern California|Tibotec Therapeutics a Division of Ortho Biotech Products L.P. USA
 April 2010 Not Applicable
NCT01090648 Completed
HIV-Infections
Tibotec Pharmaceuticals Ireland
 March 2010 Phase 1

Chemical Information & Solubility

Molecular Weight 435.28 Formula

C20H15BrN6O
CAS No. 269055-15-4 SDF Download Etravirine SDF
Smiles CC1=CC(=CC(=C1OC2=NC(=NC(=C2Br)N)NC3=CC=C(C=C3)C#N)C)C#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 87 mg/mL ( (199.87 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

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

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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.

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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