Etravirine (TMC125)

Catalog No.S3080 Synonyms: R-165335

Etravirine (TMC125) Chemical Structure

Molecular Weight(MW): 435.28

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

Size Price Stock Quantity  
In DMSO USD 120 In stock
USD 70 In stock
USD 270 In stock
USD 370 In stock
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Cited by 2 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) 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

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 Conditions Sponsor/Collaborators Start Date Phases
NCT02818348 Completed HIV-1 Infection Fundacio Lluita Contra la SIDA June 2016 Phase 1
NCT02818348 Completed HIV-1 Infection Fundacio Lluita Contra la SIDA June 2016 Phase 1
NCT02212379 Completed HIV-1 Infection French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Merck Sharp & Dohme Corp.|Janssen-Cilag Ltd. January 2015 Phase 2
NCT02212379 Completed HIV-1 Infection French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Merck Sharp & Dohme Corp.|Janssen-Cilag Ltd. January 2015 Phase 2
NCT02063360 Completed Infection Human Immunodeficiency Virus ViiV Healthcare|GlaxoSmithKline February 1 2014 Phase 1
NCT02063360 Completed Infection Human Immunodeficiency Virus ViiV Healthcare|GlaxoSmithKline February 1 2014 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

Related Reverse Transcriptase Products0

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID