1. Anti-infection
  2. Reverse Transcriptase
    HIV
  3. Etravirine

Etravirine (Synonyms: R165335; TMC125)

Cat. No.: HY-90005 Purity: 99.53%
Handling Instructions

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

For research use only. We do not sell to patients.

Etravirine Chemical Structure

Etravirine Chemical Structure

CAS No. : 269055-15-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 166 In-stock
Estimated Time of Arrival: December 31
10 mg USD 151 In-stock
Estimated Time of Arrival: December 31
50 mg USD 378 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

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Description

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

In Vitro

TMC125 is highly active against wild-type HIV-1 (50% effective concentration [EC50]=1.4 to 4.8 nM) and shows some activity against HIV-2 (EC50=3.5 μM). TMC125 also inhibits a series of HIV-1 group M subtypes and circulating recombinant forms and a group O virus. TMC125 has activity for 19 viruses with EC50 of < 5 nM[1].

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[2].

Clinical Trial
Molecular Weight

435.28

Formula

C₂₀H₁₅BrN₆O

CAS No.

269055-15-4

SMILES

N#CC1=CC(C)=C(C(C)=C1)OC2=NC(NC3=CC=C(C=C3)C#N)=NC(N)=C2Br

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (114.87 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2974 mL 11.4869 mL 22.9737 mL
5 mM 0.4595 mL 2.2974 mL 4.5947 mL
10 mM 0.2297 mL 1.1487 mL 2.2974 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

EtravirineR165335TMC125R 165335R-165335TMC 125TMC-125Reverse TranscriptaseHIVHuman immunodeficiency virusInhibitorinhibitorinhibit

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Etravirine
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HY-90005
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