Name: Etravirine
Brand: Selleck Chemicals
SKU: S3080
Rating: 5 (7 reviews)

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

Etravirine Chemical Structure

CAS: 269055-15-4

Selleck's Etravirine has been cited by 7 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 99.97%

99.97

Etravirine Related Products

Related Targets	HBV RT HIV RT RT	Click to Expand
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Related Compound Libraries	Anti-infection Compound Library Antibiotics compound Library Antiviral Compound Library Anti-parasitic Compound Library Gut Microbial Metabolite Library	Click to Expand

Signaling Pathway

Reverse Transcriptase Signaling Pathway

Choose Selective Reverse Transcriptase Inhibitors

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

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

Tel: +1-832-582-8158 Ext:3
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