Etravirine (TMC125)

For research use only.

Catalog No.S3080 Synonyms: R-165335

6 publications

Etravirine (TMC125) Chemical Structure

CAS No. 269055-15-4

Etravirine (TMC125, R-165335) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.

Size Price Stock Quantity  
10mM (1mL in DMSO) EUR 117 In stock
EUR 68 In stock
EUR 265 In stock
EUR 363 In stock
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Selleck's Etravirine (TMC125) has been cited by 6 publications

1 Customer Review

  • 1D 19F NMR spectra of RT181tfmF and several RT181tfmF mutants in the absence (black) and presence of NVP (pink), EFV (green), ETR (blue) and RPV (orange). (A) Superposition of the 19F spectra of apo-RT181tfmF and the 19F spectra of RT181tfmF in the presence of each NNRTI, (B) Superposition of the 19F spectra of apo-RT181tfmF-V108I and the 19F spectra of RT181tfmF in the presence of each NNRTI, (C) Superposition of the 19F spectra of apo-RT181tfmF-K103N and the 19F spectra of RT181tfmF-K103N in the presence of each NNRTI, (D) Superposition of the 19F spectra of apo-RT181tfmF-E138K(p51) and the 19F spectra of RT181tfmF-E138K(p51) in the presence of each NNRTI. The 19F spectra in the presence of each NNRTI at 1:1 and 1:5 molar ratios are shown in light and dark colors, respectively. Chemical formulae for each inhibitor are depicted in the individual panels.

    Biochemistry, 2016, 55(28):3864-73. Etravirine (TMC125) purchased from Selleck.

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Biological Activity

Description Etravirine (TMC125, R-165335) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
Targets
Reverse transcriptase [1]
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 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]

Protocol

Solubility (25°C)

In vitro DMSO 42 mg/mL (96.48 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 435.28
Formula

C20H15BrN6O

CAS No. 269055-15-4
Storage powder
in solvent
Synonyms R-165335
Smiles CC1=CC(=CC(=C1OC2=NC(=NC(=C2Br)N)NC3=CC=C(C=C3)C#N)C)C#N

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04194021 Recruiting -- HIV/AIDS Elizabeth Glaser Pediatric AIDS Foundation|Janssen LP January 1 2019 --
NCT02818348 Completed Drug: darunavir/cobicistat|Drug: etravirine HIV-1 Infection Fundacio Lluita Contra la SIDA June 2016 Phase 1
NCT01427504 Completed Drug: boceprevir; etravirine Hepatitis C|HIV University of Colorado Denver August 2011 Not Applicable
NCT01347658 Completed Dietary Supplement: Echinacea purpurea HIV Fundacio Lluita Contra la SIDA April 2011 Not Applicable
NCT01625169 Completed Drug: Etravirine pharmacokinetics in breast milk and plasma HIV University of Southern California|Tibotec Therapeutics a Division of Ortho Biotech Products L.P. USA April 2010 Not Applicable
NCT01090648 Completed Drug: etravirine HIV-Infections Tibotec Pharmaceuticals Ireland March 2010 Phase 1

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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Reverse Transcriptase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID